Background: Among the millions of people around the world, the most prevalent metabolic disorder is diabetes mellitus. Due to the drawbacks which are associated with commercially available antidiabetic agents, new therapeutic approaches are needed to be considered. Alpha-amylase is a membrane-bound enzyme which is responsible for the breakdown of polysaccharides such as starch to monosaccharides which can be absorbed. Methods: We searched the scientific database using alpha-amylase, diabetes, antidiabetic agents as the keywords. Here in, only peer-reviewed research articles were collected which were useful to our current work. Results: To overcome the research gap, the alpha-amylase enzyme is regarded as a good target for antidiabetic agents to design the drug and provide an alternate approach for the treatment of type 2 diabetes mellitus. Basically, alpha-amylase inhibitors are classified into two groups: proteinaceous inhibitors, and non-proteinaceous inhibitors. Recently, non-proteinaceous inhibitors are being explored which includes chalcones, flavones, benzothiazoles, etc. as the potential antidiabetic agents. Conclusion: Herein, we discuss various potential antidiabetic agents which are strategically targeted alpha-amylase enzyme. These are having lesser side effects as compared to other antidiabetic agents, and are proposed to prevent the digestion and absorption of glucose leading to a decrease in the blood glucose level.

Quercetin is one of the most important flavonoids of polyphenols group and widely distributed in varieties of fruits, vegetables, leaves, and grains. It has been used as a nutraceutical for the mitigation of various ailments such as antihypertension, anti-diabetes, anti-arthritis, anticancer, anti-inflammatory, and antiaging. This review focuses on the quercetin as an herbal product and its application in nutraceutical for the benefit in hepato-toxicity & also for various diseases. Various literatures claimed it to be nutraceutical and beneficial in various disorders therefore as Medicinal Chemist we investigated and compiled it for the readers. We observed that quercetin is associated with certain issues such as thermolability, photosensitivity, poor bioavailability, low water solubility and chemically. These limitations have created a hurdle in the path of drug formulation and development. The researchers and pharmaceutical scholars have developed various formulations like liposomes, cubosomes, nanoparticles, and cocrystals. This review article presents the importance of quercetin as a nutraceutical as well as a herbal agent in the management of various disorders, particularly as an antioxidant and anti-inflammatory.

Aim: We aimed to review the drug delivery approaches including a novel drug delivery system of doxorubicin as an important anticancer drug. Background: Doxorubicin (DOX) is widely used against breast, uterine, ovarian, lung and cervical cancer. It is listed among the essential medicines by WHO and is thus a very important drug that can be used to fight against cancer. Despite its effectiveness, the use of the drug is limited due to its dose-dependent toxicity. Several studies based on the DOX have suggested the need for novel drug delivery formulations in the treatment of malignant and cancerous diseases due to its cytotoxic nature. Objectives: This review focuses on the different formulations of DOX which is a useful drug in the management of cancers, but associated with toxicity thus these approaches found applicability in the reduction of its toxicity. Methods: We searched the scientific database using cancer, DOX, and different formulations as the keywords. Here in only peer-reviewed research articles collected which were useful to our current work. Results: This study is based on an examination of the recent advancements of its novel drug delivery formulations. DOX hydrochloride is the first liposomal anticancer drug, administered via the intravenous route, and also clinically approved for the treatment of lymphomas, leukemias, and solid tumors. DOX is prepared into a liposomal formulation that contains polyethylene glycol (PEG) layer around DOX containing liposome made by pegylation process. DOX also formulated in nano-formulations which is also discussed herein led to reduced toxicity and increased efficacy. Conclusion: In the review, we described the significance of DOX in the form of different delivery approaches in the management of cancers with a reduction in the associated toxicity.

Objective: A comparative study of anti-prostate agents to investigate the stereochemical influences on binding affinity by molecular docking.Methods: Structures of enantiomers (R and S stereoisomers) for known anti-prostate cancer (PCa) agents were drawn using ChemBioDraw 2D software. Thereafter, they were converted to 3D structures using the ChemBioDraw 3D software in which they were subjected to energy minimization using the MM2 method and then saved as PDB extension files which can be accessed using the ADT interface. AutoDock Vina (ADT) 1.5.6 software version was used for molecular docking study.Results: A total of 12 different anti-PCa agents were selected and drawn including well-known drug R-bicalutamide. All molecules showed the binding affinity with respect to the nature of stereochemistry. R-stereoisomers showed better interaction as well as binding affinity toward 1z95 (mutated androgen receptor protein involved in the progression of PCa) whereas their S-stereoisomers were found inferior in comparison.Conclusion: This study showed that CB1-R and R-bicalutamide (with R-stereochemistry) were better in binding affinity comparative to their counterpart CB1-S and S-Bicalutamide (with S-stereochemistry). All the selected anti-PCa agents were showing the effect of stereochemical center; therefore, we must choose the right kind of stereochemistry while planning to develop the newer anti-PCa agents.

Diabetes is the most prevalent metabolic disorder causing a high rate of mortality and morbidity. Recently alpha-amylase is reported to be good drug design target for the treatment of diabetes mellitus. We have designed 116 molecules based on aza-Michael adduct of trans-chalcone as 1,3 diaryl-3-(arylamino)propan-1-ones which were studied by molecular docking and among them best six derivatives were synthesized easily via aza-Michael addition on trans-chalcone using KOH as a catalyst and evaluated for alpha-amylase inhibition along with antioxidant activity. It was observed that all compounds have alpha-amylase inhibitory activity but at different extents. The molecule 3e is the most potent alpha-amylase inhibitor of this series. 3a is the second most potent compound, whereas only one molecule 3d has shown antioxidant activity.