Study On The Chemical Constituents Of Phyllanthus Acidus From Xishuangbanna

Hepatitis b virus?HBV?infection is a serious threat to human life and health.HBV infection may lead to liver failure,cirrhosis and hepatocellular carcinoma?HCC?,and even death.Currently,about 457 million people in China are infected with or have been infected with hepatitis b virus,and about 120 million of them are carriers of hepatitis b virus.The existing anti-hbv drugs mainly include nucleoside drugs and interferon,which have played a positive role in inhibiting virus replication and alleviating patients'symptoms in clinical practice,but there are still major problems such as not completely removing the virus,drug withdrawal is easy to rebound,drug resistance and side effects.Bisabolane type sesquiterpenes belong to the monocyclic sesquiterpenes,and their basic structure contains two chiral carbon atoms.Natural alkane-type sesquiterpenes of myrrh often contain functional groups such as hydroxyl group,ketone carbonyl group,ester group and epoxy group,so most of them have good biological activities and are the research focus of natural products.Team early work discovered the Phyllanthus plant of Euphorbiaceae,norbisabolane-type sesquiterpenoids has a good activity in the resistant HBV,in order to further discovery the norbisabolane-type sesquiterpenoids structure relationship which can against hepatitis b virus in phyllantus acidus.So this paper carried out the anti HBV activity in P.acidus from xishuangbanna the norbisabolane-type sesquiterpenoids research.The norbisabolane sesquiterpenes belong to monocyclic sesquiterpenes.norbisabolane-type sesquiterpenes rich in Euphorbiaceae Phyllanthus plants are rare in the natural world,and only more than 60 such components have been found so far.These compounds have significant anti-hepatitis B virus activity.Phyllanthus acidus Skeel is a plant of Phyllanthus of Euphorbiaceae,which is an evergreen shrub or small tree and widely distributed in southeast Asian countries such as Malaysia,Thailand and Philippines.It is also called Malay gooseberry,Tahiti gooseberry,etc.according to its origin.West Indian gooseberry has a long history of folk medicine,and its fruits,stems and leaves are of medicinal value.Through a variety of chromatographic separation techniques,20 monomer compounds were isolated from the P.acidus.The structures of these compounds were identified by MS,1D-NMR,2D-NMR,CD and UV spectroscopy.The structure types involved 15 norbisabolane sesquiterpenes,3 flavonoids,1 sterol and 1 monoterpene.Among them are 4 new norbisabolane sesquiterpenes.The absolute configuration of new compounds 1 and 2 is determined by single crystal diffraction.The four new compounds are named pyacidusin A?1?,pyacidusin B?2?,Pllantacidoid A1?3?and pyllanthacidoid N1?4?respectively.They have a basic skeleton consisting of three rings,namely,a six-membered ring is cis-fused with a five-membered oxygen ring,and the five-membered oxygen ring is screwed with a six-membered oxygen ring.The C-3 of the six-membered ring is often substituted by carboxyl groups,and glycoester ligands are formed.The hydroxyl groups of hexahydric-10 are often formed into esters of aromatic acids such as benzoic acid or cinnamic acid.Known sesquiterpene compounds are:phyllantHacidoids A-D,F,G,I J,L,Q,R?5-15?,Flavonoids were identified as kaempferol 4'-O-?-L-rhamnopyranoside?16?,myricetin myricitrin 3-O-?-L-rhamnopyranoside?17?,?E?-polydatin?18?,sterols as?-sitosterol?19?.The monoterpene is sachalinoside B?20?.The compound?1-3,5-15?has been tested for cytotoxicity and HBV virus inhibitory activity of hepatoma cell line?HepG2.2.15?in vitro by MTT method.The results show that the IC₅₀ value of compound 2 to HBsAg is 11.2?0.01?M,while compound 3 can inhibit HBeAg secretion the IC₅₀ value is 57.1?0.02?M.At the same time,the quality standard of P.acidus was studied and established.The above research provides a certain reference for the further development and utilization of P.acidus in the treatment of hepatitis B..