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??OBJECTIVE To study the chemical constituents of the ethyl acetate fraction from the stems of Saprosma merrillii Lo. METHODS The compounds were isolated and purified by silica gel column and Sephadex LH-20 column. Their structures were elucidated on the basis of chemical properties and spectral analysis. RESULTS Ten compounds were isolated and elucidated as 5-hydroxylmethylfuraldehyde(1), 3??-hydroxycholesta-5-ene(2), scopoletin(3), isoscopoletin(4), quercetin-3-O-glucoside-6??-gallate(5), 4??-hydroxy-7-methoxy flavanone(6), pinoresinol(7), N-trans-coumaroyltyramine(8), luteolin-7-O-B-D-glucopyranoside(9), and hypodiolide A(10). CONCLUSION All of the compounds are isolated from this genus for the first time except for compound 3     

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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.
     

GC法测定高良姜醇提物中两个二苯基庚烷类化合物

目的建立高良姜醇提物中2个二苯基庚烷类化合物的测定方法。方法采用GC法,色谱柱为Cp Sil 5CB(30 m×0.25 mm,0.25μm)石英毛细管柱;检测器:FID;柱温:初始温度80℃,保持2 min,以20℃/min升温到300℃,保持45 min。结果 1-苯基-7-(3’-甲氧基-4’-羟基)苯基-5-醇-3-庚酮在0.2～1.0 mg/mL(r=0.998 8)、1,7-二苯基-5-醇-3-庚酮在0.2～1.0 mg/mL(r=0.997 8)有较好的线性关系;平均回收率分别为99.6%、100.6%。结论本方法可靠、专属性强,可作为高良姜醇提物中2个二苯基庚烷类化合物的测定方法。     

3′,5′-二辛酰基-5-氟尿嘧啶脱氧核苷的合成及性质研究

 目的 研究5-氟尿嘧啶脱氧核苷 (FUdR)的前体药物3′,5′-二辛酰基-5-氟尿嘧啶脱氧核苷(DO-FUdR)的合成路线、降解规律和体外抗肿瘤细胞增殖活性。方法 通过酯化反应合成了DO-FUdR, 采用MS,NMR等进行了鉴定; HPLC测定DO-FUdR在不同pH 值缓冲液和小鼠组织匀浆中浓度的变化, 计算其在不同介质中的降解速率常数, 并测定了DO-FUdR的溶解度和分配系数;3H-TdR掺入法测定了DO-FUdR对U251星型胶质瘤细胞体外增殖活性的抑制作用。结果 合成化合物为DO-FUdR; 其在缓冲溶液和组织匀浆中的降解过程符合表观一级反应; 与FUdR具有相似的抗胶质瘤细胞增殖活性。结论 DO-FUdR是一种值得进行进一步研究和开发的前体药物。     

绒毛钩藤中1个新的3，4-二氢-β-咔啉型生物碱3，4-去氢-5（S）-5-羧基长春花碱的合成和绝对构型

曾从茜草科植物绒毛钩藤(Uncaria tomentosa)中首次分离得到1个新的3,4-二氢-β-咔啉环系统的类单萜葡糖吲哚生物碱3,4-去氢-5(S)-5-羧基长春花碱(1)以及该植物中的主要生物碱5(S)-5-羧基长春花碱(2)。化合物1的结构除绝对构型外,从光谱分析推断为化合物2的3,4-去氢化合物,化合物2由开联番木鳖苷(3)和L-色氨酸(4)组成。本次报道了化合物1的合成及其结构测定。     

4-羟基-3,5-二甲氧基苯甲酰甘氨酸的合成研究

目的　合成 4 -羟基 - 3,5 -二甲氧基苯甲酰甘氨酸。方法　以丁香酸为起始原料 ,经乙氧羰基化、酰氯化、酰胺化、水解四步反应制得。结果　经波谱数据及元素分析认为合成的产物为目标产物。结论　所得化合物作为 N- (4 -羟基 - 3,5 -二甲氧基苯甲酰基 ) -甘氨酰正丁基胍的中间体 ,实验还需进一步探讨改进     

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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.
     

猫爪草化学成分的研究(Ⅱ)

 目的研究猫爪草的化学成分。方法经柱色谱分离,理化常数和光谱分析鉴定化合物结构。结果从氯仿部分得到8个化合物,分别为邻苯二甲酸正丁酯(Ⅰ),β-单棕榈酸甘油酯(Ⅱ),β-单硬脂酸甘油酯(Ⅲ),2-氨基-3-(3,4-二羟基-苯基)-丙酸甲酯(Ⅳ),2-氨基-3-(3,4-二羟基-苯基)-丙酸乙酯(Ⅴ),5-羟甲基糠醛(Ⅵ),5-羟甲基糠酸(Ⅶ),维太菊苷(Ⅷ)。结论Ⅰ, Ⅱ,Ⅲ,Ⅵ,Ⅶ系首次从毛茛属中得到,Ⅳ,Ⅴ为提取分离过程中人工产物。     

Synthesis of ramosetron hydrochloride

目的 研究盐酸雷莫司琼的合成工艺.方法 主要是以4,5,6,7-四氢苯并咪唑-5-羧酸甲酯硫酸盐为中间体,经乙酰化、芳香环碳酰化制备1-乙酰基-5-[(1-甲基吲哚-3-基)羰基]-4,5,6,7-四氢苯并咪唑,此化合物再经水解、拆分得到盐酸雷莫司琼.结果 本工艺所得盐酸雷莫司琼总收率为21.2％.结论 盐酸雷莫司琼的合成工艺稳定,操作简便,适合工业化生产.     

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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 chemical constituents of Yao medicine, Zhongliuteng, the stems of Pileostegia tomentella. METHODS The chemical constituents were isolated and purified by silica gel chromatography repeatedly, and their structures were identified by spectral analysis and chemical METHODS. RESULTS Thirteen compounds were isolated from the stems of P. tomentella and the structures were identified as 1-O-(??-D-glucosyl)-2-[2-methoxy-4-(??-hydroxypropyl) phenoxy]propan-3-ol(1),(+)-lyoniresinol-3a-O-??-D-glucopyranoside (2),syringin (3),coniferin (4),dihydroconiferin (5),but-3-enyl-??-D-glucoside (6),4-(2,3-dihydroxypropyl)-2,6-dimethoxy phenyl ??-D-glucopyranoside (7),nikoenoside (8),protocatechuic acid ethyl ester (9),8-methoxy coumarin-7-O-??-D-glucopyranoside (10),6-O-R-L-rhamnopyranosyl-??-D-glucopyranoside methyl salicylate (11), nicotinamide (12), and 3,5-di-O-caffeoyl quinicacid methyl ester (13). CONCLUSION All compounds were obtained from the genus for the first time.     

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??OBJECTIVE To study the chemical constituents of Magnolia biondii.Pamp. METHODS The compounds were isolated and purified by Diaion HP-20, Toyopearl HW-40, silica gel column chromatography and semi-preparative HPLC and so on. The structures were elucidated on the basis of spectral data and physiochemical properties. RESULTS Fourteen compounds were isolated and identified as 4-O-??-D-glucopyranosylvanillic acid(1), tachinoside(2), methyl 4-hydroxy-3-methoxybenzoate(3), caffeic acid(4), 3,4,5-trimethoxyphenyl-??-D-glucopyranoside(5), benzyl-O-??-D-glucopyranoside(6), benzyl-O-??-D-galactopyranoside(7), syringin(8), vanillic acid glucosyl ester(9), vanillic acid(10), 1??-(3,4-dihydroxycinnamoyl)cyclopentane-2??,3??-diol(11), scopolin(12),7-methoxycoumarin-6-O-??-D-glucopyranoside(13), and scopoletin(14). CONCLUSION Compounds 1-9 and 11-13 are isolated from this plant for the first time.     

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??OBJECTIVE To investigate the liposoluble constituents of Urticae Rhizoma. METHODS The compounds were isolated and purified by silica gel, Sephadex LH-20, ODS gel column chromatographies, and semi-preparative HPLC. The structures were elucidated on the basis of spectral data and physiochemical properties. RESULTS Twenty-one compounds were isolated from the ethyl acetate fraction of Urticae Rhizoma, and identified as(-)-urticol(1),(-)-secoisolariciresinol(2), 23-hydroxybetulinic acid(3), 2??,3??, 24-trihydroxy-12-oleanen-28-oic acid(4), cleomiscosin A (5), dihydro-4-hydroxy-5-hydroxymethyl-2(3H)-furanone(6), methyl chlorogenate(7), kaempferol(8), pinoresinol monomethyether-4??-O-??-D-glucopyranoside(9), martairesinol-4??-O-??-D-glucopyranoside(10), cycloolivil-6-O-??-D-glucopyranoside(11), stigmasterol-3-O-??-D-glucopyranoside(12), nicotinamide(13), trans-caffeic acid-4-O-??-D-glucopyranoside(14), esculin(15), 5-hydroxyl-7-methoxycoumarin-8-O-??-D-glucopyranoside(16), 6-oxymethyluteolin-7-O-??-D-glucopyranoside(17), luteolin-7-O-??-D-glucopyranoside(18), quercetin-3-O-(4??-methoxy)-??-L-rhamnopyranoside(19), 2??-deoxy uridine(20), and apigenin-6, 8-di-C-??-D-glycoside(21), respectively. CONCLUSION All the compounds, except 8 and 12, are isolated from U. fissa for the first time. Meanwhile, compounds 5, 6, 9, 10, 11, 14, 16, 17, and 19 are all found in Urticaeae plants for the first time.     

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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 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 the stems of Viola japonica var. stenopetala Franch. ex H.METHODS The constituents were isolated and purified by silica gel, Sephadex LH-20 column chromatography, and preparative TLC. The structures were identified on the basis of spectral data and physiochemical characteristics. RESULTS Fifteen compounds were isolated from 70% ethanol extract of Viola japonica var. stenopetala Franch. ex H. and identified as ??-sitosterol (1), daucosterol(2), chlorogenic acid (3), 7-hydroxycoumarin (4), stigmastero-3-O-??-D-glucopyranoside (5), dehydrololiolide (6), kaempferol-7-O-??-D-glucopyranoside (7), characterizedas(+)-pinoresinol-O-??-D-glucopyranoside (8), 5,7-dihydroxy-3,6-dimethoxyflavone (9), apigenin-7-O-??-D-glucoside (10), chryseriol (11), ??-amyrin(12), robinin(13), kaempferol-3,7-di-O-??-L-rahmnoside(14), and solagenin-6-O-??-D-quinovopyranoside(15). CONCLUSION Compounds 8 and 15 are isolated from the plants in Gnaphalium L. for the first time. Compounds 5, 6, 8, 11, 14, and 15 are isolated from this plant material 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 bioactivity and chemical constituents of different polar parts from blueberry leaves. METHODS Blueberry leaves were extracted by ethanol and then the extract was sequentially partitioned into five fractions. Silicagel and Sephadex LH-20 chromatographic methods were applied to isolate and purify compounds. Their structures were elucidated by physiochemical properties and spectral analysis.The DPPH?? radical scavenging activity, ??-glycosidase and pancreatic lipase inhibition activity of different polar parts and partial compounds were determined. RESULTS The n-butyl alcohol fraction(BF) showed the highest DPPH?? radical scavenging activity and ??-glycosidase inhibition activity. The ethyl acetate fraction(EAF) showed the strongest pancreatic lipase inhibition activity. A total of five compounds were isolated from the EAF, and their structures were identified as ??-sitosterol(1), quercetin-3-O-??-L-arabinofuranoside(2), quercetin(3), quercetin-3-O-??-D-glucopyranoside(4) and 1-O-caffeoylquinic acid(5). A total of two compounds were isolated from the BF, and their structures were identified as quercetin-3-O-??-L-arabinoside(6) and quercetin-3-O-??-D-glucuronide(7). The results showed that compounds 3 and 5 had very good DPPH?? radical scavenging and pancreatic lipase inhibitory activity, and compounds 1 and 3 had good ??-glucosidase inhibitory activity. CONCLUSION The different polar parts and compounds of blueberry leaves show strong DPPH?? radical scavenging activity, ??-glycosidase and pancreatic lipase inhibition activity. Compounds 1, 2, 5 and 6 are isolated from blueberry leaves for the first time.     

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??OBJECTIVE To study the chemical constituents of Erigeron annuus (L.) Pers.. METHODS The compounds were isolated and purified by Diaion HP-20, Toyopearl HW-40, Sephadex LH-20, MCI Gel CHP-20, silica gel column chromatography, and preparative HPLC, and their structures were elucidated on the basis of spectral data and physiochemical properties. RESULTS Twenty compounds were elucidated as vanillic acid(1), ferulic acid(2), 4-hydroxyacetophenone(3), dihydroconiferylalcohol(4), loliolide(5), 4-hydroxy-3-methoxyphenylprop-8-ene 4-O-??-D-xylopyraosyl-(1??6)-??-D-glucopyranoside(6), 1H-indole-3-carbaldehyde(7), 5,7-dihydroxychromone(8), pyromeconic acid(9), erigeside D(10), methyl syringate 4-O-??-D-glucopyranoside(11),(7S,8R)-urolignoside(12), homoeriodictyol(13), pinobaksin(14), chrysin(15), hispidulin(16), chryseriol(17), cyclomorusin(18), cirsimaritin(19), and naringenin(20), respectively. CONCLUSION Compounds 1-8 and 11-19 is 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.