Prediction of Active Sites of Bitter Taste Receptors through X-ray Crystal Structure of COX-2 Enzyme| Chapter 10 | Pharmaceutical Research - Recent Advances and Trends Vol. 1

 

Conventional taste masking methods including the use of sweeteners, amino acids and flavoring agents are often inadequate in masking the taste of highly bitter substances such as NSAIDs, i.e. ibuprofen, diclofenac sodium, mefenamic acid and etc., especially when these drugs are administered via the orally as syrups or solutions. The X-ray crystal structure of the enzyme COX-2 and the chemical structures of widely used non-steroidal anti-inflammatory drugs (NSAIDs) that bind to COX enzymes and activate the bitter taste receptor TAS2R14 are used in this commentary to discuss a novel approach to be used in the design of active sites of bitter taste receptors, especially TAS2R14. In order to better understand the nature of the interactions between bitter tastants and the chemical groups within the active site of the TAS2R14 receptor, the suggested approach entails docking calculations of the NSAIDs (ligands) to the active site of COX-2.

 

Author(s) Details:

 

Rafik Karaman
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Al-Quds University, Jerusalem, Palestine and Department of Sciences, University of Basilicata, Viadell’Ateneo Lucano 10, 85100, Potenza, Italy.

 

Gennaro Mecca
Ricercatore at EXO Ricerca, Potenza, Italy.

 

Salma Jumaa
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Al-Quds University, Jerusalem, Palestine.

 

Please see the book here:  https://doi.org/10.9734/bpi/prrat/v1/68

Ovarian Cancer Chemotherapy: Targeted Drug Conjugate Systems | Chapter 8 | Pharmaceutical Research - Recent Advances and Trends Vol. 1

 

This chapter discusses advances in ovarian cancer chemotherapy. Ovarian cancer is one of the deadliest diseases that affect women worldwide. Unfortunately, most women with ovarian cancer receive a diagnosis when the disease has progressed to stages 3 or 4, which makes recovery from the disease difficult.  The likelihood of survival is increased in women with early-stage disease who are able to commence treatment early as a consequence of early detection. While the majority of the patients respond well to first-line treatment, i.e. cytoreductive surgery integrated with platinum-based chemotherapy, the rate of disease recurrence is very high and the available treatment options for recurrent disease are not curative. Thus, more potent ovarian cancer therapy options are therefore required. In the fight against ovarian cancer, targeted drug conjugate systems have become a potentially effective therapeutic approach. With the help of these systems, it is possible to administer chemotherapeutic agents to ovarian cancer while protecting healthy cells.  To promote the clinical translation of these drug conjugate systems, it is important to develop and utilize improved pre-clinical tumor models that more accurately mimic ovarian tumors in humans during the preclinical phase of drug development. Additionally, targeted drug conjugate systems improve therapeutic efficacy by facilitating drug accumulation in the tumor and minimizing the incidence of adverse effects. In this chapter, different targeted drug conjugate systems that have been developed or are being developed for the treatment of ovarian cancer are discussed.

 

Author(s) Details:

 

Omotola D. Ogundipe

Department of Pharmaceutical Sciences, Howard University, Washington, DC, USA.

 

Oluwabukunmi Olajubutu
Department of Pharmaceutical Sciences, Howard University, Washington, DC, USA.

 

Simeon K. Adesina
Department of Pharmaceutical Sciences, Howard University, Washington, DC, USA.

 

Please see the book here:  https://doi.org/10.9734/bpi/prrat/v1/8457E

Hepatoprotective Activity of Pongamia pinnata Leaves on Antitubercular Drugs Induced Hepatotoxicity in Rats | Chapter 9 | Pharmaceutical Research - Recent Advances and Trends Vol. 1

 

Aim: The present study highlights the hepatoprotective effect of ethanolic extract of the leaves of the plant Pongamia pinnata on antitubercular drugs (isoniazid and rifampin) induced hepatotoxicity in rats.

Introduction: The hepatotoxic character of a drug is only discovered after it has gone on sale. The most common reason for taking drugs off the market is Drug Induced Liver Injury (DILI), which calls for labelling changes. Research evidence stated that anti-tubercular medication-induced liver damage is mainly due to oxidative stress which primes to cell injury and apoptosis in humans.

Methods: The experiment used five groups of male Wistar rats, each with six animals. Two control groups were given gum acacia and a mixture of isoniazid and rifampin. The two other groups received 200 and 400 mg/kg body weights of ethanolic extract from the leaves of Pongamia pinnata respectively. The fifth group was given silymarin (50mg/kg, p.o.). The concentrations of serum Alanine aminotransferase (ALT), Aspartate aminotransferase (AST), Alkaline Phosphatase (ALP), tissue Malondialdehyde (MDA) and thiols were estimated in the blood of all animals. One-way ANOVA was used for statistical analysis followed by Tukey's test.

Results: When rats were given the mixture of anti-tubercular drugs and high dosage (400 mg/kg) of ethanolic extract of Pongamia pinnata, the blood enzymes showed lower levels than antitubercular treated groups. The co-administration of a high dose of Pongamia pinnata extract with antitubercular drugs reduced MDA levels and elevated thiol levels considerably (p˂ 0.05). These biochemical marker levels however were not adjusted. Conversely, supplementation with Pongamia pinnata attenuated all the changes prompted by the antitubercular drugs and protected the hepatocytes from oxidative destruction revealing the hepatoprotective, antioxidant, antiapoptotic and membrane stabilising action of Pongamia pinnata leaves against drugs-induced toxicity.

Conclusion: In rats, Pongamia pinnata encompasses a partial protective effect against the hepatotoxicity caused by anti-tubercular drugs at high doses.

 

Author(s) Details:

 

Dr. Samba Siva Raju Derangula
Department of Pharmacology, Sri Balaji Medical College, Hospital & Research Institute, Tirupati, Andhra Pradesh, India.

 

Prof. Dr. N. S. Muthiah
Department of Pharmacology, Sree Balaji Medical College & Hospital, Chrompet, Chennai, Tamil Nadu, India.

 

Prof. Dr. H. S. Somashekar
Department of Pharmacology, St. Peter's Medical College, Hospital & Research Institute, Hosur, Tamil Nadu, India.

 

 

Dr. E. Sukumar
Saveetha Institute of Medical & Technical Sciences, Chennai, Tamil Nadu, India.

 

Please see the book here:  https://doi.org/10.9734/bpi/prrat/v1/61

Quantitative Determination of an Antiviral Drug Ganciclovir by Redox-based Spectrophotometric Method | Chapter 11 | Pharmaceutical Research - Recent Advances and Trends Vol. 1

 

Ganciclovir functions as an antiviral medication crucial for averting cytomegalovirus disease among recipients of bone marrow and solid organ transplants. Furthermore, it plays a pivotal role in managing individuals with compromised immune systems by combatting viral infections effectively. This study aims to develop and validate a simple, rapid and sensitive redox-based spectrophotometric method for the quantification of Ganciclovir in pure and pharmaceutical dosage forms. The development process involved utilizing 0.1 M HCl as the solvent along with a combination of ferric chloride and 1,10-phenanthroline as the chromogenic reagent.

After development, the method underwent optimization across various conditions to ensure its efficacy, followed by rigorous statistical validation. Based on the optimization studies, it was determined that the optimal composition for the method included a mixture containing 0.3% w/v of ferric chloride and 0.5% w/v of 1,10-phenanthroline, with a drug-to-reagent mole ratio of 0.5:0.5. When measured at 510.0 nm, the method exhibited linearity within the concentration range of 5.0-30.0 μg/mL for Ganciclovir. Demonstrating its sensitivity, the method showcased a low limit of detection and quantification values, recorded at 0.30 and 0.90 μg/mL, respectively. The validation parameters of the method were found to align with the standards outlined by the ICH guidelines. With a % assay value of 99.2, the method demonstrated its suitability for pharmaceutical formulation analysis. The simplicity of the developed method renders it suitable for application in quality control testing of Ganciclovir within formulations.

 

Author(s) Details:

 

Dr. Naraparaju Swathi, M. Pharm., Ph.D.
Department of Pharmaceutical Chemistry, Gokaraju Rangaraju College of Pharmacy, Hyderabad-500090, Telangana, India.

 

Mrs. Barla Karuna Devi, M. Pharm. (Ph.D.)
Department of Pharmaceutical Chemistry, Gokaraju Rangaraju College of Pharmacy, Hyderabad-500090, Telangana, India.

 

Dr. Anumolu Durga Pani Kumar
Department of Pharmaceutical Analysis, Gokaraju Rangaraju College of Pharmacy, Hyderabad-500090, Telangana, India.

 

Please see the book here:  https://doi.org/10.9734/bpi/prrat/v1/196

Various Approaches and Applications of Artificial Intelligence in Preventing and Detecting Diseases | Chapter 7 | Pharmaceutical Research - Recent Advances and Trends Vol. 1

 

Artificial Intelligence (AI) is increasingly being applied in the advancement of disease prevention and early detection in recent times. The basic concept of artificial intelligence is imitating human intellect in the sense that it can execute tasks, detect patterns, or forecast events via learning from data gathered from diverse sources. It can analyze a lot of medical information, like images and records, to find patterns and identify risks for different diseases. This helps doctors diagnose and treat illnesses sooner, improving morbidity and mortality. Additionally, AI can analyze data from diverse sources like social media and travel patterns to predict and track disease outbreaks, helping public health officials take preventative measures and mitigate the spread of infections. The article explores various approaches and applications of artificial intelligence in preventing and detecting diseases across different medical domains.

 

Author(s) Details:

 

Dr. Kotha Kranthi Kumar (Associate Professor)
Department of Pharmaceutics, College of Pharmaceutical Sciences, Dayananda Sagar University, Bengaluru, Karnataka, India

 

Dr. Sheik Nasar I (Associate Professor)
Department of Pharmacology, East Point College of Pharmacy, East Point Group of Institutions, Jnana Prabha, East Point Campus, Virgo Nagar, Bidarahalli, Karnataka, India.

 

Please see the book here:  https://doi.org/10.9734/bpi/prrat/v1/193

Comparative Study of Analgesic Effect of Moringa oleifera Leaf Extracts with a Standard Drug Aspirin in Animals | Chapter 1 | Pharmaceutical Research - Recent Advances and Trends Vol. 1

 

Background: Pain is a distressing feeling to an intense or damaging stimulus. For centuries, natural analgesic compounds have been used to mediate the pain process, and often with fewer side effects. Moringa oleifera is highly valued with a wide range of medicinal uses. It is abundantly available in tropical and sub-tropical countries. It has been used as an analgesic and anti-inflammatory in Indian folk medicine for centuries. The mechanism of action of analgesic effect is by the phytochemical components of its leaves which contain alkaloids, glycosides, phenols, saponins and tannin.

Methods: Twenty-four Albino mice of either sex, weighing 20-30 grams were selected for the experiment, and divided into 4 equal groups. This experiment was carried out in the mice by using the thermal method of analgesiometer which is Eddy’s Hot Plate method. A thermostatically controlled electrically heated plate was used in this method. Ethanolic and aqueous extracts of Moringa oleifera leaf extracts were compared with aspirin. To the mice of the control group, distilled water was given, for the standard group mice aspirin at the dose of 35 mg/kg was given. For the test groups, aqueous and ethanolic extracts were given at 100 mg/kg dose.

Results: When the analgesic properties of the standard drug aspirin were compared to the analgesic properties of ethanolic and aqueous extracts of Moringa oleifera, the ethanolic extract showed a comparable analgesic effect with aspirin at 90 min. Among these two extracts, the ethanolic extract showed a higher response than the aqueous extract.

Conclusions: When the analgesic properties of the standard drug aspirin were compared to the analgesic properties of ethanolic and aqueous extracts of Moringa oleifera, the ethanolic extract showed a comparable analgesic effect with aspirin at 90 min. Among these two extracts, the ethanolic extract showed a higher response than the aqueous extract. The plant has to be further explored for its phytochemical profile to identify the active.

 

Author(s) Details:

 

Prashanth Kumar Patnaik
Department of Pharmacology, Mahavir Institute of Medical Sciences, Vikarabad, Telangana, India.

 

Mohammed Abdul Majeed
Markapuram Medical College, Andhra Pradesh-523316, India.

 

Bhuvaneshwari
Department of Pharmacology, Osmania Medical College, Hyderabad, Telangana, India.

 

Laksmi Kameswari
Department of Pharmacology, RIMS, Nizamabad, Telangana, India.

 

M. B. Niharika
Department of Pharmacology, Mahavir Institute of Medical Sciences, Vikarabad, Telangana, India.

 

Please see the book here:  https://doi.org/10.9734/bpi/prrat/v1/2965G

A Case Report on Relapsed Chronic Lymphocytic Leukaemia with Concomitant Extensive Chronic Graft Versus Host Disease after Allogeneic Haematopoietic Stem Cell Transplantation Successfully Treated with Oral Venetoclax | Chapter 2 | Recent Updates in Disease and Health Research Vol. 9

 

Chronic lymphocytic leukaemia is the most common leukaemia in adults, and it remains an incurable malignancy with conventional chemoimmunotherapy. A middle-aged gentleman who was diagnosed with high-risk chronic lymphocytic leukaemia (CLL), Rai stage IV, Binet C with del(17p) and del(13q) underwent allogeneic haematopoeitic stem cell transplantation (allo-HSCT) from a human leukocyte antigen (HLA) identical sister. Allogeneic haematopoeitic stem cell transplantation remains the only treatment with curative potential but is associated with high non-relapsed mortality (NRM). The patient developed extensive skin, oral, and liver chronic graft versus host disease (GVHD) and required tacrolimus, mycophenolate mofetil (MMF), and prednisolone. In seventh month after allo-HSCT, the patient presented with systemic symptoms, right cervical lymphadenopathy, splenomegaly, marked pancytopaenia, and elevated lactate dehydrogenase (LDH). Bone marrow study, immunophenotyping (IP), chromosome analysis, and PET-CT scan confirmed relapsed CLL with no evidence of Richter’s transformation or posttransplant lymphoproliferative disease (PTLD). Withdrawal of immunosuppressant (IS) worsened cutaneous and liver GVHD. Chemotherapy was not a suitable treatment option in view of immunodeficiency. The patient underwent extracorporeal photopheresis (ECP) therapy eventually for extensive chronic GVHD, and the IS were gradually tapered to the minimal effective dose. The relapsed CLL was treated successfully with oral venetoclax accessible via a compassionate drug program. This case highlights challenges in managing relapsed CLL and loss of graft-versus-leukaemia (GVL) effect despite extensive chronic GVHD. Venetoclax is an effective and well-tolerated oral novel agent for relapsed CLL after allo-HSCT. In conclusion, this study achieved an excellent outcome when treating a patient with relapsed CLL after allo-HSCT using oral venetoclax and concomitant ECP therapy for extensive chronic GVHD. Venetoclax is a well-tolerated oral novel agent and long-term follow-up is important to ensure the disease achieves a sustained complete remission.

 

Author (s) Details

Ching Soon Teoh

Haematology Unit, Department of Internal Medicine, Hospital Pulau Pinang, Jalan Residensi, 10990 Georgetown, Penang, Malaysia.

 

Ai Sim Goh
Haematology Unit, Department of Internal Medicine, Hospital Pulau Pinang, Jalan Residensi, 10990 Georgetown, Penang, Malaysia.

 

Please see the book :- https://doi.org/10.9734/bpi/rudhr/v9/337