In vivo sedative and muscle relaxants activity of Diospyros lotus L

ABSTRACTObjectiveTo evaluate the sedative effect of Diospyros lotus L (D. lotus) extract in mice using the open field and Rota rod tests.MethodsFor the sedative and muscle relaxants activities of extract/fractions of the plant, in-vivo open field and phenobarbitone-induced sleeping time were used, while the Roda rod test was employed in animals for the assessment of muscle relaxant activity.ResultsResults from this investigation revealed that the extracts of D. lotus have exhibited significant sedative effect in mice (45.98%) at 100 mg/kg i.p. When the extract was partitioned with different solvents, the n-hexane fraction was inactive whereas the chloroform fraction was the most active with 82.67% sedative effect at 50 and 100 mg/kg i.p. On the other hand, the ethyl acetate and n-butanol fractions displayed significant sedative effects (55.65% and 40.87%, respectively) at 100 mg/kg i.p. Among the tested extract/fractions, only chloroform and ethyl acetate fractions showed significant (P < 0.05) muscle relaxant activity in the Rota rod test.ConclusionsIn short, our study provided scientific background to the traditional uses of D. lotus as sedative

Reversal of Multidrug Resistance in Mouse Lymphoma Cells by Extracts and Flavonoids from Pistacia integerrima

Phytochemical investigation of Pistacia integerrima has highlighted isolation of two known compounds naringenin (1) and dihydrokaempferol (2). A crude extract and these isolated compounds were here evaluated for their effects on reversion of multidrug resistance (MDR) mediated by P-glycoprotein (P-gp). The multidrug resistance P-glycoprotein is a target for chemotherapeutic drugs from cancer cells. In the present study rhodamine- 123 exclusion screening test on human mdr1 gene transfected mouse gene transfected L5178 and L5178Y mouse T-cell lymphoma cells showed excellent MDR reversing effects in a dose dependent manner. In-silico molecular docking investigations demonstrated a common binding site for Rhodamine123, and compounds naringenin and dihydrokaempferol. Our results showed that the relative docking energies estimated by docking softwares were in satisfactory correlation with the experimental activities. Preliminary interaction profile of P-gp docked complexes were also analysed in order to understand the nature of binding modes of these compounds. Our computational investigation suggested that the compounds interactions with the hydrophobic pocket of P-gp are mainly related to the inhibitory activity. Moreover this study s a platform for the discovery of novel natural compounds from herbal origin, as inhibitor molecules against the P-glycoprotein for the treatment of cancer

GC/GC-MS analysis and biological activities of Lantana Camara Linn.

Medicinal plants have been a part of human history for thousands of years and are still used as healthcare throughout the world. The current research aims to explore the chemical constituents of the methanol soluble extract (LC-Me) and petroleum ether soluble fraction (LCM-PES) from the leaves of Lantana camara Linn by GC/ GC-MS. This chemical analysis revealed the existence of 16 and 23 phytoconstituents in LC-Me and LCM-PES respectively. The major constituents in LC-Me were found to beethyl 9,12,15-octadecatrienoate (31.9%), hexadecanoic acid, ethyl ester (12.6%), n-hexadecanoic acid (11.1%), linoleic acid ethyl ester (9.1%), squalene (8.7%), di-n-octyl phthalate (6.2%), 9,12-octadecadienoic acid (Z,Z)- (4.2%), (E)-9-octadecenoic acid ethyl ester (2.7%) andcyclopropanebutanoicacid,2-[[2-[[2-[(2-pentylcyclopropyl)methyl]cyclopropyl]methyl]cyclopropyl]methyl]-, methyl ester  (2.3%). The chief bioactive compounds in petroleum ether soluble fraction were found to beandrost-8-en-3-ol, 4,4,14α-trimethyl-17-(2-bromo-1-methylethyl (57.9%), 14,17-nor-3,21-dioxo-β-amyrin, 17,18-didehydro-3-dehydroxy- (13.0%), barringtogenol B (2.5%), olean-12-ene-3,16,21,22,28-pentol, 21-(2-methyl-2-butenoate), [3β,16α,21β(Z),22α]-(1.7%),perhydrocyclopropa[e]azulene-4,5,6-triol, 1,1,4,6-tetramethyl  (1.7%), ethyl iso-allocholate (1.6%) and 1,2-benzenedicarboxylic acid, diisooctyl ester (1.6%). Both the extract and its fraction have exhibited very significant antibacterial, antifungal,mosquito repellent and larvicidal propertiesoriginated by numerous bioactive metabolites. Twenty eight (20 Gram-positive and 8 Gram-negative) bacteria were tested against LC.Me and LCM-PESwith noteworthy zone of inhibition.The significant in vitro antifungal activity was observed against fifteen fungi in LC-Me and LCM-PES. Very robust initial repellency was observed for LC-Me and LCM-PES (94% and 80% respectively) against the dengue-carrying mosquito (Aedes aegypti) at 2% concentration. The extract and its fraction were also found to be an efficient larvicidal agent against fourth-stage larvae of Aedes aegypti. The effective larvicidal property was noted in methanol soluble extract as compared topetroleum ether soluble fraction and standard with LC50value of 20 and 400 ppm respectively

An Efficient, Mild and Solvent-Free Synthesis of Benzene Ring Acylated Harmalines

A facile synthesis of a series of benzene ring acylated analogues of harmaline has been achieved by Friedel-Crafts acylation under solvent-free conditions at room temperature using acyl halides/acid anhydrides and AlCl3. The reaction afforded 10- and 12-acyl analogues of harmaline in good yield, along with minor quantities of N-acyl-tryptamines and 8-acyl analogues of N-acyltryptamines