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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 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 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 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 study the chemical constituents of the chloroform extract from the aerial parts of Artemisa sacrorum. METHODS The chemical constituents were isolated and purified by silica gel and LH-20 column chromatography and preparation HPLC. Their structures were identified by spectral analysis methods. RESULTS Thirteen compounds were obtained and identified as 5-hydroxyl-7,4??-dimethoxyflavone(1), 4-hydroxylacetophenone(2), 5,4??-dihydroxyl-7,3??-dimethoxyflavone(3), 5,7-dihydroxyl-6,4??-dimethoxyflavone(4), 5,7-dihydroxyl-4??-methoxyflavone(5), 5,4??-dihydroxyl-7-methoxyflavone(6), caffeic acid(7), 8-hydroxyl-6,7-dimethoxycoumarin(8), 3,4-dihydroxylbenzoic acid(9), acetophenone-4-O-??-D-glucoside(10), 6-methoxycoumarin-7-O-??-D-glucoside(11), 6,8-dimethoxycoumarin-7-O-??-D-glucoside(12), and 2-hydroxyl-6-methoxyacetophenone-4-O-??-D-glucoside(13). CONCLUSION Compounds 3, 4, 5, 9, 10 and 12 are isolated from this plant for the first time.
     

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??OBJECTIVE To study the chemical constituents of Patrinia villosa (Thunb.) Juss. METHODS The compounds were isolated by a combination of various chromatographic techniques including column chromatography over macroporous resin, Sephadex LH-20, and reversed-phase HPLC. Their structures were elucidated by physiochemical property and spectral analysis. RESULTS Eleven compounds were isolated and identified as(7R,8S)-3,3??,5-trimethoxy-4??,7-epoxy-8,5??-neolignan-4,9,9??-triol-9-O-??-D-glucopyranoside(1), massonianoside D(2),(7R,8S)-dihydroxydehydrodiconiferyl alcohol-4-O-??-D-glucopyranoside(3),(7S,8R)-dihydroxydehydrodiconiferyl alcohol-4-O-??-D-glucopyranoside(4), 7R,8S-glochidioboside(5), lariciresinol-4-O-??-D-glucopyranoside(6), lariciresinol-9-O-??-D-glucopyranoside(7), lariciresinol-4??-O-??-D-glucopyranoside(8), tortoside B(9), tanegool(10), and tanegool-7??-methyl ether(11). CONCLUSION All compounds are isolated from Patrinia genus for the first time.     

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??To analyze recent studies on the role of transient receptor potential vanilloid 4(TRPV4) in fibrosis diseases and related mechanism. TRPV4 is a class of non-selective cation channel protein, which involved in intracellular divalent cations, mainly regulate Ca²⁺ homestasis and participate in the development of multiple organ fibrosis broadly. TRPV4 plays an important role in the prevention and treatment of fibrosis diseases. But for its complex mechanism of action, further research needs to be studied.     

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??OBJECTIVE To study the chemical constituents of Swertia binchuanensis. METHODS The constituents were isolated and purified by column chromatography of silica gel. Their structures were identified on the basis of spectral analysis and chemical properties. RESULTS Five compounds are isolated and identified as 7-O-????-L-rhamnopyranosyl-(1??2)-??-D-xylopyranosyl??-1,8-dihydroxy-3-methoxyxanthone(1), 3-O-??-D-glucopyranosyl-1,8-dihydroxyl-5-methoxyxanthone(2), 7-O-??-D- glucopyranosyl-1,8-dihydroxyl-3-methoxyxanthone(3), amarogentin(4), and amaroswerin(5). CONCLUSION All of the compounds were isolated from S.binchuanensis for the first time.     

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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 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 To investigate the sustained-release ability of Na-montmorillonite (Na-MMT) on 1-deoxynojirimycin (DNJ) in mulberry leaf extract (MLE). METHODS In order to prepare DNJ-MMT composite, DNJ was intercalated into the interlayer of MMT by stirring. Time and temperature for adsorption and ratio of DNJ to MMT were determined by calculating the loading of DNJ, then in vitro release experiment was carried out to estimate the sustained-release characteristics of DNJ-MMT. RESULTS DNJ-MMT composite with a drug loading of 111.64 mg??g^-1 was obtained by stirring 5.00 g Na-MMT and 16.00 g MLE containing 4 016.0 mg DNJ in 1 000 mL deionized water at 100 ?? for 1 h. The composite released DNJ quickly in water, potassium phosphate buffer (pH 7.4), and 0.1 mol??L^-1 hydrochloric acid solution. With the increasing of volume of hydrochloric acid solution, the release ratio of DNJ also increased correspondingly. CONCLUSION The sustained-release effect of Na-MMT on DNJ is proved. Na-MMT can be used for study of DNJ sustained-release preparations.     

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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 the chemical constituents of the aerial parts of Ribes diacanthum Pall. METHODS The compounds were isolated and purified by silica gel, Sephadex LH-20 colunm chromatography and HPLC. The structures were elucidated on the basis of spectral data and physiochemical properties. RESULTS Nineteen compounds were isolated from 95% ethanol extracts and identified as quercetin (1), quercetin-3-O-??-D-glucopyranoside (2), quercetin-3-O-??-L-rhamnopyranoside (3), quercetin-3-O-??-D-neohesperoside (4), mearnsetin (5), myricetin-3-O-??-L-rhamnoside (6), myricetin-3-O-??-D-glucopyranoside (7), mearnsetin 3-O-??-D-glucopyranoside (8), mearnsetin 3-O-??-L-rhamnopyranoside (9), kaempferol-3-O-??-D-glucopyranoside (10), kaempferol 3-O-??-D-(2-O-??-L-rhamnopyranosyl) glucopyranoside (11), kaempferol 3-(2??,6??-di-O-??-L-rhamnosyl)-??-D-glucoside (12), 1,2,4-trihydroxybenzene (13), vanillic acid (14), protocatechuic acid (15), 4-hydroxy benzoic acid (16), gallic acid (17), blumenol C glucoside (18), conocarpan (19). CONCLUSION All the compounds are isolated from the title plant and the NMR data for 8 is reported here for the first time.     

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??OBJECTIVE To investigate the chemical constituents from Bletilla striata (Thunb.) Reichb.f and study their anti-tumor activities and effect on progression of cell cycle. METHODS The compounds were isolated by various chromatographic methods including silica gel, ODS, Sephadex LH-20, and so on. Their structures were identified by extensive analysis of spectiroscopic data. The antiproliferative effects of the compounds were evaluated using MTT test, and compound 1 was tested for the effect on the cell cycle of A549 cells. RESULTS Five compounds were isolated from Bletilla striata and identified as 3??-hydroxyoleane-12-en-28-oic acid 3-O-??-L-rhamnopyranosyl-(1??2)-??-D-glucopyranoside(1),2-hydroxysuccinic acid(2),4-hydroxybenzylamine(3),palmitic acid(4),and 4-hydroxybenzoic acid(5). Compound 1 showed antiproliferative activity against the cancer cells and could induce G₀/G₁ phase arrest effectively after 24 h treatment. CONCLUSION Compounds 1-4 are isolated from Bletilla striata for the first time. Compound 1 shows potent inhibitory effect and might produce their action through inducing cell cycle arrest.     

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??OBJECTIVE To investigate the chemical constituents in the roots of Allium tuberosum. METHODS Colum chromatography with different materials such as silica gel was used to isolate and purify the chemical constituents. Their structures were identified by spectroscopic analysis. RESULTS Nine compounds were isolated from the roots of Allium tuberosum and their structures were identified as 4,8-dihydroxyacetophenone-8-O-ferulate(1), 4,8-dihydroxyacetophenone(2), 3,4,5-trimethoxybenzoic acid(3), 3,4,5-trimethoxycinnamic acid(4), buddlenol D(5), E-1,6,11-triene-4,5,9-trithiadodeca-9,9-dioxide(6), tianshic acid(7), daucosterol(8), and linoleic acid(9). CONCLUSION Compound 1 is a new compound and compounds 2-5 are obtained from Allium tuberosum for the first time.     

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??OBJECTIVE To study the polar chemical constituents from Prunella vulgaris L.. METHODS Silica gel, reverse-phase octadecylsilyl (ODS), Sephadex LH-20 chromatographic methods, MCI and HPLC were applied to isolate and purify compounds. MS and NMR methods were used to determine the structures of the compounds. Furthermore, the cytotoxicity of these chemical components for MCF-7, MDA-MB-231 and MCF-10A cell lines was measured by MTT method. RESULTS A total of 12 compounds were isolated from the fruits of P. vulgaris and their structures were identified as methyl 3,4,??-trihydroxypropionate(1), danshensu (2), methyl rosmarinate (3), 3,4-dihydroxybenzoic acid (4), quercetin-3-O-glycopyranoside (5), hyperoside (6), 2??,3??,19??,24-tetrahydroxylurs-12-en-28-oic acid (7), 2??,3??,24-trihydroxyolean-12-en-28-oic acid (8), cytidine (9), daucosterol (10), (3S,5R,10S)-7-oxo-12-methoxyabieta-8,11,13-triene-3,11,14-triol (11), and 2??,3??,24-trihydroxyolean-12,20(30)-dien-28-oic acid (12). The results of antitumor assay indicated that compound 2, 3, 5 and 6 significantly inhibited the activity of MCF-7, compound 3 could inhibit the activity of MDA-MB-231, but all of them also significantly inhibited the activity of normal cell lines MCF-10A. CONCLUSION Compounds 9 and 11 are isolated from the genus of Prunella L. for the first time. Some chemical constituents form Prunella L. show certain anti-breast cancer activity.     

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??OBJECTIVE To study the chemical constituents of the ethnic drug Dicranopteris pedata. METHODS The compounds were isolated and purified by comprehensive application of silica gel and Sephadex LH-20 chromatography, and their structures were identified on the basis of comprehensive analysis of their physical and chemical properties, NMR data and references. RESULTS Fourteen compounds were isolated and elucidated as quercitrin(1), kaempferol 3-O-??-L-rhamnoside(2), rutin(3), hyperoside(4), kaempferol(5), quercetin(6), 2-hydroxy-4-methoxy-2??, 3??-benzochalcone(7), stigmasterol(8), cycloastragenol(9), shikimic acid(10), protocatechuic acid(11), gallic acid(12), ??-sitosterol(13), and daucosterol(14). CONCLUSION Compound 1-14 are for the first time isolated from D. pedata.     

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??OBJECTIVE To investigate the effects of interferon-??(IFN-??) and all-trans retinoic acid(ATRA) on multidrug resistance reversal effect and mechanism of human leukemia K562/ADM cells. METHODS The cytotoxicity and reversal times of IFN-?? and ATRA were detected by CCK-8 method. Apoptosis rate and cell cycle were detected by flow cytometry. PI3K, Akt and Bad mRNA were detected by RT-PCR method. Western blot method was used to detect the expression of PI3K, AKt, P-AKt and Bad protein.RESULTS The drug resistance of K562/ADM cells to adriamycin(ADM) was 54 times. ADM, respectively, with IFN-??, ATRA or combined application, the drug resistance of K562/ADM cells to ADM was 1.24, 2.34 and 8.14, respectively. The apoptosis rate of K562/ADM cells was significantly increased by using ADM 4 mg??L^-1alone or in combination with IFN-?? 2.5??10⁶ U??L^-1, ATRA 7.5 ??mol??L^-1, and the cell cycle was blocked in G₀/G₁ phase. PI3K mRNA and protein expression were significantly lowered, Akt mRNA and protein has no obvious change, Bad mRNA and protein expression are raised, phosphorylated Akt protein expression decreased, the expression is more obvious when the two drug combination. CONCLUSION IFN-?? and ATRA can reverse the multidrug resistance of K562/ADM cells, its mechanism may be the inhibition of the PI3K/Akt pathway.     

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??OBJECTIVE To investigate the mechanism and the protective effect of arginyl-fructosyl-glucose(AFG) on the kidney of diabetic nephropathy(DN) mice and the correlation between TGF-??1 and collagen ??. METHODS Twelve mice were randomly selected as control group; all others were induced by streptozotocin (STZ). The mice were randomly divided into 5 groups, each of which has 12 mice, DN model group, metformin group, 10,20,40 mg??kg^-1 AFG group; each group was treated for 5 weeks, during when mice were weighed weekly and blood glucose concentration were measured. At the end of 5 weeks, the final body weight and the renal index of the mice was calculated; 24 h urinary protein and blood biochemical indexes were recorded (TC, TG, HDL-C, SCr, BUN, SOD, GSH, CAT, T-AOC); the pathological changes of the kidney was observed using HE staining. The expressions of TGF-??1 and collagen ?? mRNA in kidneys were detected by real-time fluorescence quantitative PCR (RT-PCR). RESULTS The levels of urinary protein, TC, TG and HDL-C in the AFG group were significantly lower than those in the control group. The contents of SOD, GSH, CAT and T-AOC in the AFG-treatment group were significantly higher than those in the control group. Pathological condition was relieved; the mRNA expression of TGF-??1 and collagen ?? in the kidneys of each dose group was significantly lower than that of the control group. CONCLUSION AFG protects the kidneys by reducing the total amount of 24 h urinary protein, decreasing renal pathological damage and decreasing the expression of TGF-??1 and collagen ?? genes in kidney.     

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??OBJECTIVE To study the chemical constituents of the aqueous extract from the aerial part of Sibiraea angustata. METHODS The constituents were isolated by various chromatographic techniques(HP-20 macroporous absorption resin, Sephadex LH-20 gel, Reverse-phase silical gel and PHPLC) and their structures were determined on the basis of physicochemical properties and their spectroscopic data, as well as the literatures. RESULTS Twelve compounds were separated and identified as veratric acid(1),(+)-cycloolivil(2), 3,7-dimethyl-3(E)-6-octadien-5-one-1-O-??-D-glucoside(3), 3,7-dimethyl-3(Z)-6-octadien-5-one-1-O-??-D-glucoside(4), 1-O-??-D-glucopyranosyl(1??2)-??-D-glucopyranosyl-3,7-dimethyl-2(E)-6-heptdiene(5),(7R,8S)-dihydrodehydrodiconiferyl alcohol-9??-O-??-D-glucopyranoside(6),(+)-1-hydroxypinoresinol-1-??-D-glucoside(7), skimmin(8), kaempferol 3-O-??-L-arabinopyranosyl-(1??6)-??-D-galactopyranoside(9), isorhamnetin-3-O-??-D-galactopyranosyl(1??6)-??-D-glucopyranoside(10), isorhamnetin 3-O-??-arabinopyranosyl-(1??6)-??-galactopyranoside(11), and quercetin 3-O-[2''-O-(E)-caffeoyl]-??-L-arabinopyranosyl-(1??6)-??-D-galactopyranoside(12). CONCLUSION All compounds are obtained from the genus of Sibiraea for the first time.