1.Comparative molecular docking studies of lupeol and lupenone isolated from Pueraria lobata that inhibits BACE1: Probable remedies for Alzheimer's disease.
Koirala P;Seong SH;Jung HA;Choi JS Asian Pac J Trop Med. 2017 Dec;10(12):1117-1122. doi: 10.1016/j.apjtm.2017.10.018. Epub 2017 Oct 28.
OBJECTIVE: ;To discover lead lupane triterpenoid's potential isolated from Pueraria lobata roots against β-site amyloid precursor protein cleaving enzyme 1 (BACE1), which serve as a rate limiting step in amyloid beta (Aβ) production altering the course of Alzheimer's disease. In addition, enzyme kinetics study and molecular docking were conducted to establish the inhibition type and structure activity relationship.;METHODS: ;A systematic study of 70% ethanolic P. lobata root extract was employed to identify its BACE1 inhibitory potential. Further, BACE1 inhibitory potential of two lupane terpenoids, yielded from ethanolic extract, was assessed. In order to determine their inhibition mode, Lineweaver-Burk plots and Michaelis-Menten model for BACE1 was performed. AutoDock 4.2 program in addition determined the molecular interaction of BACE1 with isolated terpenoids.;RESULTS: ;Considering the inhibitory potential of 70% ethanolic extract of P. lobata against BACE1 (IC;50; = 80.35 μg/mL), lupeol and lupenone were subsequently isolated and exhibited notable or moderate BACE1 inhibitory activity with IC;50; values of 5.12 and 62.98 μmol/L, respectively, as compared to the positive control quercetin (IC;50; = 21.
2.GC-MS analysis and hepatoprotective activity of the n-hexane extract of Acrocarpus fraxinifolius leaves against paracetamol-induced hepatotoxicity in male albino rats.
Abd El-Ghffar EA;El-Nashar HA;Eldahshan OA;Singab AN Pharm Biol. 2017 Dec;55(1):441-449.
CONTEXT: ;In Egypt, the burden of liver diseases is exceptionally high.;OBJECTIVE: ;To investigate the components of the n-hexane extract of Acrocarpus fraxinifolius Arn. (Leguminosae) and its hepatoprotective activity against paracetamol (APAP)-induced hepatotoxicity in rats.;MATERIAL AND METHODS: ;TRACE GC ultra gas chromatogaphic spectrometry was used for extract analysis. Thirty albino rats were divided into six groups (five rats in each). Group 1 was the healthy control; Groups 2 and 3 were healthy treated groups (250 and 500 mg/kg b.w. of the extract, respectively) for seven days. Group 4 was hepatotoxicity control (APAP intoxicated group). Groups 5 and 6 received APAP + extract 250 and APAP + extract 500, respectively.;RESULTS: ;Chromatographic analysis revealed the presence of 36 components. Major compounds were α-tocopherol (18.23%), labda-8 (20)-13-dien-15-oic acid (13.15%), lupeol (11.93%), phytol (10.95%) and squalene (7.19%). In the acute oral toxicity study, the mortality rates and behavioural signs of toxicity were zero in all groups (doses from 0 to 5 g/kg b.w. of A. fraxinifolius). LD;50; was found to be greater than 5 g/kg of the extract. Only the high dose (500 mg/kg b.
3.Anti-oxidative and anti-inflammatory activities of some isolated constituents from the stem bark of Allanblackia monticola Staner L.C (Guttiferae).
Nguemfo EL;Dimo T;Dongmo AB;Azebaze AG;Alaoui K;Asongalem AE;Cherrah Y;Kamtchouing P Inflammopharmacology. 2009 Feb;17(1):37-41. doi: 10.1007/s10787-008-8039-2.
Stem bark of Allanblackia monticola has been used in association with others plant in the Cameroonian folk medicine for the treatment of various diseases such amoebic dysentery, diarrhoea, lung infections, and skin diseases. The methylene chloride fraction, its isolated compounds like alpha-mangostin, lupeol and acid betulinic were screened for antioxidant activity using free radical scavenging method. These isolated compounds were further tested for anti-inflammatory properties using carrageenan-induced model. Methylene chloride fraction, showed concentration-dependent radical scavenging activity, by inhibiting 1,1-diphenyl-1-picryl-hydrazyl radical (DPPH) with an IC(50) value of 14.60 microg/ml. alpha-Mangostin and betulinic acid (500 microg/ml), showed weak radical scavenging activity with a maximum inhibition reaching 38.07 microg/ml and 26.38 microg/ml, respectively. Betulinic acid, lupeol and alpha-mangostin (5 mg/kg and 9.37 mg/kg) showed anti-inflammatory activity with a maximum inhibition of 57.89%, 57.14% and 38.70%, respectively. Methylene chloride fraction of Allanblackia monticola and some derivatives, have antioxidant and anti-inflammatory activities.