Antidiabetic activity of gossypin, a pentahydroxyflavone glucoside, in streptozotocin‐induced experimental diabetes in rats

“…However, kaempferitrin failed to change the glucose tolerance curve during the time course [89]. In another study, gossypin, a natural pentahydroxyflavone glucoside isolated from the flowers of Hibiscus vitifolius, was proven to display remarkable antihyperglycemic activity in STZ-induced diabetic rats [90]. glucose serum (↓) [79]; plasma insulin and pancreatic islet mass (↑), HbA1c (↓) [80] Chen et al glucose tolerance, plasma protein and urea levels (→), blood glucose, HbA1c (↓), glycogen content in liver and muscles, plasma insulin, hemoglobin levels (↑) [90] Abbreviations: HbA1c, glycated hemoglobin; GSH, glutathione; TG, triglyceride; MDA, malondialdehyde; NO, nitric oxide; T2B, type 2 diabetes; PPAR, peroxisome proliferator-activated receptor; AMPK, AMP-activated protein kinase; TC, total cholesterol; SOD, superoxide dismutase; AST, aspartate aminotransferase; ALT, alanine aminotransferase; TBARS, thiobarbituric acid reactive substances; GSH-PX, glutathione peroxidase; Symbol meaning: ↑, increase; ↓, decrease; →, normalize Studies on flavonoids used for the treatment of diabetic complications: Diabetes needs careful management otherwise it can lead to various complications such as cardiovascular disease, kidney failure, nerve damage and blindness.…”

Section: Inhibition Of α-Glucosidase To Reduce Intestinal Glucose Absmentioning

confidence: 99%

Natural Flavonoids as Potential Herbal Medication for the Treatment of Diabetes Mellitus and its Complications

Chen

Mangelinckx

Adams

et al. 2015

Natural Product Communications

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Diabetes mellitus, together with its various complications, is becoming a serious threat to human health. Natural products are secondary metabolites widely distributed in plants, having a broad range of biological activities. The development of antidiabetic medication from natural products, especially those originating from plants with a traceable folk-usage history in treating diabetes, is receiving more attention. Many studies highlighted not only the benefits of natural flavonoids with hypoglycemic effects, but also their importance in the management of diabetic complications. This review describes selected natural flavonoids that have been validated for their hypoglycemic properties, together with their mechanisms of action. Also discussed are their activities in the treatment of diabetic complications demonstrated via laboratory diabetic animal models, in vitro and clinical trials using human subjects. Published papers from 2000 to date on flavonoids and diabetes were covered through accessing Web of Science and multiple databases for biomedical sciences. The major potential benefits of natural flavonoids discussed in this review clearly suggest that these substances are lead compounds with sufficient structural diversity of great importance in the antidiabetic drug developing process.

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“…The anticancer properties of natural products have been suggested to play an important role in the prevention of cancers (Li et al, ). Gossypin is traditionally used for the treatment of diabetes (Venkatesan & Sorimuthu Pillai, ) and exerts anti‐inflammatory (Rajagopal, Lankadasari, Aranjani, & Harikumar, ), antioxidant (Katary & Salahuddin, ), and anticancer activities (Babu et al, ). However, the mechanistic targets of gossypin have not been clearly elucidated.…”

Section: Discussionmentioning

confidence: 99%

Gossypin inhibits gastric cancer growth by direct targeting of AURKA and RSK2

Wang

Chen

et al. 2018

Phytotherapy Research

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Gossypin is a flavone extracted from Hibiscus vitifolius, which has been reported to exhibit anti‐inflammatory, antioxidant, and anticancer activities. However, the anticancer properties of gossypin and its molecular mechanism of action against gastric cancer have not been fully investigated. In the present study, we report that gossypin is an Aurora kinase A (AURKA) and RSK2 inhibitor that suppresses gastric cancer growth. Gossypin attenuated anchorage‐dependent and anchorage‐independent gastric cancer cell growth as well as cell migration. Based on the results of in vitro screening and cell‐based assays, gossypin directly binds to and inhibits AURKA and RSK2 activities and their downstream signaling proteins. Gossypin decreased S phase and increased G2/M phase cell cycle arrest by reducing the expression of cyclin A2 and cyclin B1 and the phosphorylation of the CDC protein. Additionally, gossypin also induced intrinsic apoptosis by activating caspases and PARP and increasing the expression of cytochrome c. Our results demonstrate that gossypin is an AURKA and RSK2 inhibitor that could be useful for treating gastric cancer.

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Antidiabetic activity of gossypin, a pentahydroxyflavone glucoside, in streptozotocin‐induced experimental diabetes in rats

Abstract: The results of the present study indicate that gossypin has potent antidiabetic activity in STZ-induced experimental diabetes in rats.

Cited by 25 publications

References 30 publications

Flavonoids and Their Biological Secrets

Flavonoids and Their Biological Secrets

Natural Flavonoids as Potential Herbal Medication for the Treatment of Diabetes Mellitus and its Complications

Gossypin inhibits gastric cancer growth by direct targeting of AURKA and RSK2

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