ß-keto amyrin isolated from Cryptostegia grandiflora R. br. inhibits inflammation caused by Daboia russellii viper venom: Direct binding of ß-keto amyrin to phospholipase A2.

The search for mechanism-based anti-inflammatory therapies is of fundamental importance to avoid undesired off-target effects. Phospholipase A2 (PLA2) activity is a potential molecular target for anti-inflammatory drugs because it fuels arachidonic acid needed to synthesize inflammation mediators, such as prostaglandins. Herein, we aim to investigate the molecular mechanism by which ß-keto amyrin isolated from a methanolic extract of Cryptostegia grandiflora R. Br. Leaves can inhibit inflammation caused by Daboia russellii viper (DR) venom that mainly contains PLA2. We found that ß-keto amyrin neutralizes DR venom-induced paw-edema in a mouse model. Molecular docking of PLA2 with ß-keto amyrin complex resulted in a higher binding energy score of -8.86 kcal/mol and an inhibition constant of 611.7 nM. Diclofenac had a binding energy of -7.04 kcal/mol and an IC50 value of 620 nM, which predicts a poorer binding interaction than ß-keto amyrin. The higher conformational stability of ß-keto amyrin interaction compared to diclofenac is confirmed by molecular dynamics simulation. ß-keto amyrin isolated from C. grandiflora inhibits the PLA2 activity contained in Daboia russellii viper venom. The anti-inflammatory property of ß-keto amyrin is due to its direct binding into the active site of PLA2, thus inhibiting its enzyme activity.

Interaction of media, sexual activity and academic achievement in adolescents.

BACKGROUND: Adolescence is a period when the individual is vulnerable and exposure to sexually implicit/explicit programs on television and internet can influence their sexual behaviour and make them more permissive towards premarital sex, which is known to influence their academic performance. This can be modified by parental discussion on these matters with their children. There have been only few studies from India that have explored such issues therefore this study aimed to explore the impact of television, internet and parental discussion on sexual activity and academic performance. METHODS: This study was conducted in two co-education schools using a self reporting questionnaire administered to students of class IX-XII. This study evaluated the relation of academic performance, exposure to media such as television & internet to sexual activity & academic performance of the students and the role of parental discussion on these. RESULTS: The study sample size was 586. There is no significant association between the number of hours of watching television per day and academic performance as measured by marks in examinations. Significant positive association was found among boys between sexual contact and average score in academics & unsupervised use of internet. In both genders a significant positive association was found between those watching English serials, movies and increased chances of indulging in sexual activity while a negative relation with those watching Cartoons. There is no significant difference in occurrence of sexual contact in those who discussed sexual matters with parents and those who did not. CONCLUSION: This being first of it's kind of study from India and a cross sectional study, further prospective and detailed studies are warranted to delineate the interaction of media, parental discussion, academic performance and sexual activity.