Transient Receptor Potential Vanilloid (TRPV4) channel inhibition: A novel promising approach for the treatment of lung diseases.

Research on transient receptor potential vanilloid-4 (TRPV4) can provide a promising potential therapeutic target in the development of novel medicines for lung disorders. TRPV4 expresses in lung tissue and plays an important role in the maintenance of respiratory homeostatic function. TRPV4 is upregulated in life-threatening respiratory diseases like pulmonary hypertension, asthma, cystic fibrosis, and chronic obstructive pulmonary diseases. TRPV4 is linked to several proteins that have physiological functions and are sensitive to a wide variety of stimuli, such as mechanical stimulation, changes in temperature, and hypotonicity, and responds to a variety of proteins and lipid mediators, including anandamide (AA), the arachidonic acid metabolite, 5,6-epoxyeicosatrienoic acid (5,6-EET), a plant dimeric diterpenoid called bisandrographolide A (BAA), and the phorbol ester 4-alpha-phorbol-12,13-didecanoate (4α-PDD). This study focused on relevant research evidence of TRPV4 in lung disorders and its agonist and antagonist effects. TRPV4 can be a possible target of discovered molecules that exerts high therapeutic potential in the treatment of respiratory diseases by inhibiting TRPV4.

Drug repurposing - A search for novel therapy for the treatment of diabetic neuropathy.

Diabetic neuropathy is a chronic complication to metabolic disorder, diabetes mellitus. Till date, diagnosis and treatment of diabetic neuropathy remain elusive with challenges associated with the efficacy and safety of the current therapeutics. Considering, the hurdles associated with discovery of de novo drugs, repurposing of old drugs for new therapeutic modalities sounds promising. This review, focuses on a molecular pathways involved in the progression of diabetic neuropathy, and the current pharmacological and non-pharmacological therapies implemented. Furthermore, a holistic and mechanism centric drug repurposing approach is pursued for identification of existing drugs as novel therapy in the treatment of diabetic neuropathy. The global status of ongoing clinical research on diabetic neuropathy is also highlighted. In conclusion, the barriers associated with drug repurposing is identified to stimulate the curiosity of the researchers to overcome them and rapidly translate the drugs to the patients suffering from diabetic neuropathy.

Role of semi-purified andrographolide from Andrographis paniculata extract as nano-phytovesicular carrier for enhancing oral absorption and hypoglycemic activity.

Objective: Andrographis paniculata is a well-known medicinal plant in Southeast Asia, India and China. The plant contains andrographolide (AN), a very important phytochemical used in various health problems. However, AN is low in oral absorption bioavailability of AN due to the rapid clearance and high protein binding capacity. Methods: The present study was aimed to develop a nano-phytovesicular formulation of semi-purified AN extracts from a naturally occurring phospholipid (soya phosphatidylcholine) in order to increase the oral absorption and antihyperglycemic activity in rats. Results: The nano-phyto vesicle of semi-purified AN extracts equivalent to 25 mg /kg AN significantly protected the hyperglycemic condition of rats. The in vitro and in vivo experiments results proved that the nano- phytovesicular system of plant extracts containing AN produced better oral absorption, bioavailability and improved antihyperglycemic activity compared with that of free AN at dose of 50 mg/kg. Conclusion: Hence, the prepared semi-purified extract nano-phytovesicular system is helpful in solving the problem of rapid clearance of AN.

Facile Synthesis, Characterization, and In Vitro Antimicrobial Screening of a New Series of 2,4,6-Trisubstituted-s-triazine Based Compounds.

A series of new 2,4,6-trisubstituted-s-triazine was synthesized, assessed for antimicrobial activity, and characterized by FTIR, (1)HNMR, (13)CNMR, and elemental analysis. The tested compounds, 4d, 4g, 4h, 4k, and 4n, have shown considerable in vitro antibacterial efficacy with reference to the standard drug ciprofloxacin (MIC 3.125 µgmL(-1) against B. subtilis, E. coli, and K. pneumoniae). It was observed that compounds 4d and 4h displayed equipotent antibacterial efficacy against B. subtilis (MIC 3.125 µgmL(-1)) and S. aureus (MIC 6.25 µgmL(-1)). The studies demonstrated that the para-fluorophenylpiperazine substituted s-triazine (4n) was potent and exhibited broad spectrum antibacterial activity against S. epidermidis, K. pneumoniae, and P. aeruginosa with MIC of 6.25 µgmL(-1) and for E. coli, it showed an MIC of 3.125 µgmL(-1) equipotent with reference to the standard drug. Among all the compounds under investigation, compound 4g also demonstrated significant antifungal activity (3.125 µgmL(-1)) against C. albicans.