Phenolic Phytochemicals for Prevention and Treatment of Colorectal Cancer: A Critical Evaluation of In Vivo Studies.

Colorectal cancer (CRC) is the third most diagnosed and second leading cause of cancer-related death worldwide. Limitations with existing treatment regimens have demanded the search for better treatment options. Different phytochemicals with promising anti-CRC activities have been reported, with the molecular mechanism of actions still emerging. This review aims to summarize recent progress on the study of natural phenolic compounds in ameliorating CRC using in vivo models. This review followed the guidelines of the Preferred Reporting Items for Systematic Reporting and Meta-Analysis. Information on the relevant topic was gathered by searching the PubMed, Scopus, ScienceDirect, and Web of Science databases using keywords, such as "colorectal cancer" AND "phenolic compounds", "colorectal cancer" AND "polyphenol", "colorectal cancer" AND "phenolic acids", "colorectal cancer" AND "flavonoids", "colorectal cancer" AND "stilbene", and "colorectal cancer" AND "lignan" from the reputed peer-reviewed journals published over the last 20 years. Publications that incorporated in vivo experimental designs and produced statistically significant results were considered for this review. Many of these polyphenols demonstrate anti-CRC activities by inhibiting key cellular factors. This inhibition has been demonstrated by antiapoptotic effects, antiproliferative effects, or by upregulating factors responsible for cell cycle arrest or cell death in various in vivo CRC models. Numerous studies from independent laboratories have highlighted different plant phenolic compounds for their anti-CRC activities. While promising anti-CRC activity in many of these agents has created interest in this area, in-depth mechanistic and well-designed clinical studies are needed to support the therapeutic use of these compounds for the prevention and treatment of CRC.

Current Breakthroughs in Structure-based Design of Synthetic and Natural Sourced Inhibitors Against Zika Viral Targets.

BACKGROUND: Zika is a worldwide pandemic dreadful viral transmission through Aedes mosquito vector. It significantly causes fever, joint pain or rash, and conjunctivitis. Pregnant mothers suffering from Zika viral infection may have fetal abnormalities due to severe neurological problems, characterized by microcephaly along with Guillain-Barré syndrome, issuing ZIKV a major public health concern as declared by the World Health Organization. There is hardly any FDA approved anti-Zika viral drugs available. OBJECTIVE: Therefore, it is a big panic for the scientists to destroy the virus completely by generating potent inhibitors. METHODS: For the purpose, various Zika viral targets were explored by structure-based design in the present review in connection with the discovery of various synthetic and natural sourced inhibitors against Zika virus. RESULTS: The structure-based drug design tools such as x-ray crystallography and molecular docking reported various co-crystallized ligands and Zika virus inhibitors. CONCLUSION: Such inhibitors could further be modified for the design of highly active leads to combat Zika virus utilizing chemoinformatics modules.

Polyphenol extract of ichnocarpus frutescens leaves modifies hyperglycemia in dexamethasone (dex) treated rats.

INTRODUCTION: The leaves of Ichnocarpus frutescens are used extensively as a decoction for the treatment of diabetes mellitus by the tribals of Karnataka and Uttar Pradesh states. METHODS: Anti-diabetic activity of polyphenol extract of Ichnocarpus frutescens was investigated using dexamethasone (DEX) induced hyperglycemia in Wistar rats. Experimental animals were injected subcutaneously with dexamethasone 3 mg/kg/day. After one week, hyperglycemic rats were orally treated with polyphenol extract (PPE) extracts at the dose of 300 mg/kg/day and 150 mg/kg/day for a period of 14 days. RESULTS: Administration of DEX to fasted rats for 21 days resulted in insulin resistance evidenced by the significant increase in mean fasting blood glucose level (162.33 ± 4.72 mg/dl). Both 300 mg/kg and 150 mg/kg of PPE markedly reversed DEX induced mean fasting blood glucose level to 104.00 ± 3.30 mg/dl and 145.5 ± 1.99 mg/dl, respectively when compared with the positive control (p < 0.01). CONCLUSION: The possible mechanism by which polyphenol extract of I. frutescens brings about its antihyperglycemic action might be through potentiation of insulin sensitivity enhanced transport of blood glucose to the peripheral tissues. However, these findings suggest that polyphenol extract of I. frutescens therapy may reduce the risk of dexamethasone induced hyperglycemia in Wistar rats. These observations suggest that I. frutescens is a potential glucose lowering agent to ameliorate glucocorticoids induced hyperglycemia.

α-Glucosidase and α-amylase inhibitory activity of Senna surattensis.

In this study, we investigated the inhibitory effects of ethanolic extract of the leaves of Senna surattensis (EESS) on α-glucosidase and α-amylase. We also studied the in vitro antidiabetic activity of S. surattensis using the glucose uptake by isolated rat hemidiaphragm model. In vitro studies using mammalian α-glucosidase extracted from the small intestine homogenate of mouse showed that the extract was found to be more effective in inhibiting the activities of maltase [half maximal inhibitory concentration (IC(50)): 209.15 µg/mL] and sucrase (IC(50): 366.44 µg/mL) when compared with the control group (acarbose). The extract of S. surattensis were further quantified with respect to porcine pancreatic α-amylase inhibition using the chromogenic 3,5-dinitrosalicylic acid method. Interestingly, S. surattensis was also found to exhibit α-amylase (IC(50): 123.95 µg/mL) inhibitory activity. The glucose uptake in the rat hemidiaphragm was significantly (p < 0.01) increased by EESS (220.95 ± 5.4 mg/g/30 minute) when compared with the control group. The total polyphenolic content of EESS was found to be 98 µg pyrocatechol/mg of the extract. These results suggest that EESS inhibited carbohydrate digestive enzymes and increased the peripheral uptake of glucose. This study endorses the use of this plant for further studies to determine their potential for managing type II diabetes.