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??OBJECTIVE To study the flavonoid glycosides of Urena lobata. METHODS Compounds were isolated and purified using various column chromatographies such as D101 macroporous adsorption resin, silica gel, Sephadex LH-20, and prep HPLC. Their structures were identified on the basis of their physicochemical properties and various spectroscopic experiments, including HRESIMS, ¹H-NMR, ¹³C-NMR, HSQC, and HMBC. RESULTS Ten flavonoid glycosides were obtained from the n-BuOH extract of U. lobata including quercetin-3-O-??-D-glucopyranosyl-(1??2)-??-D-galactopyranoside(1), kaempferol-3-O-??-D-glucopyranosyl-(1??2)-??-D-glucopyranosyl-7-O-??-L-rhamnopyranoside(2), quercetin-3-O-??-D-apiofuranosyl-(1??2)-??-D-glucopyranosyl-7-O-??-L-rhamnopyranoside(3), kaempferol-4'-O-??-D-apiofuranosyl-3-O-??-D-glucopyranosyl-7-O-??-L-rhamnopyranoside(4), kaempferol-3-O-??-D-apiofuranosyl-(1??2)-??-D-glucopyranosyl-7-O-??-L-rhamnopyranoside(5), quercetin-3-O-??-D-glucopyranosyl-7-O-??-L-rhamnopyranoside(6), quercetin-3-O-??-D-glucopyranosyl-(1??2)-??-D-glucopyranoside(7), kaempferol-3-O-??-L-rhamnopyranosyl-(1??6)-??-D-glucopyranosyl-(1??2)-??-D-glucopyranoside(8), kaempferol-3-O-??-D-glucopyranosyl-(1??2)-[??-L-rhamnopyranosyl-(1??6)]-??-D-glucopyranoside(9) and kaempferol-3-O-??-D-glucopyranosyl-(1??2)-??-D-glucopyranoside(10). CONCLUSION Compounds 1-3 and 6-10 are firstly obtained from U. lobata.     

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??OBJECTIVE ??-Conotoxin LtIA (??-CTX LtIA, LtIA) is a specific inhibitor of ??3??2 nicotinic acetylcholine receptors (nAChRs) from Conus litteratus, a marine snail native to Hainan. The aim of this study was to evaluate the analgesic activity of ??-CTX LtIA. METHODS The analgesic effect of ??-CTX LtIA on pain models was evaluated using mice hot-plate and tail-flick models by intracerebroventricular (icv) injection. RESULTS In tail-flick test, the maximum analgesia percentage (PMAP) was 37.74% at 15 min after LtIA administration by icv injection with dose of 0.2 nmol per mouse. While in hot-plate test, PMAP was 48.81% at 60 min after LtIA administration by icv injection with same dose of 0.2 nmol per mouse. ??-CTX LtIA showed good analgesic activity in two pain models. CONCLUSION ??-CTX LtIA exhibits good analgesic activity by specific interaction with ??3??2 nAChRs subtype. These RESULTS have great significance for the research and development of LtIA painkiller in the future.     

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??OBJECTIVE To study the chemical constituents from the aerial parts of Paris polyphylla var. chinensis. METHODS The compounds were isolated and purified from the 75% ethanol extract by chromatography on HPD100 macroporous resin, silica gel, and Sephadex LH-20 as well as semi-preparative HPLC. Their structures were elucidated on the basis of spectral data. RESULTS Eleven compounds were isolated and identified as corchionoside C (1), ??-ecdysterone (2), coronatasterone (3), kaempferol-3-O-??-D-galactopyranoside (4), astragalin (5), isorhamnetin-3-O-??-D-glucopyranoside (6), kaempferol-3-O-??-D-glucopyranosyl-(l??2)-??-D-galactopyranoside(7), isorhamnetin-3-O-??-D-glucopyranosyl-(l??2)-??-D-galactopyranoside (8), kaempferol-3-O-??-D-glucopyranosyl-(l??2)-??-D-glucopyranoside (9), isorhamnetin-3-O-??-D-galactopyranosyl-(l??6)-??-D-glucopyranoside (10), and isorhamnetin-3-O-??-D-gentiobioside (11). CONCLUSION Compounds 1 and 3-11 are isolated from this plant for the first time and compounds 1, 3-5 and 8-10 are isolated from Paris plants for the first time.     

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??OBJECTIVE To study the synthesis and activities of AHPN derivatives. METHODS Starting from p-bromophenol and 1-adamantanol, a series of AHPN derivatives were synthesized by substitution reaction, condensation reaction, oxidation reaction and reduction reaction. These new compounds were characterized by ¹H-NMR, ¹³CNMR and HR-MS. Biacore technique was used to test the derivatives?? combining activities with RAR??. RESULTS Four compounds, 7c, 6c, 6e, and 6h, exhibited significant combining activities with RAR?? compared with AHPN. The introduction of phosphoric acid groups and nitrogen heterocyclic ring increased the activities of these compounds. CONCLUSION Compounds 7c, 6c, 6e, and 6h show significant combining activities with RAR??, which are worthy of further study.     

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??OBJECTIVE To investigate antagonistic activities of three isomers of ??-conotoxin TxIB on rat and human ??6/??3??2??3 nicotinic acetylcholine receptors (nAChRs). METHODS Three disulfide bond isomers were synthesized using Fmoc chemistry, which were identified by ultra performance liquid chromatography (UPLC)and confirmed by MALDI-TOF mass spectrometry. Rat and human ??6/??3??2??3 nAChRs were expressed in oocytes of Xenopus laevis, which were used to test the antagonistic abilities of the 3 isomers. RESULTS The three isomers of ??-conotoxin TxIB were synthesized successfully.The retention time of each isomer of ??-conotoxin TxIB was different each other significantly. The observed molecular masses of three isomers were the same, which were consistent with their theoretical molecular mass.Their hydrophilicity orders were globular > ribbon> bead. Both rat and human ??6/??3??2??3 nAChRs were expressed in oocytes well. Inhibition of three isomers of ??-conotoxin TxIB on rat and human ??6/??3??2??3 nAChRs were evaluated respectively. Among the three isomers of TxIB, the activity of the globular isomer was the most potent one, which had almost same activity at rat and human ??6/??3??2??3 nAChRs with corresponding IC₅₀ of 28.2 and 32.0 nmol??L^-1respectively. However, the other two isomers, ribbon and bead isomers displayed little antagonistic effect on both rat and human ??6/??3??2??3 nAChRs only with an IC₅₀ of ??10 ??mol??L^-1. CONCLUSION The synthesized globular isomer of ??-conotoxin TxIB in this work has a high selectivity and potent antagonistic activity on rat and human ??6/??3??2??3 nAChRs, which would be helpful for its new drug development.     

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??OBJECTIVE To prepare the inclusion complex of Lignum dalbergia odorifera oil with hydroxyl-??-cyclodextrin(HP-??-CD), and to optimize the preparation process of it. METHODS The inclusion complex was prepared by the stirring-freeze-dry method. The preparation process was optimized by central composite design-response surface method (CCD-RSM),with the colligation score which was calculated by the yield of inclusion, the utilization rate of volatile oil and the content of trans-nerolidol as index. The inclusion complex was verified by phase-solubility method, DSC,UV and microscopical identification. RESULTS The optimum inclusion technology was: inclusion solvent 5% ethanol, stirring rate 500 r??min^-1, HP-??-CD to volatile oil 33??1, inclusion temperature 42 ??,inclusion time 2.5 h. The formation of inclusion complex can change the solubility, optical and thermodynamic properties of volatile oil. CONCLUSION The preparation process of inclusion complex of Lignum dalbergia odorifera oil with HP-??-CD optimized by CCD-RSM is reasonable and feasible, and provide a reliable experiment basis for its application.     

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??OBJECTIVE To investigate the chemical constituents from the stems of Lythrum salicaria L..METHODS The constituents were isolated and purified by silica gel, Sephadex LH-20 column chromatography, and TLC. The structures were identified on the basis of spectral data and physiochemical characteristics. RESULTS Twenty compounds were isolated from 70% ethanol extracts and identified as betulinic acid(1), 2??,3??,24-trihydroxy-12(13)-en-urs-28-oic acid(2), 6-O-(E)- sinapoylpoligalitol(3), feruloyl-6??-O-??-D-glucopyranoside(4), 7-oxo-??-sitosterol(5), en-tisolariciresinol(6), muramine(7), aesculetin(8), apigenin(9),(2E,6S)-2,6-dimethyl-6-O-??-D-xylpyranosyloxy-2,7-menthiafolic acid(10), quercetin3-O-(6??-caffeoyl)-??-D-galactopyranoside(11), cycloart-23-ene-3??,25-diol(12), (1??S,6??R)-8??-hydroxyabscisic acid-??-D-glucoside(13), 3??,5-dihydroxy-3,6,4??-trimethoxyl-7-O-??-D-glucopyranoside flavonoid(14), aurantiamide acetate(15), 5,6,3??,4??-tetrahydroxy-3,7-dimethoxy-flavone(16), ursolic acid(17), oleanolic acid(18), 4-O-11-methyl-oleoside-p-hydroxyphenyl-(6??-11-methyloleoside)-??-D-glucopyranoside(19), and 6-O-galloylarbutin(20). CONCLUSION Except for compounds 8 and 9, all the compounds were isolated from this plant material for the first time.
     

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??OBJECTIVE To investigate the rheological property of Kappa carrageenan and the effects of standing time, concentration, and temperature on the viscosity of carrageenan solution.METHODS The fluid type was determined by fitting the rheological profiles to Power law model.The effect of temperature on the rheological behavior was investigated according to the viscous flowactivation energy(E??) which was calculated by the Arrhenius formula. RESULTS The viscosity of carrageenan solution decreased with the increase of shear rate and temperature,whereas it increased with the concentration. There existed a positive correlation between E?? and concentration. Furthermore, the effects of different cations on the viscosity were also studied and the results indicated that the viscosity increased significantly with the ionic concentration, especially that of potassium chloride.CONCLUSION Carrageenan was inferred to be pseudo-plastic fluid which hasthe character of shear thinning effect and its viscosity is significantly affected by cationic species.     

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??OBJECTIVE To study the chemical constituents of Inula cappa. METHODS Chromatographic techniques were employed for isolation and purification of the constituents and their structures were determined by spectral analysis and chemical evidence. RESULTS Seventeen compounds were obtained and identified as friedelin(1), epifriedelanol(2), ??-amyrin(3), ??-amyrin(4), benzyl 2-O-??-D-glucopyranosy-2,6-dihydroxybenzoate(5), scopoletin(6), luteolin-7-O-??-D-glucuronide ethyl ester(7), benzyl alcohol glucoside(8), ophiopogonoside A(9), apigenin-7-O-??-D-glucoside(10), luteolin-7-O-??-D-rutinoside(11), hydnocarpin-D(12), luteolin(13), luteolin-7-O-??-D-glucoside(14), luteolin-4??-O-??-D-glucoside(15), quercetin-3-O-??-D-glucoside(16), and juglans cerebroside A(17). CONCLUSION Compounds 5, 7, 9, 11, 12, and 17 are for the first time obtained from the genus Inula and compounds 8, 10, 14, and 16 are isolated from Inula cappa for the first time.     

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??OBJECTIVE To investigage the effects of celastrol-triggered HeLa cells autophagy and the molecular mechanisms in vitro and in vivo. METHODS The antiproliferative effect of celastrol was detected using MTT assay. Apoptotic rate and cell cycle were evaluated using flow cytometric analysis. Autophagy was detected using fluorescence microscope. Protein expression was evaluated using Western blotting. Tumor growth was evaluated by subcutaneous xenograft model in vivo. RESULTS Celastrol inhibited HeLa cells proliferation and induced HeLa cells autophagy and cell cycle arrest at G₀/G₁ phase, but not induced HeLa cell apoptosis in vitro. The protein expression of Beclin 1 was up-regulated and the conversion from LC3 ?? to LC3 ?? was increase in HeLa cells in vitro after treatment with celastrol. Moreover, celastrol promoted the protein expression of PTEN??p-ERK1/2??p-MEK1/2 and inhibited the phosphorylated of Akt, p70S6K and mTOR in HeLa cells. After pretreatment with 3-methyladenine (5 mmol??L^-1), the antiproliferative and induced-autophagy effects of celastrol were reversed. Furthermore, celastrol inhibited tumor growth and the protein expression of p-Akt and p-mTOR, but up-regulated the protein expression of LC3 ?? and Beclin 1 in vivo. CONCLUSION Antitumor effect of celastrol dependent on cells autophagy in HeLa cells via inhibition of Akt/mTOR signaling pathway in vitro and in vivo.     

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??OBJECTIVE To study the chemical constituents of Noni enzyme (Morinda citrifolia L.) and their antitumor activities. METHODS Compounds were isolated by various chromatographic techniques, including silica gel, TLC, sephadex LH-20, and semi-preparative HPLC, and their structures were identified by their physicochemical properties and ¹H-NMR and ¹³C-NMR data. The in vitro antitumor activities of the isolated compounds were studied by MTT method. RESULTS Sixteen compounds were isolated from Noni enzyme. They were xylogranatinin(1), pelargonic acid(2), 1,5,15-tri-O-methylmorindol(3), sesquipinsapol B(4), (+)-syringaresinol(5), pinonesinol(6), 3-methylhexahydropyrrolopyrazine-1,4-dione(7), (2S)-3??-hydroxybutan-2-yl-2-hydroxypropanoate (8), 3-(sec-butyl)-6-methylpiperazine-2,5-dione(9), cyclo-(L-Pro-L-Leu)(10), gentisic acid(11), vomifoliol(12), scopoletin(13), 3-(2-hydroxy-4,5-dimethoxyphenyl) propanoic acid(14), medioresinol(15), hydroxychavicol(16). CONCLUSION Compounds 1-10, 12 and 14-16 are isolated from Noni enzyme for the first time. Compound 10 displays the stronger cytotoxicity against HepG2 and HeLa cells with an IC₅₀ value of 23.73, 16.55 ??g??mL^-1. Compound 5 had a certain inhibitory activity against HeLa cells with an IC₅₀ value of 47.12 ??g??mL^-1.     

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??OBJECTIVE To study the chemical constituents of the leaves of Magnolia grandiflora Linn and their antitumor activities. METHODS The constituents were isolated and purified by various chromatographic METHODS, including column chromatographies on silica gel, Sephadex LH-20, as well as recrystallization. Their structures were identified by analysis of physical and spectral data and confirmed by comparison of their spectral data with the reported values in the literature or those of authentic samples. The antiproliferative activities of the purified compounds were evaluated by MTT assay. RESULTS Twelve compounds were isolated and identified as parthenolide(1), ergosterol peroxide(2), N-formyl-annonain(Z)(3_Z), N-formyl-annonain(E)(3_E), vitamin E quinone(4), ??-sitosterol(5), 11,13-dehydrocompressanolide(6), scoparone(7), liriodenine(8), aurantiamide acetate(9), michelenollide(10), and 2,6,2??,6??-tetramethoxy-4,4??-bis(2,3-epoxy-1-hydroxypropyl)biphenyl(11). CONCLUSION Compounds 2, 3_Z, 3_E, and 4 are isolated from this plant for the first time. Compounds 9 and 11 are isolated from the plants in Magnoli Linn for the first time.     

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??OBJECTIVE To study the chemical constituents of Microtropis triflora Merr. et Freem. METHODS The compounds were isolated and purified by various chromatographic technigues such as silica gel, Sephadex LH-20, and pre-HPLC. Their structures were identified on the basis of chemical properties and spectral analysis. RESULTS Ten triterpenes were isolated and elucidated as 3, 25-epoxy-1??, 3??, 11??, 12, 23, 25-hexahydroxy-urs-12-en(1), ??-amyrin(2), ??-amyrin palmitate(3), 3??-hydroxy-11-oxo-olean-12-enyl-3-palmitate(4), lupeol(5), friedelin(6), 3-oxo-28-friedelanoic acid(7), oleanolic acid(8), salaspermic acid(9), and orthosphenic acid(10). CONCLUSION Compound 1 is a new compound and has cytotoxic activity against Bcap37 and SMMC7721 cells with IC₅₀ values of 27.86 and 11.38 ??g??mL^-1, respectively.     

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??OBJECTIVE To determine the immunosuppressive activity of a novel benzothiazole derivative BD759 on T cell proliferation and its potential mode of action. METHODS T cell proliferation, CD25 expression and cell cycle distribution were measured by flow cytometer. Cytokine levels, including IL-2, IL-4, IL-6, IL-10, IL-17A and IFN-??, were determined by ELISA. RESULTS BD759 significantly inhibited human T cell proliferation, stimulated either by anti-CD3/anti-CD28 monoclonal antibodies or by an alloantigen, in a dose-dependent manner with IC₅₀ values of (3.5??0.7) and (3.3??0.9) ??mol??L^-1, respectively. No obvious cytotoxic effects of BD759 were observed on human resting na??ve T cells and peripheral blood mononuclear cells in our experimental conditions. Furthermore, BD759 did not inhibit CD25 expression or IL-2, IL-4 and IL-10 secretion, but inhibited IL-6, IL-17A and IFN-?? production and induced cell cycle arrest at the G₀/G₁ phase in activated T cells. CONCLUSION These data indicate that BD759 has no effect on T cell activation, but induces T cell cycling arrest at G₀/G₁ phase. BD759 also inhibits the secretion of inflammatory cytokines, such as IL-6, IL-17A and IFN-gamma. Thus, BD759 has the potential to be used as a lead compound for the design and development of new immunosuppressants for treating autoimmune diseases and preventing graft rejection.     

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??OBJECTIVE To study the chemical constituents from the roots of Rubus parvifolius. METHODS Various chromatographic techniques such as silica gel, Sephadex LH-20, and prep-HPLC column chromatography were used. RESULTS Nineteen compounds, including 12 triterpenoids were isolated from the roots of Rubus parvifolius. Based on the analysis of their spectroscopic data, the structures of these 19 compounds were identified as p-hydroxybenzoic acid(1), 4-hydroxy-3,5-dimethoxybenzoic acid(2), 3-methoxy-4-hydroxybenzoic acid(3), ??-sitosterol(4), oleanolic acid(5), ursolic acid(6), 2-oxopomolic acid(7), pomolic acid(8), p-hydroxyphenylethyl alcohol(9), psiguanin A(10), 2??-hydroxyursolic acid(11), tormentic acid(12), 2??,3??,19??,23-tetrahydroxyurs-12-en-28-oic acid(13), L-epicatechin(14), 2??,3??,19??,24- tetrahydroxyolean-12-en-28-oic acid(15), 2??,3??,19??,24-tetrahydroxyurs-12-en-28-oic acid(16), 2??,3??,19??-trihydroxyolean-12-en-23,28-dioic acid(17), suavissimoside R₁ (18), and daucosterol(19), respectively. CONCLUSION Compounds 1-3, 5, 7-10, 12, and 15-17 are isolated from the roots of R. parvifolius for the first time. Compounds 7 and 9 are isolated from the genus Rubus L. for the first time. Compounds 10 and 15-17 are isolated from the family Rosaceae for the first time.     

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??OBJECTIVE To study the secondary metabolites of marine-derived fungus Aspergillus fumigatus YK-7. METHODS The compounds were isolated by several column chromatographic techniques, including silica gel, ODS, Sephadex LH-20 column chromatography, and HPLC, and their structures were identified on the basis of physicochemical properties and spectroscopic analysis. Trypan blue and MTT methods were applied for determining the effects of the compounds on proliferation of cancer cells in vitro. RESULTS Ten compounds were obtained, and their structures were identified as pseurotin A (1), pseurotin A₁(2), 14-norpseurotin A (3), FD-838 (4), demethoxyfumitremorgin C (5), 9??-hydroxyverruculogen TR-2 (6), 6-methoxyspirotryprostatin B (7), spiro[5H,10H-dipyrrolo[1,2-a:1??,2??-d]pyrazine-2-(3H),2??-[2H]indole]-3??,5,10(1??H)-trione (8), terezine D (9), and 14-hydroxyterezine D (10). CONCLUSION Compounds 3, 6, 7, 9, and 10 are isolated from marine-derived fungus Aspergillus fumigatus for the first time. Compounds 1-4 exhibite moderate antiproliferative activity against selected cancer cell lines in vitro.     

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??OBJECTIVE To study the chemical constituents from the rhizome of Drynaria fortunei and the protective effects of them on PC12 cells induced by A??_25-35. METHODS The compounds were isolated and purified by silica gel, Sephadex LH-20, ODS column chromatography, and their structures were identified on basis of spectroscopic methods, such as MS and NMR. PC12 cells were treated with A??_25-35 to establish the Alzheimer' s disease models. The compounds of different concentrations were added into culture medium to detect the protection. MTT assay was used to detect cell vitality and to observe the protective effects of compounds on PC12 cells induced by A??_25-35. RESULTS Nine compounds were isolated and identified as naringin(1), neoeriocitrin(2), 5,7-dihydroxychromone-7-neohesperidoside(3), (E)-4-O-??-D-glucopyranosyl caffeic acid(4), kaempferol(5), luteolin(6), protocatechoic acid(7), psoralen(8), and ??-sitosterol(9) . The cell experiments were performed on the compounds 1-8 and the results showed they can promote the proliferation of PC12 cells. The cell vitality increase with concentration rising, and the difference is statistically significant (P<0.05). CONCLUSION Compounds 1-8 play an important role in protecting A??_25-35-induced injury in PC12 cells and they are the main active components of Drynaria fortunei in the protection of central nervous function.     

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??OBJECTIVE To study the chemical constituents from the rhizome of Saururus chinensis. METHODS The chemical constituents from the rhizome of Saururus chinensis were extracted by supercritical CO₂ extraction and isolated by various chromatographic methods, such as silica gel, MCI and pre-HPLC. Their structures were elucidated by physico-chemical constants and spectroscopic methods. RESULTS Seventeen compounds were isolated and identified as aurantiamide acetate (1), echinuline (2), (-)-(7R,8R)-7-O-acetylpolysphorin (3), elemicin (4), isoelemicin (5), 1,4-bis(3,4-dimethyoxyphenyl)-2,3-dimethyl-1,4-butanedione (6), saucerneol D (7), (2R)-3-(3??,4??,5??-trimethoxyphenyl)-1,2-propanediol (8), grandisin (9), rel-(7R,8R,7??R,8??R)-3??,4??-methylenedioxy-3,4,5,5??-tetramethoxy-7,7-epoxylignan(10), zanthopyranone (11), (??)-eritro-1-(3,4,5-trimethoxy)-1,2-propanodiol (12), threo-3,4,5-trimethoxy-7-hydroxy-1??-allyl-3??,5??-dimethoxy-8.O.4??-neolignan (13), (+)-(8R)-(2,6-dimethoxy-4-propenylphenoxy)-1-(3,4,5-trimethoxyphenyl)propan-1-one (14), meso-dihydroguaiaretic acid(15), (-)-galbacin (16), and (-)-(7R,8R)-7-O-acetylraphidecursinol B (17). CONCLUSION Compound 6 is a new natural compound. Compounds 1-2, 4-6, 8-9 and 11-13 are isolated from this plant for the first time.     

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??OBJECTIVE To investigate the chemical constituents in chloroform extraction of Tetrastigmatis hemsleyani diels et. Gilg and their antitumor activities. METHODS Various chromatography techniques such as column chromatography on silica gel, Sephadex LH-20 and preparative TLC were used to isolate and purify the compounds. Their structures were identified by¹H-NMR,¹³C-NMR and MS. Their antitumor activities was tested by MTT method. Moreover, the other compounds of chloroform extraction were detected by GC-MS. RESULTS Six compounds were isolated by classic chromatography and identified as ??-sitosterol(1), 4-hydroxy-3-methoxybenzaldehyde(2), oleanolic acid (3), 5-hydroxymethyl furfural(4), azelaic acid(5), vanillic acid(6). Twenty-two compounds were identified by GC-MS. CONCLUSION Compounds 2-6 are isolated from this plant for the first time. Compounds 1 and 3 shows strong cytotoxic activities against Hela229 with IC₅₀ values of 40.78, 25.69 ??g??mL^-1, respectively. Compound 3 also showed strong cytotoxic activities against with IC₅₀ values of 69.87 ??g??mL^-1. The result proved that antitumor activity of chloroform extraction of Tetrastigmatis hemsleyani diels et. Gilg is due to the contribution of multi-components.