Current Drug Research Reviews - Volume 16, Issue 1, 2024

Background: Mucormycosis has been infesting the universe for a while back, often with no prompt treatments. The disease devastation is spreading at an alarming rate. Many researchers are still hoping for a good potential drug that could help the healthcare system in this tussle. Molecular docking is an in silico tool that has gained popularity over the last few decades. Knowing the mechanism of enzymatic action is aided by imitating membrane protein actions in binding ligands. Aim: The aim of this perspective is to determine whether an existing drug, daclatasvir, has antifungal activity. Objective: The primary objective of this in silico study was to investigate the potential effects of the binding affinity of daclatasvir with the crucial protein (1XFF) of mucormycosis, as well as the binding pattern of the active site amino acids with the drug molecule. Materials and Methods: To calculate the binding affinity of daclatasvir to the fungal protein 1XFF, Auto Dock Vina was used for molecular docking studies. The CDOCKER protocol was used to determine the receptor-ligand interaction by configuring various parameters. Results: The docking energy of the ligand (daclatasvir) on the protein (1XFF) was found to be - 16.7216 kcal/mol, while the interaction energy was found to be -42.1314 kcal/mol. Conclusion: The binding pattern completely alters the dynamics of the protein, resulting in the breakdown of the fungal wall. The vital protein (1XFF) of Rhizopus oryzae is proposed as a possible protein target for the non-structural protein 5A inhibitor/antiviral drug daclatasvir in this study.

Potassium-competitive acid blockers (P-CABs), such as tegoprazan, are a new and diverse class of drugs that can completely block the potassium-binding site of gastric H⁺/K⁺ ATPase, potentially overcoming the limitations of proton-pump inhibitors (PPIs). A number of studies have compared the effectiveness as well as the safety profile of tegoprazan to PPIs and other P-CABs for the treatment of gastrointestinal diseases. The current review study evaluates the published works of literature related to clinical pharmacology and clinical trials of tegoprazan for the treatment of diseases related to the gastrointestinal tract. According to the publications included in the study, tegoprazan was found to be safe and well-tolerated and can be used to treat a group of gastrointestinal diseases, including gastroesophageal reflux disease (GERD), non-erosive reflux disease (NERD), and H. pyloricombination therapy.

Background: Carotenoids are natural hydrocarbons that play an important role in photomorphogenesis, photosynthesis, photoprotection, development, and defense mechanism of plants. Carotenoids have good anti-oxidants and provitamin A contents with their additional colorant nature, which are indispensable to plants and human diets. Capsicum species are well known for their culinary uses worldwide; they are not only cultivated as vegetables but used in numerous medicinal preparations as well due to their medicinal aspects. This article aims to collect data on the beneficial aspects of capsaicinoids with a major emphasis on capsanthin. Methods: In order to investigate the biological potential and therapeutic benefit of capsanthin in medicine, in the present work, scientific research data on capsanthin were collected from different literature sources and analyzed. The biological potential of Capsicum annuumin medicine was also investigated through literature data analysis of different scientific research work. Scientific data on capsanthin were collected from Google, Google Scholar, PubMed, Science Direct, and Scopus using the term capsanthin and capsicum in the present work. Detailed pharmacological activities of capsanthin were presented and discussed in the present work through scientific data analysis of research work. Analytical techniques for the separation, isolation, and identification of capsanthin were taken into consideration in this work. Results: Scientific data analysis revealed the biological importance and therapeutic benefit of capsanthin and capsicum in medicine. Capsicum annuumis a member of the Solanaceae family, which is one of the most cultivated spices worldwide. Capsaicinoids are one of the main classes of phytochemicals found in chili peppers, i.e., Capsicum annuum, and are mainly responsible for the pungent and spicy flavor of chili peppers. Capsanthin is a crystalline red color pigment found as the main component of Capsicum annuumfruits during ripening. Capsanthin is also found in Lilium, Aesculus, Berberis, and Asparagus officinalis. Chemically, capsanthin contains a cyclopentane ring, 11 conjugated double bonds, and a conjugated keto group. Capsanthin is a powerful antioxidant, exhibits anti-tumor activities, attenuates obesity-induced inflammation, and raises plasma HDL cholesterol levels. Scientific studies have proven the pharmacological benefits of capsanthin in medicine as it is helpful in pain relief, cardioprotection, weight loss, and body temperature regulation. Moreover, it also has anti-inflammatory, anticancer, antioxidant, and antimicrobial activities. In the literature database, numerous extraction and isolation techniques have been documented for capsanthin. In addition, the analytical techniques and other bioanalytical tools for the isolation and identification of capsanthin were also discussed in the present article. Conclusion: Medicinal importance and pharmacological activities of capsanthin were reviewed and discussed in this paper. This review aimed to highlight the literature on capsanthin in drug discoveries with their analytical development.

Odevixibat is synthesized through chemical modification of Benzothiazepine's structure. It is a tiny chemical that inhibits the ileal bile acid transporter and is used to treat a variety of cholestatic illnesses, including progressive familial intrahepatic cholestasis (PFIC). For cholestatic pruritus and liver disease development, bile acid transporter inhibition is a unique treatment strategy. Odevixibat reduces enteric bile acid reuptake. Oral odevixibat was also studied in children with cholestatic liver disease. Odevixibat received its first approval in the European Union (EU) in July 2021 for the treatment of PFIC in patients aged 6 months, followed by approval in the USA in August 2021 for the treatment of pruritus in PFIC patients aged 3 months. Bile acids in the distal ileum can be reabsorbed by the ileal sodium/bile acid cotransporter, a transport glycoprotein. Odevixibat is a sodium/bile acid co-transporter reversible inhibitor. An average 3 mg once-daily dose of odevixibat for a week resulted in a 56% reduction in the area under the curve of bile acid. A daily dose of 1.5 mg resulted in a 43% decrease in the area under the curve for bile id. Odevixibat is also being evaluated in many countries for the treatment of other cholestatic illnesses, including Alagille syndrome and biliary atresia. This article reviews the updated information on odevixibat with respect to its clinical pharmacology, mechanism of action, pharmacokinetics, pharmacodynamics, metabolism, drug-drug interactions, pre-clinical studies, and clinical trials.

Neurodegeneration is an elucidating feature of many neuronal disorders including Alzheimer’s, disease, Parkinson’s disease, and cerebral ischemia. These neurodegenerative disorders are a major public health concern with high mortality and morbidity rates around the world. Presently, researchers have concentrated their efforts on determining the neuroprotective activity of natural products for the management of neurological manifestation associated with neurodegeneration or aging. Silibinin, an active component of the plant Silybum marianum(family: Asteraceae) was used for the treatment of liver diseases from ancient times. Recently several preclinical studies provide supportive evidence for the neuroprotective activity of silibinin in experimental animals. Besides its antioxidant effect, silibinin exhibits neuroprotective activities by altering several cellular and molecular signaling pathways like BDNF, ER/PI3/Akt, NfΚB, JNK, IR & IGF-IR, mTOR, and many more against brain-related neurotoxicity. This review provided a comprehensive summary of the chemistry, pharmacokinetics, side effects, and pharmacological effects of silibinin against various neurodegenerative disorders with a prominent cellular and molecular mechanism. The literature reviews and preclinical studies demonstrated that silibinin could be an alternate candidate for the management of neurodegenerative disorders. Thus, there is a scope for further preclinical and clinical research to introduce this phytoconstituent as a therapeutic alternative candidate.

GIT is seriously affected by inflammatory bowel disease (IBD), which is characterized by extreme inflammation and an imbalance in a person's healthy life span. The frequency of occurrence of such chronic diseases as IBD would continue to increase. In the past decade, increasing attention has been paid to polyphenols from natural sources have been shown to serve as successful therapeutic agents for altering the signalling pathways linked to IBD and oxidative stress. We conducted a structured search for peer-reviewed research articles using the various keywords in bibliographic databases. By using common tools and a deductive qualitative content analysis technique, the quality of the retrieved papers and the distinctive findings of the articles included in the study were evaluated. Notably, experimental and clinical evidence has proved that natural polyphenols could act as a targeted modulator to play a key role in the prevention or treatment of IBD. Polyphenol phytochemicals have shown noticeable alleviative effects by acting on the TLR/NLR, and NF-ΚB signaling pathway in intestinal inflammation. This study examines the potential of polyphenols for treating IBD, with an emphasis on modulating cellular signalling mechanisms, regulating the balance of gut microbiota, and restoring the epithelial barrier. The available evidence concluded that the utilization of polyphenol-rich sources could control inflammation, mucosal healing, and positive benefits with minimal side effects. Even though additional study is required in this area, particularly that which focuses on the interactions, connections, and precise mechanisms of action linking polyphenols and IBD.

Background: A novel, simple, efficient, rapid, and precise reverse-phase highperformance liquid chromatography (RP-HPLC) method was developed for the estimation of Tenofovir and Emtricitabine in the bulk and pharmaceutical dosage form. The currently developed method was subsequently validated according to ICH guidelines in terms of linearity, accuracy, precision, the limit of detection, the limit of quantification, robustness, etc. Methods: The separation of the selected drugs was optimized after several trials including change of mobile phase and its composition, stationary phase, flow rate, column temperature, etc. The separation was performed by using an Inertsil ODS C18 column (250 mm x 4.6 mm, 5μ) and UV absorption was measured at 231 nm. Methanol: Acetonitrile: Water was selected as the mobile phase in the ratio of 50:20:30 (V/V/V) at a flow rate of 1 mL/min. As per International Conference on Harmonization (ICH) Q2 R1 guidelines, several validation parameters were evaluated which include specificity, linearity, precision, accuracy, the limit of detection (LOD), and the limit of quantitation (LOQ). Results: The acceptable degree of linearity range was found to be 40-100 μg/mL. The standard solution exhibited retention times of 3.06 minutes and 5.07 minutes for Tenofovir and Emtricitabine respectively. The LOD and LOQ obtained were 0.05 μg/ml and 0.02 μg/mL, 15 μg/mL, and 0.08 μg/mL for Tenofovir and Emtricitabine respectively. The percent recovery was found to be 98 to 102%. Conclusion: Hence, the proposed method is simple, selective, and specifically meets the requirements of ICH guidelines for the validation of the analytical method.