The purpose of the research is to synthesise a novel series of (E)-2-(4-(1H-indol-3-yl)-6-p-substituted phenylpyrimidin-2-yl)dimethylguanidine derivatives since 3-(1H-indol-3-yl)-1-p-substituted phenylprop-2-en-1-one and evaluate their molecular docking studies, antimicrobial, and anti-diabetic activities. Among all the synthesized compounds (), compound exhibits excellent CDOCKER energy (-11.36 kcal/mol). The entire compounds () confirm very good antimicrobial activity towards the tested microorganisms. In the in vitro anti-diabetic studies, compounds confirm higher alpha-amylase and alpha-glucosidase inhibition activity. In the in vivo anti-diabetic activities, the synthesized compounds (10 mg/kg, p.o.) investigated by the streptozotocin (60 mg/kg, ip) -nicotinamide (120 mg/kg, p.o.) - induced model in adult male albino Wistar rat and these derivatives show considerable fasting blood glucose level when compared to metformin hydrochloride a potent and well-known anti-diabetic drug as a reference.
Introduction: Use of plants as a source of medicine has been inherited and is an important component of the health care system. Plants are a good source of biologically active compounds known as phytochemicals. The search for anticancer agents from plant sources started in 1950s with the discovery and development of vinca alkaloids, vincristine and vinblastine and the isolation of cytotoxic podophyllotoxin. Many chemotherapeutic agents are avilable their usage is limited due to development of side effects. Recent research demonstrates that plant based phytonutrients are effective in combating the incidence of carcinogenesis. So the purpose of this study is to reveal the relationship between breast cancer and chemopreventive effect of bark of Albizia lebbeck benth to protect against NMU induced mammary cancer in female spraque- dawley rats, and would foster further studies that could ultimately lead to prevention and therapy for breast cancer. Materials and methods: Virgin Female Sprague-Dawley rats were grouped into 5 groups (n=6). Thirty days before the induction of tumor the animals were treated with extracts. At the end of the 30th day tumor was induced by administrating NMU (50 mg/ kg i.p) was induced by single i.p injection, and then the treatment is continued up to a period of 120 days. At the end of the 120th day the animals were sacrificed through cervical decapitation, the mammary tumors were excised out and various parameters were studied such as tumor incidence, tumor burden, tumor volume, tumor weight and tumor latency. Also immunohistochemistry and histopathology were performed. Result: The i.p administration of NMU to the rats showed significant decrease in the body weight compared to normal control rats. After the administration of methanolic extract of Albizia lebbeck benth at different doses showed considerable prevention of weight loss when compared to NMU control rats. Also,in treated groups tumor incidence and tumor burden was decreased and tumor latency got increased. In addition histopathological studies supported significant decrease in formation of infiltrating duct carcinoma in mammory tissue sections. Conclusion: In the present study, methanolic extract of Albizia lebbeck benth showed protective effect against N-methyl-N-nitrosourea induced breast cancer.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.