Effect of Lactobacillus plantarum HFY05 on Regulating NF-κ B Pathway Related Inflammatory Response and Inhibiting Thrombosis | Chapter 6 | Application of Probiotics in Exercise and Thrombosis Inhibition

 a

Cardiovascular and cerebrovascular diseases continue to threaten the lives of humans, especially those of middle-aged adults and the elderly. Thrombosis is the main cause of death due to cardiovascular diseases, which includes chronic thrombosis and results in cerebral ischemia, hypoxia, tissue softening, and necrosis. This study investigated the anti-thrombotic potential of Lactobacillus plantarum KFY05 (LP-KFY05) and its underlying mechanism via the NF-κB pathway in a murine carrageenan-induced thrombosis model. Biochemical assays, microscopic examination, qPCR, and western blotting were employed to analyse serum and tissue parameters, while faecal microbial abundance was assessed to determine changes in gut microbiota composition. Results demonstrated that LP-KFY05 significantly reduced tail blackening in thrombotic mice (n=10 per group), prolonged activated partial thromboplastin time (APTT), and decreased thrombin time (TT), fibrinogen (FIB) level, and prothrombin time (PT). Furthermore, LP-KFY05 treatment lowered serum and renal tissue concentrations of tumour necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Histopathological analysis via hematoxylin and eosin staining revealed that LP-KFY05 alleviated renal tissue injury and tail vein thrombosis. qPCR results indicated that LP-KFY05 downregulated mRNA expression of NF-κB p65, IL-6, TNF-α, and interferon-γ (IFN-γ) in renal tissues, as well as NF-κB p65, intercellular adhesion molecule-1 (ICAM-1), vascular cell adhesion molecule-1 (VCAM-1), and E-selectin in tail vein vascular tissues. Western blot analysis confirmed the downregulation of NF-κB protein expression in both renal and tail vein tissues. Additionally, LP-KFY05 increased the abundances of Bacteroidetes, Lactobacillus, and Bifidobacterium, while reducing the abundance of Firmicutes. In conclusion, LP-KFY05 effectively mitigates inflammation and inhibits thrombosis in mice, with high-dose LP-KFY05 exhibiting the most pronounced effects, comparable to those of the positive control drug dipyridamole. However, this study was conducted in a murine model, and further clinical investigations are necessary to confirm the efficacy and safety of LP-KFY05 in humans.

 

 

Author(s) Details

 

Shi Zeng
Department of Neurosurgery, People’s Hospital of Chongqing Banan District, Chongqing, China.

 

Ruokun Yi
Chongqing Collaborative Innovation Center for Functional Food, Chongqing Engineering Research Center of Functional Food, Chongqing Engineering Laboratory for Research and Development of Functional Food, Chongqing University of Education, Chongqing, China.

 

Fang Tan
Department of Public Health, Our Lady of Fatima University, Valenzuela, Philippines.

 

Peng Sun
Chongqing Collaborative Innovation Center for Functional Food, Chongqing Engineering Research Center of Functional Food, Chongqing Engineering Laboratory for Research and Development of Functional Food, Chongqing University of Education, Chongqing, China.

 

Qiang Cheng
Department of Neurosurgery, People’s Hospital of Chongqing Banan District, Chongqing, China.

 

Xin Zhao
Chongqing Collaborative Innovation Center for Functional Food, Chongqing Engineering Research Center of Functional Food, Chongqing Engineering Laboratory for Research and Development of Functional Food, Chongqing University of Education, Chongqing, China.

 

Please see the book here :- https://doi.org/10.9734/bpi/mono/978-81-998509-9-6/CH6

Bioactivity of Mineral-Enriched Organic Carrots: Anticancer Effects in HT-29 Cells and Anti-Inflammatory Activity in Mice Splenocytes | Chapter 2 | Molecular Mechanisms and Signaling Pathways of the Anti-inflammatory Effects of Functional Foods

 

Carrot (Daucus carota) is a globally important root vegetable with diverse biological activities. Currently, organic cultivation places a greater focus on ecosystem health by using natural organic fertilisers and organic pesticides, such as animal and plant-based fertilisers and natural insecticides, reducing reliance on chemical substances, promoting soil health and ecological balance, and providing healthier and environmentally friendly agricultural products.  However, research on the anti-inflammatory properties of carrots, especially comparing traditionally cultivated and organically grown varieties, remains limited. Therefore, this study examined the anticancer and anti-inflammatory properties of carrots cultivated using Natural Dream Cultivation (NC), an organic farming method enhanced with mineral supplementation. The inhibitory effect of NC carrot extracts on HT-29 human colon cancer cells was assessed via MTT assay, while qPCR was used to evaluate mRNA expression of cell cycle- and apoptosis-related genes. Nitric oxide (NO) concentration was measured using the Griess method. In LPS-induced mouse splenocytes, levels of inflammatory cytokines were determined by enzyme-linked immunosorbent assay, and natural killer (NK) cell activity was evaluated via LDH release assay. Results showed that NC significantly suppressed cancer cell proliferation. It up-regulated the expression of cell cycle arrest genes (p53, p21) and pro-apoptotic genes (Bim, Bad, Bax, Bak, caspase-9, caspase-3), while down-regulating anti-apoptotic genes (Bcl-2, Bcl-xL). Furthermore, NC treatment inhibited NO production and reduced the release of inflammatory cytokines (TNF-α, IL-6, IL-1β, IFN-γ, IL-12) in LPS-stimulated splenocytes. NC also promoted NK cell activation. By elucidating the inhibitory effects on cancer cells and modulation of inflammatory responses, this study reveals potential mechanisms behind the anticancer and anti-inflammatory activities of carrots. The innovative mineral-enhanced organic cultivation method presented here offers new possibilities for developing carrots as a functional food candidate supported by in vitro and ex vivo bioactivity relevant to cancer- and inflammation-associated pathways. These findings may inform the future design of dietary research hypotheses and preclinical studies, pending validation in animal models and clinical settings.

 

Author(s) Details

Yanni Pan
Collaborative Innovation Center for Child Nutrition and Health Development, Chongqing Engineering Research Center of Functional Food, Chongqing Engineering Laboratory for Research and Development of Functional Food, Chongqing University of Education, Chongqing 400067, China and Department of Food Science and Biotechnology, CHA University, Seongnam 13488, Republic of Korea.

 

Yeon-Jun Lee
Department of Food Science and Biotechnology, CHA University, Seongnam 13488, Republic of Korea.

 

Sin-Il Sin
Agriculture Research Center for Carbon Neutral and Healing, Gurye 57607, Republic of Korea.

 

Seung-Hwan Park
Agriculture Research Center for Carbon Neutral and Healing, Gurye 57607, Republic of Korea.

 

Kun-Young Park

Collaborative Innovation Center for Child Nutrition and Health Development, Chongqing Engineering Research Center of Functional Food, Chongqing Engineering Laboratory for Research and Development of Functional Food, Chongqing University of Education, Chongqing 400067, China and Graduate School of Integrative Medicine, CHA University, Seongnam 13488, Republic of Korea.

 

Please see the book here :- https://doi.org/10.9734/bpi/mono/978-81-998509-0-3/CH2

 

Dermatological Applications of Punica granatum: Phytochemistry and Therapeutic Potential in Skin Disorders |Chapter 7 | Pharmaceutical Science: New Insights and Developments Vol. 9

 

Pomegranate (Punica granatum) is a popular fruit known for its rich nutritional value and diverse bioactive compounds. The fruit has many potential health benefits, and it has been evaluated in clinical trials for different diseases. There are limited studies investigating the comprehensive use of pomegranate in cosmetic and dermatological applications. This chapter presents a comprehensive review of the dermatological applications and therapeutic potential of Punica granatum, with a focus on its phytochemistry and mechanisms of action. The increasing use of botanical extracts in skincare and cosmetic formulations underscores the relevance of Punica granatum, a plant native to Iran. A structured literature search was conducted across various databases, including PubMed, ScienceDirect, Springer, and Google Scholar, to evaluate evidence from preclinical and clinical studies. Key findings indicate that pomegranate extracts and their bioactive compounds—particularly punicalagin, ellagic acid, and anthocyanins—exhibit significant antioxidant, anti-inflammatory, antimicrobial, and wound-healing properties. Specific dermatological benefits explored include the promotion of wound repair, inhibition of acne pathogenesis, protection against UV-induced photoaging, skin brightening, and management of inflammatory skin conditions such as atopic dermatitis. This review consolidates current scientific research to highlight the promising role of Punica granatum as a multifunctional agent in the treatment and prevention of skin disorders, supporting its continued integration into dermatological and cosmetic products.

 

Author(s) Details

Farshad Akbarnejad
Dr. Akhavi Laboratory Co, Scientific Department, Tehran, Iran.

 

 

Please see the book here :- https://doi.org/10.9734/bpi/psnid/v9/6868

Prominent Use of Malva sylvestris L in Dermatology | Chapter 8 | Research Perspective on Biological Science Vol. 9

 

Malva sylvestris L. (common mallow) is a flowering plant belonging to the Malvaceae family. The plant has laxative, diuretic, spasmogenic and laxative properties. This plant has a rich history in traditional medicine across Asia, Europe, and Africa, and presents a compelling natural therapeutic agent for a wide range of dermatological conditions. Among the various species used in herbal medicine, M. sylvestris stands out for its diverse usage, which has been documented since 3000 BC. In Iran, M. sylvestris is recognised as an edible herb and has been consumed raw in various vegetable salads; however, it is most commonly used as a medicinal herb. This review consolidates scientific evidence to validate its traditional use in treating wounds, eczema, atopic dermatitis, and skin infections. The therapeutic efficacy of M. sylvestris is primarily attributed to its diverse profile of bioactive phytoconstituents. Key among these are mucilaginous polysaccharides, which provide emollient and soothing effects for sensitive skin and irritations; flavonoids (e.g., gossypetin, malvidin 3-glucoside) and phenolic compounds, which exert potent antioxidant and anti-inflammatory activities by scavenging free radicals and modulating inflammatory mediators like PGE₂; and tannins and essential oils, which contribute to its significant antibacterial effects against pathogens such as Staphylococcus aureus. Preclinical and clinical studies demonstrate that topical applications of M. sylvestris extracts promote wound healing by enhancing collagen deposition and fibroblast proliferation, reduce inflammation and pruritus in atopic dermatitis, and accelerate burn wound contraction, often showing superior efficacy compared to standard treatments like silver sulfadiazine. The convergence of its demulcent, antibacterial, anti-inflammatory, and antioxidant properties, underpinned by its distinct phytochemical composition, justifies its traditional use and positions M. sylvestris as a versatile and effective candidate for integrative dermatological therapy. Future studies, including well-designed clinical trials and standardised extract formulations, are required to validate the therapeutic efficacy of Malva sylvestris in dermatological conditions.

 

 

Author(s) Details

Farshad Akbarnejad
Scientific Department, Rayka Shimi Saba Pharmaceutical & Hygienic Knowledge-Based Co., Tehran, Iran.

 

Please see the link:- https://doi.org/10.9734/bpi/rpbs/v9/6800

 

Plant-Based Natural Compounds for Wound Healing: A Comprehensive Review | Chapter 6 | Research Perspectives of Microbiology and Biotechnology Vol. 4

The study presents a comprehensive assessment of plant-sourced natural compounds for wound healing, encompassing their chemical origins and the biological processes involved in their therapeutic effects on wound healing. Wound healing involves multiple stages, and any interruption during this sequence can result in improper wound healing. Restoration of the structure and function of damaged tissues, which is an intricate process, is governed by the discharge of multiple cytokines and growth factors at the site of injury. Wound healing may benefit greatly from a variety of plants or compounds derived from plants with high concentrations of antioxidants as well as anti-inflammatory, immunomodulatory, and antibacterial properties.

 

Author(s) Details

Monika

Department of Bioscience and Biotechnology, Banasthali Vidyapith, Banasthali-304022, Rajasthan, India.

Surabhi Bajpai

Department of Bioscience and Biotechnology, Banasthali Vidyapith, Banasthali-304022, Rajasthan, India.

Rakesh Mishra

Institute for Stem Cell Biology and Regenerative Medicine (inStem), NCBS Campus, Bengaluru -560065, Karnataka, India.

 

Please see the link:- https://doi.org/10.9734/bpi/rpmab/v4/774

Spasmolytic Activity, Anti-Inflammatory Potential, and Molecular Docking Studies of Anthranilic Acid Hybrids | Chapter 8| Chemical and Materials Sciences - Developments and Innovations Vol. 3

Anthranilic acid and its analogs have an impressive biological profile; its structural nucleus has been thoroughly studied for the development of pharmaceuticals. Due to the predicted in silico methods spasmolytic activity, we synthesized a hybrid molecule of anthranilic acid and substituted 2-phenylethylamines. Phenylethylamines are serotonin agonists and are building blocks of isoquinoline alkaloids. Therefore, the synthesis of a new hybrid molecule of anthranilic acid and substituted 2-phenylethylamines, is extremely interesting in view of what properties the newly obtained molecule would inherit from both fragments. The current study has shifted towards the synthesis of novel hybrids as spasmolytic and anti-inflammatory agents. DFT calculations and docking simulations were performed on the synthesized compounds. The obtained results from all the experiments demonstrate that the hybrid molecule and its diamides inherit spasmolytic, antimicrobial, and anti-inflammatory capabilities, making them excellent candidates for future medications. Based on the experimental data, we can conclude that a collection of Novel 2-phenylethylamine hybrids were successfully synthesized and they can be considered as antispasmodics and anti-inflammatory drug candidates – alternatives to current therapeutics.

 

 

Author(s) Details

 

Miglena Milusheva

Department of Organic Chemistry, Faculty of Chemistry, University of Plovdiv, 4000 Plovdiv, Bulgaria and Department of Bioorganic Chemistry, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria.

Vera Gledacheva

Department of Medical Physics and Biophysics, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria.

Iliyana Stefanova

Department of Medical Physics and Biophysics, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria.

Mehran Feizi-Dehnayebi

Department of Organic Chemistry, Faculty of Chemistry, Alzahra University, Tehran, Iran.

Mina Todorova

Department of Organic Chemistry, Faculty of Chemistry, University of Plovdiv, 4000 Plovdiv, Bulgaria.

Yulian Tumbarski

Department of Microbiology, Technological Faculty, University of Food Technologies, 4002 Plovdiv, Bulgaria.

Ghodsi Mohammadi Ziarani

Department of Organic Chemistry, Faculty of Chemistry, Alzahra University, Tehran, Iran.

Stoyanka Nikolova

Department of Organic Chemistry, Faculty of Chemistry, University of Plovdiv, 4000 Plovdiv, Bulgaria.

 

Please see the link:- https://doi.org/10.9734/bpi/cmsdi/v3/11872F

Plant-Based Natural Compounds for Wound Healing: A Comprehensive Review | Chapter 6 | Research Perspectives of Microbiology and Biotechnology Vol. 4

 

The study presents a comprehensive assessment of plant-sourced natural compounds for wound healing, encompassing their chemical origins and the biological processes involved in their therapeutic effects on wound healing. Wound healing involves multiple stages, and any interruption during this sequence can result in improper wound healing. Restoration of the structure and function of damaged tissues, which is an intricate process, is governed by the discharge of multiple cytokines and growth factors at the site of injury. Wound healing may benefit greatly from a variety of plants or compounds derived from plants with high concentrations of antioxidants as well as anti-inflammatory, immunomodulatory, and antibacterial properties.

 

 

Author(s) Details

 

Monika

Department of Bioscience and Biotechnology, Banasthali Vidyapith, Banasthali-304022, Rajasthan, India.

Surabhi Bajpai

Department of Bioscience and Biotechnology, Banasthali Vidyapith, Banasthali-304022, Rajasthan, India.

Rakesh Mishra

Institute for Stem Cell Biology and Regenerative Medicine (inStem), NCBS Campus, Bengaluru -560065, Karnataka, India.

 

Please see the link:- https://doi.org/10.9734/bpi/rpmab/v4/774

The Ability of a Methylated Extract of Hibiscus plantifolius to Reduce Inflammation | Chapter 12 | Pharmaceutical Science: New Insights and Developments Vol. 4

Background: Inflammation, a complex reaction to injurious agents such as microbes, usually necrotic cells consisting of vascular response, leads to accumulation of fluids, migration, and activation of leukocytes and systemic reactions. Inflammation is fundamentally a protective response, the ultimate goal of which is to rid the organism of both the initial causes of cell injury such as microbes and toxins and the consequence of injuries such as necrotic cells and tissue.

 

Objective: The goal of this study was to find out if a methanolic extract of Hibiscus plantifolius (MEHP), a plant in the Malvaceae family, could reduce inflammation.

 

Methods: One kilogram of the shade-dried stem portion of H. plantifolius was ground into a powder and soxhleted with methanol. In order to produce crude methanol extract, which was then used for additional research, the extract was concentrated using a rotary evaporator at 40°C and reduced pressure until it was solvent-free. Carrageenan-induced paw edema in rats at dose levels of 50, 150, and 300 mg/kg was used to study the anti-inflammatory impact. Research on acute oral toxicity was also conducted.

 

Results: The findings show that the increase in paw edema at the fourth hour was significantly (p<0.001) inhibited by MEHP, 300 mg/kg.

 

Conclusion: The experimental study's findings demonstrated that MEHP had strong anti-inflammatory properties. The presence of flavonoids, tannins, and phenolic compounds which were present in MEHP exhibited antioxidant activity.

 

Author (s) Details

SOWJANYA KA
Department of Pharmaceutical Chemistry, Nirmala College of Pharmacy, Atmakur, Mangalagiri, Andhra Pradesh, India.

P.PARVATHI
Department of Pharmaceutical Analysis, Nirmala College of Pharmacy, Atmakur, Mangalagiri, Andhra Pradesh, India

 

P.ROJA DURGA BHAVANI
Doctor of Pharmacy, Nirmala College of Pharmacy, Atmakur, Mangalagiri, Andhra Pradesh, India.

 

CH.SHAINY GRACE
Doctor of Pharmacy, Nirmala College of Pharmacy, Atmakur, Mangalagiri, Andhra Pradesh, India.

 

DEEPIKA
Bachelor of Pharmacy, Nirmala College of Pharmacy, Atmakur, Mangalagiri, Andhra Pradesh, India.

 

Please see the book here:- https://doi.org/10.9734/bpi/psnid/v4/4779

 

Current Developments in the Biological Functions of 1,3,4-Thiadiazoles: A Review | Chapter 3 | Pharmaceutical Science: New Insights and Developments Vol. 5

1,3,4-thiadazoles have become an important class of heterocycles and a great interest of researches because of their broad types of biological activity. The 1,3,4-thiadiazole ring's exceptional flexibility and wide range of therapeutic activity have made it an intriguing pharmacophore. This study clarifies the inherent characteristics of this five-membered heterocycle, emphasizing its polar and aromatic nature as well as its adaptability to changes that optimise its biological effect.  The broad spectrum of pharmacological action that 1,3,4-thiadiazole compounds display, including antimicrobial, antifungal, antiviral, anticancer, and anti-inflammatory effects was discussed. In this study, the maximal electroshock (MES) model was employed to evaluate the anticonvulsant potential of thiadiazole-based compounds, while their antiviral efficacy was assessed using the Tobacco Mosaic Virus (TMV) model. Numerous studies have also demonstrated the anticancer, anti-inflammatory, antifungal, antiviral, antibacterial, anticonvulsant, and antiparasitic properties of molecules having thiadiazole rings. Additionally, this study highlights the enormous potential for developing targeted medicines with improved effectiveness and selectivity and examines the intriguing possibilities of this flexible framework in the next drug discovery and development. Overall, this analysis highlights how important 1,3,4-thiadiazole is as a flexible pharmacophore that has the potential to completely change the field of medicine.

 

Author (s) Details

P. Indhumathy
Department of Pharmaceutical Chemistry and Analysis, School of Pharmaceutical Sciences, Vels Institute of Science Technology and Advanced Studies, Chennai, Tamil Nadu, India.

 

R. Gandhimathi
Department of Pharmaceutical Chemistry and Analysis, School of Pharmaceutical Sciences, Vels Institute of Science Technology and Advanced Studies, Chennai, Tamil Nadu, India.

 

Please see the book here:- https://doi.org/10.9734/bpi/psnid/v5/4810

Biological Activities of Natural Products | Chapter 6 | Natural Products Chemistry: From Discovery to Applications, Edition 1

Natural products exhibit a wide range of biological activities that have proven beneficial in drug discovery, agriculture, and the cosmetic industries. The majority of these compounds are bioactive from plants, microorganisms, and marine organisms, demonstrating antimicrobial activity, antioxidant properties, anti-inflammatory effects, anticancer potential, and immunomodulatory activity. Owing to variations in their molecular characteristics, they are capable of interacting with various biological targets, thereby producing a therapeutic effect. This abstract outlines the actions associated with these activities, particularly in the production of pharmaceuticals and health products. Understanding the biological processes utilized by natural products is essential for optimizing their effectiveness in disease management and enhancing human welfare.

 

Author (s) Details

 

Vidivay
Department of Chemistry, Dharma Samaj College, Aligarh, Uttar Pradesh -202001, India.

 

Please see the book here:- https://doi.org/10.9734/bpi/mono/978-93-48388-70-4/CH6

Docosanoic Acid, Quercetin, and Vitexin from Dennettia tripetala Bak. f.: Isolation, Characterization, and Evaluation of their In-vivo Anti-inflammatory and Analgesic Effects | Chapter 8 | Medical Science: Trends and Innovations Vol. 11

Among the medicinal plants that have found usefulness in ethnomedicine and attracted scientific interests is Dennettia tripetala Baker f. (Annonaceae). D. tripetalais widely used in African traditional medicine for managing diabetes, inflammation, pain, and other ailments. This study aimed to isolate and characterize bioactive compounds from the root and stem bark of D. tripetalaand evaluate their anti-inflammatory and analgesic properties through in vivo models. The stem bark and root of D. tripetalawere collected from Itak Ikot Akap village in Ikono Local Government Area, Akwa Ibom State, Nigeria. The plant materials were extracted using 70% aqueous methanol, and the extracts were partitioned into n-hexane, dichloromethane, ethyl acetate, and n-butanol fractions. Compounds were isolated through open-column chromatography and thin layer chromatography and characterized using ¹H NMR, ¹³C NMR, and FTIR spectroscopy. Anti-inflammatory activity was evaluated using egg albumin and xylene-induced oedema models, while analgesic activity was assessed using formalin-induced paw licking and hot plate tests, respectively. Data were analyzed using one-way ANOVA, with significance level set at p<0.05. The dichloromethane and ethyl acetate fractions exhibited the highest anti-inflammatory activity, with the root extract at 447 mg/kg significantly inhibiting egg albumin-induced oedema by 81% at 5 hours, compared to 77% for aspirin. In the xylene-induced oedema model, the root extract at 670 mg/kg achieved 76% inhibition, comparable to the standard drug. Analgesic effects were most pronounced in the formalin test, where the root extract reduced paw licking duration by 85% in the late phase. ¹H NMR, ¹³C NMR, and FTIR spectroscopy were utilized in identification of compounds. Docosanoic acid showed ester signals (C=O at 1736 cm⁻¹, 174.0 ppm). Quercetin had hydroxyl signals (12.5–9.3 ppm) and a carbonyl at 175.9 ppm, while vitexin displayed glycosidic signals (3.85–3.24 ppm) and a carbonyl at 182.6 ppm, confirming their bioactive potential. These findings validate the traditional use of D. tripetalaand highlight its potential as a source of natural therapeutic agents.

 

Author (s) Details

 

Enema, Onojah John
Department of Pharmacognosy and Natural Medicine, Faculty of Pharmacy, University of Uyo, Uyo, Nigeria.

 

Umoh, Uwemedimo Francis
Department of Pharmacognosy and Natural Medicine, Faculty of Pharmacy, University of Uyo, Uyo, Nigeria.

 

Ekarika, C. Johnson
Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, University of Uyo, Uyo, Nigeria.

 

Khalid, Doudin
Department of Mathematical and Physical Sciences, The University of Sheffield, Sheffield, S3 7HF, United Kingdom.

 

Johnny, I. Imoh
Department of Pharmacognosy and Natural Medicine, Faculty of Pharmacy, University of Uyo, Uyo, Nigeria.

 

Please see the book here:- https://doi.org/10.9734/bpi/msti/v11/4839

Functionalization of Natural Compounds to Enhance the Bioactivity of Zerumbone in Cancer Chemotherapy | Chapter 4 | Recent Developments in Chemistry and Biochemistry Research Vol. 10

The alkylation reaction was employed to conjugate zerumbone with 3-substituted quinazolinone-4(3H)-ones and quinolines, resulting in the synthesis of 11 novel conjugates. These conjugates were thoroughly characterized using 1D-, 2D-NMR, and HRMS spectral data. Their enhanced bioactivity was evaluated through anti-inflammatory assays, specifically by inhibiting NO production in RAW 267.4 cells. Additionally, their cytotoxic activity was assessed against three human cancer cell lines: HepG2, SK-LU-1, and MCF-7. The results demonstrated that all 11 conjugates exhibited significantly potent cytotoxic activity, with IC50 values ranging from 1.01 to 9.86 µg/mL, surpassing the efficacy of the parent compound zerumbone. Furthermore, in silico studies, including EGFR inhibitory activity through docking and molecular dynamics simulations, were conducted to identify the most potent compounds. These studies highlighted the key interactions of zerumbone derivatives 16a-k with critical amino acids in the active site of the EGFR (PDB ID 4HJO) protein.

 

Author (s) Details

Ngoc Hung Truong
Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology, 1H Building, 18 Hoang Quoc Viet Street, Cau Giay, Hanoi, 100000, Vietnam.

 

Duc Anh Le
Institute of Chemistry and Material, Academy of Military Science and Technology, 17 Hoang Sam Street, Cau Giay, Hanoi, 100000, Vietnam.

 

Thi Ha Vu
Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology, 1H Building, 18 Hoang Quoc Viet Street, Cau Giay, Hanoi, 100000, Vietnam.

 

Thi Inh Cam
Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology, 1H Building, 18 Hoang Quoc Viet Street, Cau Giay, Hanoi, 100000, Vietnam.

 

Huu Nghi Do
Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology, 1H Building, 18 Hoang Quoc Viet Street, Cau Giay, Hanoi, 100000, Vietnam.

 

Manh Cuong Nguyen
Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology, 1H Building, 18 Hoang Quoc Viet Street, Cau Giay, Hanoi, 100000, Vietnam.

 

Khac Vu Tran
Hanoi University of Science and Technology, 1 Dai Co Viet Str., Hai Ba Trung Street, Hanoi 100000, Vietnam.

 

Hanh Nguyen Tran
University of Science and Technology of Hanoi, A21 Building, 18 Hoang Quoc Viet Street, Cau Giay, Hanoi 100000, Vietnam.

 

Van Chung Pham
Applied Medicinal Chemistry and Pharmaceutical Technology JSC, 45/24 Dien Bien Phu Street, Ngo Quyen, Hai Phong 180000, Vietnam.

 

Van Chinh Luu
Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology, 1H Building, 18 Hoang Quoc Viet Street, Cau Giay, Hanoi, 100000, Vietnam.

 

Please see the book here:- https://doi.org/10.9734/bpi/rdcbr/v10/3608

Spasmolytic Activity, Anti-Inflammatory Potential, and Molecular Docking Studies of Anthranilic Acid Hybrids | Chapter 8| Chemical and Materials Sciences - Developments and Innovations Vol. 3

 Anthranilic acid and its analogs have an impressive biological profile, its structural nucleus has been thoroughly studied for the development of pharmaceuticals. Due to the predicted in silico methods spasmolytic activity, we synthesized a hybrid molecule of anthranilic acid and substituted 2-phenylethylamines. Phenylethylamines are serotonin agonists and are building blocks of isoquinoline alkaloids. Therefore, the synthesis of a new hybrid molecule of anthranilic acid and substituted 2-phenylethylamines, is extremely interesting in view of what properties the newly obtained molecule would inherit from both fragments. The current study has shifted towards the synthesis of novel hybrids as spasmolytic and anti-inflammatory agents. DFT calculations and docking simulations were performed on the synthesized compounds. The obtained results from all the experiments demonstrate that the hybrid molecule and its diamides inherit spasmolytic, antimicrobial, and anti-inflammatory capabilities, making them excellent candidates for future medications. Based on the experimental data, we can conclude that a collection of Novel 2-phenylethylamine hybrids were successfully synthesized and they can be considered as antispasmodics and anti-inflammatory drug candidates – alternatives to current therapeutics.

 

Author (s) Details

Miglena Milusheva,
Department of Organic Chemistry, Faculty of Chemistry, University of Plovdiv, 4000 Plovdiv, Bulgaria and Department of Bioorganic Chemistry, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria.

Vera Gledacheva,
Department of Medical Physics and Biophysics, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria.

Iliyana Stefanova,
Department of Medical Physics and Biophysics, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria.

Mehran Feizi-Dehnayebi,,
Department of Organic Chemistry, Faculty of Chemistry, Alzahra University, Tehran, Iran.

Mina Todorova
Department of Organic Chemistry, Faculty of Chemistry, University of Plovdiv, 4000 Plovdiv, Bulgaria.

Yulian Tumbarsk,
Department of Microbiology, Technological Faculty, University of Food Technologies, 4002 Plovdiv, Bulgaria.

Ghodsi Mohammadi Ziarani,
Department of Organic Chemistry, Faculty of Chemistry, Alzahra University, Tehran, Iran.

Stoyanka Nikolova,
Department of Organic Chemistry, Faculty of Chemistry, Alzahra University, Tehran, Iran.

 

Please see the book here:-  https://doi.org/10.9734/bpi/cmsdi/v3/11872F

Molecular Docking, Synthesis, Characterization of Sulphamethoxazole Schiff Base Metal Complexes and its Antibacterial, Anti-Inflammatory and Anti Depressant Activity | Chapter 9 | Advanced Concepts in Pharmaceutical Research Vol. 1

 The aim of the study is to create mineral complexes that are above schiff's base using metals like copper, hardware, and metallic material, as well as to synthesis schiff's base, an uncontaminated medication, utilizing aromatic organic compounds like p-diethyl amino benzyldehyde and p-dimethyl amino benzyldehyde. Schiff bases are adjustable organic compounds that are widely used and synthesized by abridgment reaction of various amino compound with aldehydes or ketones known as imine. Schiff base ligands are thought-out as privileged ligands as they are plainly synthesized by condensation. The combined schiff’s bases were regenerate to allure ion Schiff bases by treating with methyl group halide. The ion Schiff bases were rejuvenate to metal composites by treating with metals like CuCl2, ZnCl2 and CdCl2. All the combined compounds were characterised by Elemental analysis, IR and 1H proton drawing resonance.  Docking study was performed to experience the interaction of binding sites accompanying protein receptor using MAO-B enzymes (PDB ID: 2BK5) and COX-2 enzyme (PDB ID: 5IKR) by Virtual Screening operating system for Computational Drug Discovery. Synthesized metal aggregates were evaluated for antibacterial, antagonistic inflammatory and antidepressant endeavor. Copper metal complexes demonstrated potent decontaminating and anti-inflammatory endeavor. Significant anti-sedative activity was shown for 2A2 and 2B2 metallic mineral metal aggregates.

Author(s) Details:

Mugdivari Sangeetha,
Department of Pharmaceutical Chemistry and Analysis, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies (VISTAS), Pallavaram, Chennai-600117, Tamilnadu, India.

R. Gandhimathi,
Department of Pharmaceutical Chemistry and Analysis, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies (VISTAS), Pallavaram, Chennai-600117, Tamilnadu, India.

Shushma Voggu,
Department of Pharmaceutical Chemistry and Analysis, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies (VISTAS), Pallavaram, Chennai-600117, Tamilnadu, India.

Jammula Prathyusha,
Department of Pharmaceutical Chemistry and Analysis, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies (VISTAS), Pallavaram, Chennai-600117, Tamilnadu, India.

Please see the link here: https://stm.bookpi.org/ACPR-V1/article/view/12080

Strong Anti-inflammatory Effect of Soluble Curcumin Shown at Cellular Level | Chapter 11 | Current Progress in Medicine and Medical Research Vol. 8

 This phase aims to explore potential of a suitable drug molecule that can symbolize an ideal candidate for bringing to bear its therapeutic conduct in order to cure or manage pathological conditions at instigative levels. Inflammatory mechanisms have combine of the strongest underlying creative factors private of the diseases. Atherosclerosis is individual such inflammatory synopsis wherein Endothelial container (EC) activation and chronic swelling can cause the initiation and progress of the disease. A promising competitor medicine accompanying few negative effects is curcumin (CM). However, its healing usage is forced by poor water solubility, a lack of bioavailability, and important hydrolytic breakdown. Conjugation of CM to Albumin (Alb) producing CM-Alb increases the solubility of the potential drug in addition to targeted drug transfer with negligible antagonistic effects from the drug one who carries or transmits something. This study evaluates an albumin-CM conjugate for cellular rude answer demonstrating bioavailability, deciding the non-cytotoxic concentrations and anti-inflammatory answer in human in the middle vein endothelial cells (HUVECs). The maximum indulged biocompatible dose driven in HUVEC (EC) culture is 30µM; therefore, this study evaluates an anti-inflammatory answer at non-toxic concentrations. The experiments utilizing fluorescence microscopy and flow cytometry confirmed the endocytosis of glowing-tagged CM-Alb and granted comparable cellular rude answer of native albumin. Cytokine- induced incitement of inflammation in EC culture was patterned as in vitro model for judging the response to CM-Alb. A important increase in the expression of VCAM-1 in EC upon incubating accompanying TNF-α for a period of 24h gives a good model method to study the effect of the anti-inflammatory drug particle. Further, the treatment of swelling-induced ECs with CM-Alb combine at 5, 10, 20µM concentrations down-controlled the expression of VCAM-1 significantly distinguished to the TNF-α treated containers. Expressions of markers at a protein level in cytokine-mobilized EC drop down to normalcy when doctored with CM-Alb. In the swelling-induced culture example, the improved liquid solubility and receptor-mediated absorption of the CM- Alb compound by ECs developed in an anti-instigative response, suggesting the possibility for further research as an drip medicinal expression.

Author(s) Details:

Deepa Sathee,
Division of Thrombosis Research, Biomedical Technology Wing, Sree Chitra Tirunal Institute for Medical Sciences and Technology, Thiruvananthapuram, Kerala, India.

Lissy Kalliyana Krishnan,
Division of Thrombosis Research, Biomedical Technology Wing, Sree Chitra Tirunal Institute for Medical Sciences and Technology, Thiruvananthapuram, Kerala, India.

Please see the link here: https://stm.bookpi.org/CPMMR-V8/article/view/11742

Evaluation of Phytochemical Composition, Safety Profile, Analgesic Properties, and Anti-inflammatory Effects of Ethanol Extract of Allium fistulosum L. | Chapter 3 | Novel Aspects on Pharmaceutical Research Vol. 5

 The study was transported to evaluate the phytochemical, security profile, painkiller, and anti-instigative effects of A. fistulosum. Allium fistulosum, a perpetual herb in the type Allium of the Alliaceae family, is secondhand widely as an ingredient in Chinese, Japanese, and Korean food. In addition, A. fistulosum has been as a rule applied to treat coarse colds, headache, intestinal pain, and cardiovascular disease. A total of 50 rodent were separated into five groups. Group 1 mammals were given, 5 ml/kg of common saline verbally, when in fact groups 2, 3, and 4 were given Ethanol extract of A. fistulosum at a application of 200, 400, and 600 mg/kg, respectively. Animals of group 5 were executed the standard drug Aspirin at a dose of 300 mg/kg verbally. Aspirin 300 mg/kg was given verbally as a standard drug to a group of 5 animals. An antagonistic-inflammatory effect was completed activity on 50 rats. 1% carrageenan was used to induce edema in the fondle. Group 1 acted as a control group inasmuch as the other three groups taken A. fistulosum at a dose of 200, 400, and, 600 mg/kg. The having five of something group was given the standard drug Ibuprofen. The elements of the ethanol extract of A. fistulosum were labeled using the phytochemical reasoning. The screening shows the attendance of pharmacologically potent elements such flavonoids, sugars, amino acids, glycosides, phenols, and tannins. The present study told that the therapeutic plant reduces pain completely three doses when compared accompanying the animal that received rational saline. The intoxicating extracts of A.fistulosum showed a meaningful anti-instigative effect from 2 hrs to 24 employment recruiting and management. However, the anti-instigative effect of A.fistulosum at 400mg/kg was highly important at 5 hours, while the anti-angering effect of A.fistulosum at 600mg/kg demonstrated highly important at 5hr and 24 hours.The safety description of A. fistulosum was accessed by Lorke’s pattern which was erect safe at the discussed dose. Anti-instigative and analgesic features could be from the presence of miscellaneous phytochemical substances. Although more studies are necessary with an raised sample size because very limited news is available to date.

Author(s) Details:

Syeda Afroz  ,
Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, Pakistan.

Shireen Nazir,
Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, Pakistan.

Azmat Ara,
Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, Pakistan.

Please see the link here: https://stm.bookpi.org/NAPR-V5/article/view/11047

A Critical Examination of the Potential Benefits of Theophylline on Extended Acute Inflammation in Old Age | Chapter 15 | Novel Aspects on Pharmaceutical Research Vol. 3

 This episode presents a critical review of the potential benefits of theophylline by way of to reduce the burden of post-acute redness in older age groups. A supporting-inflammatory state often perseveres, or is extended, following in position or time sepsis, trauma and added acute sicknesses in old age, particularly above the age of 80 age. The presence of swelling at above-baseline amplitudes or excessive event is associated with a bigger likelihood of delirium, eating disorder, unplanned burden loss, lethargy, despair, weakness and added markers of weakness. There is also an association accompanying less favourable clinical consequences and a higher risk of losing individual independence. Theophylline has happened shown to have an anti-instigative effect, probably arbitrated through the induction of histone deacetylase-dependent deoxyribonucleic acid switching in invulnerable competent cells, that has happened observed at basic and whole organism levels. The main effects are a decline in the production and release of TNF, IL-1 and IL-6, accompanying a sequential fall in CRP and increase in IL-10, and a change of invulnerable cells to their antagonistic-inflammatory phenotypes. This occurs when theophylline levels are between 5 and 10 mg/L, which is inferior the range for bronchodilators (10 to 15 mg/L) and presents a relatively reduced risk of toxicity. We hypothesize that low-measure theophylline treatment likely to elderly subjects accompanying acute swelling, for example due to respiring infection, septicaemia or damage, will change the setting of their biochemical status from an incorrectly extended supporting-inflammatory pattern toward a more normalized baseline pattern and therefore reduce the risk of unfavorable clinical outcomes.

Author(s) Details:

S. C. Allen,
University Hospitals Dorset, Bournemouth, UK and Centre for Postgraduate Medical Research and Education, Bournemouth University, Dorset, UK.

G. T. C. Wong,
Faculty of Medicine, University of Hong Kong, Hong Kong SAR, China.

D. Tiwari,
University Hospitals Dorset, Bournemouth, UK and Centre for Postgraduate Medical Research and Education, Bournemouth University, Dorset, UK.

A. Khattab,
Centre for Postgraduate Medical Research and Education, Bournemouth University, Dorset, UK.

J. S. K. Kwan,
Imperial College London, London, UK.

M. Vassallo,
University Hospitals Dorset, Bournemouth, UK and Centre for Postgraduate Medical Research and Education, Bournemouth University, Dorset, UK.

Please see the link here: https://stm.bookpi.org/NAPR-V3/article/view/10890

Brief Overview on Sustained Release Theophylline (SRT): An Older Drug for COPD | Chapter 11 | Novel Aspects on Pharmaceutical Research Vol. 3

 This branch aimed to stress the value of specific a drug which needs to be employed as it has withstood the test momentary and the efficacy and appropriate inclusion concerning this drug may still be the elixir of COPD situation. With the advent of more recent drugs, the treatment of incessant obstructive pulmonary ailment (COPD) is undergoing a tremendous and active revolution. Newer drugs, mainly inhalational, with better operation and reduced side-belongings, are being introduced regularly in the administration of this alternatively difficult- to-treat ailment. We believe that the principle that states that the development of new drugs does not diminish the dispassionate advantage of earlier used one applies to SRT. We try to emphasise the significance of Sustained- Released Theophylline (SRT) in the administration of COPD in this abstract. The endeavour is to orderly emphasize the myriad conduct of SRT which specify relief by diversified means to patients in Acute exacerbations of Chronic Obstructive Pulmonary Disease (AECOPD).

Author(s) Details:

A. Sharma,
National Institute of Chest Physician, National Institute of Tuberculosis and Respiratory Diseases (NITRD), New Delhi–110030, India.

A. R. Kansal,
National Institute of Tuberculosis and Respiratory Diseases (NITRD), New Delhi–110030, India.

Please see the link here: https://stm.bookpi.org/NAPR-V3/article/view/10886

2-Amino-N-(Substituted Alkyl) Benzoxazole-5- Carboxamide Derivatives as Antiinflammatory and Antioxidant Drugs| Chapter 9 | Current Overview on Pharmaceutical Science Vol. 2

 The objective of the Present work is to synthesize, characterization and Pharmacological evaluation of 2-Amino-N-(substituted alkyl) benzoxazole-5- carboxamides for anti-inflammatory and antioxidant activities starting from 4-carbomethoxynitrophenol. Evaluation of the compounds showed Vc(R=ethyl), Ve(R=propyl) and Vg (R=diisopropyl) V g (R=propyl) as the most powerful ones. When compared to the standard ascorbic acid, compound Vf (R=isopropyl) demonstrated a substantially higher percentage of free radical scavenging activity with an IC 50 of 4.65. Vf is regarded as a medication that has both anti-inflammatory and antioxidant properties.

Author(s) Details:

Arunadevi Parlapalli,
Department of Pharmaceutical Chemistry, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506009, India.

Kishore,
Department of Pharmaceutical Chemistry, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506009, India

Manasa Cidda,
Department of Pharmaceutical Chemistry, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506009, India.

Sarangapani Manda,
Department of Pharmaceutical Chemistry, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506009, India.

Please see the link here: https://stm.bookpi.org/COPS-V2/article/view/9171

Phytochemical, Pharmacological and Toxicity Study of Siddha Formulation- Neeradimuthu Vallathi Mezhugu| Chapter 8 | Perspective of Recent Advances in Medical Research Vol. 6

 Neeradimuthu Vallathi Mezhugu, a Traditional Siddha Herbo-not organic formulation is indicated for individual type of Vali diseases that is to say Thandaga Vatham. To ensure the security and influence of this medication, pre-dispassionate study was conducted. This Internal Medicine search out be given to patients in a measure of 1 gm. twice a day for a ending of 48 days. According to shastric literature, the trial medications were devised. Analgesic and anti-angering studies were conducted as part of this cure's preclinical safety (acute spoken and repeated spoken toxicity) and efficacy trials. Blood counts and Hb% acted not significantly alter all along the 15-day spoken toxicity study with the medication. In severe experimental inflammatory environments in rats, the test medication demonstrated notable painkiller and anti-angering action. The test drug demonstrated defeater in competition anti-inflammatory venture at the end of the one of four equal parts hour following carrageenan challenge; the mechanism of antagonistic-inflammatory activity of the test drug concede possibility be attributed to allure inhibitory activity on cyclooxygenase (COX) enzymes. Moreover, phytochemical and antioxidant studies revealed allure efficacy in treating Vatha afflictions, particularly Thandaga Vatham.

Author(s) Details:

K. S. Maanickha Chelvi,
Siddha Medicinal Plants Garden, (Under C.C.R.S, Ministry of Ayush, Govt.of India), Mettur, Tamilnadu, India.

V. Mahalakshmi,
Department Siddhar Yoga Maruthuvam, National Institute of Siddha, Chennai, India.

N. J. Muthukumar,
Varma Maruthuvam, National Institute of Siddha, Chennai, India.

Please see the link here: https://stm.bookpi.org/PRAMR-V6/article/view/9275