Studies On The Constituents And Their Biological Activities Of The Roots Of Kadsura Coccinea

Kadsura coccinea(Lem.)A.C.Sm.,a plant belonging to the family of Schisandraceae,is distributed widely in the southern part of mainland China.The roots of K.coccinea are used as a folk medicine for the treatment of rheumatoid arthritis and for gastric and duodenal ulcers,and K.coccinea has been developed as an anti-inflammatory traditional Chinese medicine.Based on the review on the chemical constituents and pharmacological research of Kadsura genus,the chemical constituents and their antitumor and anti-platelet aggregation activities were investigated.By means of various chromatographic methods such as silica gel,Sephadex LH-20,opening ODS column chromatography,preparative TLC,and semi-preparative HPLC,44 compounds were isolated from the 95%ethanol extract of the roots of K.coccinea,and their structures were elucidated on the basis of spectroscopic data and physico-chemical methods.The compounds comprised 18 new lanostane-type triterpenoids,6 lignans,and 6 steroids.The 18 new compounds were named as seco-coccinc acid A[23-oxo-3,4-seco-9βH-lanost-4(28),7-dien-3-oic acid, 1],seco-coccinc acid B[23-oxo-3,4-seco-9βH-lanost-4(28),7,24-trien-3-oic acid,2], seco-coccinc acid C[25-hydroxy-23-oxo-3,4-seco-9βH-lanost-4(28),7-dien-3-oic acid,3],seco-coccinc acid D[25-hydroxy-3,4-seco-9βH-lanost-4(28),7, 23-trien-3-oic acid,4],seco-coccinc acid G[3,4-seco-9βH-lanost-4(28),7, 24-trien-3-oic acid,5],seco-coccinc acid E[24i?-hydroxy-3,4-seco-9βH-lanost-4(28), 7,25(26)-trien-3-oic acid,6],seco-coccinc acid K[24R,25-dihydroxy-3, 4-seco-9βH-lanost-4(28),7-dien-3-oic acid,7],seco-coccinc acid H[17-oxo-3, 4-seco-9βH-17-octanorlanost-4(28),7-dien-3-oic acid,8],seco-coccinc acid F[24 (E)-3,4-seco-8βH-lanost-4(28),9(11),24-trien-3,26-dioic acid,9],seco-coccinc acid J[4-hydroxy-23-oxo-3,4-seco-8βH-lanost-9(11)-en-3-oic acid,10], seco-coccinc acid L[methyl 23-oxo-3,4-seco-8βH-lanost-4(28),9(11)-dien-3-oate, 11],seco-coccinc acid I[3,4-seco-lanost-4(28),8,24-trien-3-oic acid,12],coccinone A(lanost-7-en-3,23-dione,13),coccinone B(lanost-7,24-dien-3,23-dione,14), coccinone C[lanost-9(11)-en-3,23-dione,15],coccinone D[lanost-9(11),24-dien-3, 23-dione,16],coccinilactone A[23-oxo-8βH-lanost-9(11)-en-3,4-olide,17], coccinilactone B[23-oxo-8βH-lanost-9(11),24-dien-3,4-olide,18].The other 26 known compounds were identified as isovaleroyl-binankadsurin A(19),kadsuralignan J(20),acetyl-binankadsurin A(21),deoxyschizandrin(22),dehydrodiisoeugenol(23), meso-dihydroguaiaretic acid(24),24ξ-n-propyl-cholestan-3-one(25), 3β-hydroxyl-stigmast-5-en-7-one(26),stigmast-5-en-3β,7α-diol(27), stigmast-4-en-3-one(28),β-sitosterol(29),daucosterol(30),vanillic acid(31), vanillin(32),gallic acid(33),salicylic acid(34),2-methoxy benzoic acid(35), protocatechuic acid(36),shikimic acid(37),clovane-2β,9α-diol(38),androsin(39), n-butyl-β-D-fructopyranoside(40),tianshic acid(41),α-glyceryl palmitate(42), dibutylphthalate(43),5-hydromethyl furaldehyde(44).Among them,compounds 23, 25-28,33-43 were obtained from Kadsura genus for the first time,and compounds 19 and 24 were obtained from K.coccinea for the first time.The antitumor activities of the eleven new lanostane-type triterpenoids isolated from the roots of K.coccinea were tested.It was found that all tested triterpenoids showed growth inhibitory activities against human leukemia HL-60 cells,in which compounds 1 and 15 were the most potent.The anti-platelet aggregation activities of some triterpenoids and lignans isolated from the roots of K.coccinea were assayed. Compounds 2,12,15,19 and 21 showed anti-platelet aggregation activities in vitro.