黄素馨化学成分及其抗氧化活性

对黄素馨Jasminum giraldii根皮的化学成分进行研究。采用正相硅胶、Sephadex LH-20以及Rp-HPLC制备柱色谱法,从黄素馨乙醇提取物的乙酸乙酯萃取部位中分离得到10个化合物,通过MS和NMR等谱学方法,鉴定结构为（+）-梣皮树脂醇（1）,（+）-丁香树脂醇（2）,（+）-丁香脂素-4’-O-β-D-葡萄糖苷（3）,齐墩果酸（4）,3-甲氧基-4-羟基桂皮醛（5）,芥子醛（6）,3,5-二甲氧基对羟基苯甲醛（7）,1-（4-甲氧基苯基）乙醇（8）,反式桂皮酸（9）,4-（1-甲氧基乙基）苯酚（10）。化合物1~3,5~8以及10为首次从素馨属植物中分离得到;化合物4和9为首次从该植物中分离得到。采用 DPPH自由基清除法对分离得到的化合物进行抗氧化活性的筛选。结果显示,化合物1显示出强的自由清除能力（IC₅₀为55.1 μmol·L^-1）,活性强于维生素C（IC₅₀为59.9 μmol·L^-1）,化合物2显示中等强度自由清除能力（IC₅₀为79.0 μmol·L^-1）,活性弱于维生素C,但强于2,6-二羟丁基对甲酚（IC₅₀为236 μmol·L^-1）。     

珍珠菜中黄酮苷类成分研究

研究珍珠菜Lysimachia clethroides的黄酮苷类成分。珍珠菜乙醇提取物经硅胶、Sephadex LH-20和Pre-HPLC等色谱技术分离纯化,通过质谱和核磁共振等波谱学方法鉴定化合物的结构。从珍珠菜中分离得到11个黄酮苷类化合物,分别鉴定为紫云英苷(1),异槲皮苷(2),异鼠李素-3-O-β-D-吡喃葡萄糖苷(3),槲皮素-3-O-β-D-6"-乙酰基吡喃葡萄糖苷(4),槲皮素-7-O-β-D-吡喃葡萄糖苷(5),江户樱花苷(6),2-羟基-柚皮素-5-O-β-D-吡喃葡萄糖苷(7),山柰酚-3-O-芸香糖苷(8),山柰酚-3-O-洋槐糖苷(9),芦丁(10),山柰酚-3,7-二-O-β-D-吡喃葡萄糖苷(11)。化合物4, 7和11为首次从该属植物中分离得到,化合物3 、 5和9为首次从该种植物中分离得到。体外活性测试结果显示化合物2, 6, 8具有一定的醛糖还原酶抑制活性,IC₅₀分别为2.69,1.00,1.80 μmol·L^-1;化合物1 ~ 11对5种人肿瘤细胞均没有明显的细胞毒活性(IC₅₀ > 10 μmol·L^-1)。     

蝉翼藤根中的皂苷类成分及其肿瘤细胞毒活性

采用硅胶柱色谱、MPLC、制备与半制备HPLC等分离技术从蝉翼藤根的95%乙醇提取物中分离得到7个乙酰化的三萜皂苷类化合物。通过理化性质和MS,NMR等波谱数据鉴定其结构分别为蝉翼藤皂苷A(1),蝉翼藤皂苷B(2),3-O-β-D-glucopyranosyl presenegenin 28-O-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-[β-D-glucopyranosyl-(1→3)]-4-O- [(E)-3,4-dimethoxycinnamoyl]-β-D-fucopyranosyl ester (3), 3-O-β-D-glucopyranosyl presenegenin 28-O-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-[β-D- glucopyranosyl-(1→3)]-4-O- [(E/Z)-3,4-dimethoxycinnamoyl]-β-D-fucopyranosyl ester(3/4),3-O-β-D-glucopyranosyl presenegenin 28-O-α-L-arabinopyranosyl-(1→3)-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-4-O-[(E)-3,4-dimethoxycinnamoyl]-β-D-fucopyranosyl ester(5),远志皂苷XLV(6),远志皂苷XLVI(7)。其中化合物 5~7 为首次从该属植物中分离得到,化合物 3,3/4 为首次从该种植物中分离获得。采用MTT法对所得化合物进行抗肿瘤活性评价,结果表明化合物 2,3/4,5 对肺癌细胞株LLC具有中等抑制作用,其IC₅₀分别为41.10, 38.17, 48.92 μmol·L^-1;化合物 2对乳腺癌细胞株MCF-7有中等抑制作用,其IC₅₀为47.93 μmol·L^-1。     

长穗桑中的α-葡萄糖苷酶抑制剂成分研究

 目的 研究长穗桑中具有α-葡萄糖苷酶抑制活性的化学成分。方法 采用各种离子交换树脂对长穗桑水提取物进行分离纯化,通过NMR、MS等波谱分析手段鉴定化合物结构。结果 从长穗桑水提取物中分离到11个化合物,其中7个多羟基生物碱类化合物,2个酰胺类化合物,1个氨基酸以及甜菜碱。分别鉴定为1-deoxynojirimycin (1),fagomine (2),3-epi-fagomine (3),1,4-dideoxy-1,4-imino-D-arabinitol (4),2-O-α-D-galactopyranosyl-1-deoxynojirimycin (5),4-O-β-D-glucopyranosyl-fagomine (6),1,4-dideoxy-1,4-imino-(2-O-β-D-glucopyranosyl)-D-arabinitol (7),(2S)-citrullinamide (8),grateloupinamide (9),天冬氨酸(10),甜菜碱(11)。化合物1~10分别进行了α-葡萄糖苷酶抑制活性筛选。结论 化合物1~11均为首次从该植物中分离得到。4个多羟基生物碱(1,5~7)以及1个酰胺类化合物(9)有较强的α-葡萄糖苷酶抑制活性,其中化合物1的IC₅₀为0.07 μmol·L^-1;化合物5的IC₅₀为0.39 μmol·L^-1,与阳性对照阿卡波糖(acarbose,IC₅₀=0.52 μmol·L^-1)相当;化合物6,7,9的IC₅₀值在1~5 μmol·L^-1。     

吊球草的化学成分及抑菌活性研究

研究吊球草Hyptis rhomboidea的化学成分,并对部分单体化合物进行抑菌活性测定。采用Toyopearl HW-40,Sephadex LH-20,MCI-Gel CHP-20,RP-18,PTLC及硅胶等色谱法对吊球草进行化学成分研究,根据理化性质和波谱技术鉴定化合物的结构,并评价部分单体化合物对8种植物病原菌的抑菌活性。从乙酸乙酯部位中共分离鉴定了11个化合物,分别为咖啡酸乙酯（1）、熊果酸（2）、齐墩果酸（3）、vanillactic acid（4）、迷迭香酸甲酯（5）、山柰酚-3-O-α-L-吡喃鼠李糖-（1→6）-β-D-吡喃葡萄糖苷（6）、山柰酚-3-O-α-L-吡喃鼠李糖-（1→2）-β-D-吡喃葡萄糖苷（7）、冬青素A（8）、β-香树脂醇（9）、山柰酚-3-O-β-D-吡喃葡萄糖苷（紫云英苷,10）和胆甾-5-烯-3β,4β-二醇（11）。其中化合物1对核盘菌的抑制活性最强,MIC为16.2 mg·L^-1,化合物5对玉米大斑病菌和小核盘菌的抑制活性最强,MIC分别为8.1,16.2 mg·L^-1。所有化合物均为首次从该植物中分离得到,化合物1 ,5具有较强的抗真菌活性。     

美洲刺人参酚类化学成分研究

利用正向硅胶、反相硅胶、Sephadex LH-20和制备液相色谱等多种分离技术进行分离纯化,依据理化性质和波谱数据鉴定结构,从美洲刺人参Oplopanax horridus的根皮醇提物乙酸乙酯和正丁醇萃取部位分离并鉴定了16个酚类化合物,其中7个苯丙素类成分阿魏酸（1）,3-乙酰咖啡酸（2）,咖啡酸（3）,3-甲氧基二氢肉桂醇-4-O-β-D-葡萄糖苷（4）,3-羟基二氢肉桂醇-4-O-β-D-葡萄糖苷（5）,3,5-二甲氧基肉桂醇-4-O-β-D-葡萄糖苷（6）,3-甲氧基肉桂醇-4-O-β-D-葡萄糖苷（7）;3个香豆素类成分,东莨菪内酯（8）,6,7-二羟基香豆素（9）,反式-3’-当归酰基-4’-乙酰基角型吡喃香豆素（10）;6个木脂素类成分,（+）-异落叶松脂素9’-O-β-D-葡萄糖苷（11）,3,3’-二甲氧基-4,9,9’-三羟基-4’,7-环氧-5’,8-木脂素-4,9-O-β-D-二葡萄糖苷（12）,（+）-5,5’-二甲氧基落叶松脂素 4’-O-β-D-葡萄糖苷（13）,（-）-5,5’-二甲氧基落叶松脂素 4’-O-β-D-葡萄糖苷（14）,（-）-松脂醇 4’-O-β-D-葡萄糖苷（15）,（±）-5,5’-二甲氧基落叶松脂素 9’-O-β-D-葡萄糖苷（16）。所有化合物均为首次从该植物中分离得到,除化合物4,6,12和13外,其余化合物均为首次从该属植物中报道。     

掌叶梁王茶茎皮的化学成分研究

利用各种现代色谱方法从掌叶梁王茶Nothopanax delavayi茎皮70%乙醇提取物中分离得到11个化合物,通过波谱技术和理化性质鉴定它们的结构为三对节酸3-O-α-L-吡喃阿拉伯糖-28-O-β-D-吡喃葡萄糖酯苷（1）,三对节酸3-O-α-L-吡喃阿拉伯糖-28-O-α-L-吡喃鼠李糖-（1→4）-β-D-吡喃葡萄糖-（1→6）-β-D-吡喃葡萄糖酯苷（2）,三对节酸（3）,三对节酸3-O-α-L-吡喃阿拉伯糖苷（4）,三对节酸3-O-β-（2’,4’-O-二乙酰基）-D-吡喃木糖-28-O-α-L-吡喃鼠李糖-（1→4）-β-D-吡喃葡萄糖-（1→6）-β-D-吡喃葡萄糖酯苷（5）,三对节酸3-O-α-（4’-O-乙酰基）-L-吡喃阿拉伯糖-28-O-α-L-吡喃鼠李糖-（1→4）-β-D-吡喃葡萄糖-（1→6）-β-D-吡喃葡萄糖酯苷（6）,三对节酸3-O-α-（2’-O-乙酰基）-L-吡喃阿拉伯糖-28-O-α-L-吡喃鼠李糖-（1→4）-β-D-吡喃葡萄糖-（1→6）-β-D-吡喃葡萄糖酯苷（7）,三对节酸3-O-β-D-吡喃木糖-28-O-α-L-吡喃鼠李糖-（1→4）-β-D-吡喃葡萄糖-（1→6）-β-D-吡喃葡萄糖酯苷（8）,原儿茶酸（9）,咖啡酸乙酯（10）,咖啡酸酐（11）。其中化合物3~4,9~11为首次从梁王茶属植物中分离得到,化合物5~8为首次从该植物中分离得到。     

鬼针草化学成分研究

对鬼针草Bidens bipinnata中的化学成分进行研究,筛选具有抗肝纤维化活性单体。采用大孔树脂、硅胶、MCI树脂、Sephadex LH-20等方法进行分离纯化,得到15个化合物,并运用波谱技术测试,鉴定其结构为槲皮素（1）,槲皮素-3-O-α-L-鼠李糖苷（2）,紫云英苷（3）,山柰酚-3-O-α-L-鼠李糖苷（4）,5,3’-二羟基-3,6,4’-三甲氧基-7-O-β-D-吡喃葡萄糖苷黄酮（5）,7,8,3’,4’-四羟基二氢黄酮（6）,（R/S）-异奥卡宁-7-O-β-D-葡萄糖苷（7）,（R/S）-异奥卡宁-3’-甲氧基-7-O-β-D-葡萄糖苷（8）,6,7,3’,4’-四羟基橙酮（9）,海生菊苷（10）,6,7-二羟基香豆素（11）,3-咖啡酸酰基-2-甲基-D-赤藓糖酸-1,4内酯（12）,（7S,8R）苯并二氢呋喃新木脂素-4-O-β-D-葡萄糖苷（13）,丁香酚-O-β-D-呋喃芹糖-（1"-6’）-O-β-D-吡喃葡萄糖苷（14）,（+）丁香脂素-4-O-β-D-吡喃葡萄糖苷（15）。其中化合物8,13~15为首次从本属植物中分离得到。在初步的活性筛选中化合物 1,6有较强体外抑制肝星状细胞增殖的能力;化合物1,2,6,7有较强体外抑制腹腔巨噬细胞分泌炎症因子的能力。     

杭白菊中黄酮类化合物及其抑制人源肿瘤细胞增殖活性的研究

 目的 分离和鉴定杭白菊中黄酮类化合物并对其进行抗肿瘤活性研究。方法 利用系统溶剂萃取法、聚酰胺柱色谱、半制备型高效液相色谱法分离。通过理化性质和IR、UV、MS、¹H-NMR、¹³C-NMR等光谱数据鉴定化合物。采用MTT法测定化合物对人肿瘤细胞增殖的影响, 并以氟尿嘧啶（5-FU）作为阳性对照,比较其对正常细胞的毒性作用。流式细胞术检测细胞周期分布的改变。结果 分离得到8个黄酮化合物单体,分别鉴定为木犀草素(Ⅰ),木犀草素7-O-β-D-葡萄糖苷(Ⅱ),木犀草素7-O-β-D (6″-O-丙二酸单酰) -葡萄糖苷(Ⅲ),芹菜素(Ⅳ),芹菜素 7-O-β-D-葡萄糖苷(Ⅴ),芹菜素 7-O-β-D-(6″-O-丙二酸单酰)-葡萄糖苷(Ⅵ),香叶木素(Ⅶ),香叶木素 7-O-β-D-葡萄糖苷(Ⅷ)。MTT法测定木犀草素抑制乳腺癌MDA-MB-231细胞 和肝癌SMMC-7721细胞的IC₅₀分别为56.67和72.92 μmol·L^-1。结论 化合物Ⅲ和Ⅵ首次从杭白菊中分离得到。木犀草素能抑制MDA-MB-231和SMMC-7721增殖,阻滞其细胞周期于G2/M期,且对正常细胞无毒性。     

刺萼龙葵化学成分研究

对刺萼龙葵Solanum rostratum地上部分的化学成分进行研究。采用硅胶,Sephadex LH-20,ODS柱色谱及半制备HPLC等方法进行分离和纯化,根据理化性质和波谱数据鉴定化合物结构。从刺萼龙葵地上部分分离得到10个化合物,分别鉴定为薯蓣皂苷（1）,hypoglaucin H（2）,金丝桃苷（3）,异槲皮苷（4）,异鼠李素-3-O-β-D-半乳糖苷（5）,山柰酚-3-O-β-D-葡萄糖苷（6）,smilaxchinoside A（7）,26-O-β-D-吡喃葡萄糖基-3β,20α,26-三醇-25（R）-Δ^5,22-二烯-呋甾-3-O-α-L-吡喃鼠李糖基（1→2）-[α-L-吡喃鼠李糖基（1→4）]-β-D-吡喃葡萄糖苷（8）,β-谷甾醇（9）,胡萝卜苷（10）,其中化合物 7 和 8 为首次从茄属植物中分离得到,其余8个化合物为首次从该植物中分离得到。     

Investigation of plant extracts in traditional medicine of the Brazilian Cerrado against protozoans and yeasts

Aim of the study

To investigate the activities of the 217 plant extracts in traditional medicine of the Brazilian Cerrado against protozoans and yeasts.

Materials and methods

Plant extracts were prepared by the method of maceration using solvents of different polarities. The growth inhibition of chloroquine-resistant Plasmodium falciparum strain (FcB1) was determined by measuring the radioactivity of the tritiated hypoxanthine incorporated. Activity against Leishmania (Leishmania) chagasi and Trypanosoma cruzi was measured by the MTT colorimetric assay. The antifungal tests were carried out by using the CLSI method. The active extracts were tested also by cytotoxicity assay using NIH-3T3 cells of mammalian fibroblasts.

Results

Two hundred and seventeen extracts of plants were tested against Plasmodium falciparum. The eleven active extracts, belonging to eight plant species were evaluated against L. (L.) chagasi, Trypanosoma cruzi, yeasts and in NIH-3T3 cells. The results found in these biological models are consistent with the ethnopharmacological data of these plants. The ethyl acetate extract of Diospyros hispida root showed IC₅₀ values of 1 μg/mL against Plasmodium falciparum. This extract demonstrated no toxicity against mammalian cells, resulting in a significant selectivity index (SI) of 435.8. The dichloromethane extract of Calophyllum brasiliense root wood was active against Cryptococcus gattii LMGO 01 with MIC of 1.95 μg/mL; and Candida albicans ATCC 10231 and Candida krusei LMGO 174, both with MIC of 7.81 μg/mL. The same extract was also active against Plasmodium falciparum and L. (L.) chagasi with IC₅₀ of 6.7 and 27.6 μg/mL respectively. The ethyl acetate extract of Spiranthera odoratissima leaves was active against Cryptococcus gattii LMGO 01 with MIC of 31.25 μg/mL, and against Plasmodium falciparum with IC₅₀ of 9.2 μg/mL and Trypanosoma cruzi with IC₅₀ of 56.3 μg/mL.

Conclusion

The active extracts for protozoans and human pathogenic yeasts are considered promising to continue the search for the identification and development of leading compounds.     

Effect of feeding Mucuna pruriens on helminth parasite infestation in lambs

Ethnopharmacological relevance

Mucuna pruriens is a tropical legume anecdotally reputed to have anthelmintic properties. This study was conducted to examine the validity of such claims.

Aim of the study

The aim of this study was to determine if ingestion of Mucuna seeds reduces helminth parasite infestation in lambs.

Materials and methods

Thirty-six Dorper × Katahdin ram lambs were assigned to three treatments, a cottonseed meal based control diet, a diet in which Mucuna replaced cottonseed meal and the control diet with levamisole (7.5 mg/kg body weight) administration. All diets were isonitrogenous and isocaloric. The 12 lambs in each treatment were assigned randomly to 4 pens, each containing 3 lambs. Lambs were trickle infected three times per week by gavage with infectious Haemonchus contortus larvae (2000 larvae/lamb) for 3 weeks.

Results

Levamisole treatment decreased fecal egg counts by 87% and abomasal worm counts by 83%. Mucuna intake did not statistically affect fecal egg counts or abomasal worm counts, though numerical (P > 0.10) reductions of 7.4% and 18.1%, respectively were evident. Anemia indicators, feed intake, and lamb growth were unaffected by treatment.

Conclusions

Levamisole reduced the Haemonchus parasite burden in lambs significantly but feeding Mucuna reduced the burden by levels unlikely to eliminate the clinical effects of parasitism.     

Screening of the topical anti-inflammatory activity of the bark of Acacia cornigera Willdenow, Byrsonima crassifolia Kunth, Sweetia panamensis Yakovlev and the leaves of Sphagneticola trilobata Hitchcock

Ethnopharmacological relevance

An investigation of topical anti-inflammatory activity was undertaken on plants used in Central America traditional medicine.

Aim of study

Four herbal drugs used in the folk medicine of Central America to treat inflammatory skin affections (Acacia cornigera bark, Byrsonima crassifolia bark, Sphagneticola trilobata leaves and Sweetia panamensis bark) were evaluated for their topical anti-inflammatory activity.

Materials and methods

Petroleum ether, chloroform and methanol extracts were obtained for herbal medicines and then extracts were tested on Croton oil-induced ear dermatitis model in mice.

Results

Almost all the extracts reduced the Croton oil-induced ear dermatitis in mice and the chloroform ones showed the highest activity, with ID₅₀ (dose giving 50% oedema inhibition) values ranging from 112 μg/cm² (Byrsonima crassifolia) to 183 μg/cm² (Sphagneticola trilobata). As reference, ID₅₀ of the non-steroidal anti-inflammatory drug indomethacin was 93 μg/cm².

Conclusions

Lipophilic extracts from these species can be regarded as potential sources of anti-inflammatory principles.     

中国石斛属植物文献计量研究

石斛是珍稀濒危中药材,目前正处于快速发展阶段。为全面了解我国石斛属植物研究的历史和发展现状,作者以1954～2010年"中国知网中国学术期刊网络出版总库"收录的石斛研究文献为依据,采用文献计量学的原理和方法,对我国石斛属植物研究文献从文献年代分布、期刊分布与被引频率、主题分布、研究对象分布、作者与研究机构分布等方面进行了统计与分析。结果表明,我国石斛研究明显分为起步(2个)、停滞、平稳发展、快速上升5个阶段;期刊分布存在离散性与集中性并存的现象,已形成核心期刊研究群,并以《中国中药杂志》、《中草药》和《陕西中医》为代表;研究主题广泛涉及临床与药理、组织培养与种苗繁育、成分分析等多个领域,已经形成比较稳定的研究机构和团队,但研究对象差异显著,以铁皮石斛、金钗石斛和霍山石斛最为集中。我国石斛属植物的研究已取得显著成果,但种植产业发展缓慢,供需矛盾突出,预计种苗繁育与人工种植、产品开发、化学与药理等方面是未来的研究热点,其文献报道仍将进一步上升。     

厚朴与凹叶厚朴群体遗传学研究

目的:对厚朴与凹叶厚朴的群体遗传学进行研究,为中药厚朴的质量控制提供分子生药学方面的依据。方法:对厚朴与凹叶厚朴15个居群应用2个叶绿体基因间序列psbA-trnH和trnL-trnF进行PCR扩增并测序,计算厚朴与凹叶厚朴单倍型频率,用程序HaploNst分析遗传多样性和遗传结构,应用TCS version 1.13软件构建单倍型网状进化树。结果:厚朴与凹叶厚朴均无特有单倍型存在,但单倍型频率存在显著差异,已开始出现遗传分化的趋势,NST略大于GST。结论:厚朴与凹叶厚朴在遗传上已出现遗传分化的趋势,但尚未完全分化成彼此独立的单系。     

Experimental study on anti-inflammatory activity of a TCM recipe consisting of the supercritical fluid CO2 extract of Chrysanthemum indicum, Patchouli Oil and Zedoary Turmeric Oil in vivo

Ethnopharmacological relevance

Chrysanthemum indicum (Compositae) Linné, Pogostemon cablin (Blanco) Benth and Curcuma wenyujin (Zingiberaceae) Y. H. Chen et C. Ling are three of the extensively used herbal remedies among traditional Chinese medicines for the purpose of anti-inflammation. A traditional Chinese medicine (TCM) recipe named CPZ consisting extracts of the above three herbs, has shown noteworthy anti-influenza activity, which is closely related to its anti-inflammatory feature.

Aim of this study

To investigated the anti-inflammtory activity of CPZ in vivo for a further exploration of the recipe's anti-inflammatory properties.

Materials and methods

The anti-inflammatory property of CPZ on acute inflammation was evaluated by inflammatory models of dimethylbenzene (DMB)-induced ear vasodilatation and acetic acid-induced capillary permeability enhancement in mice, as well as the carrageenan-induced paw edema rat model, in which inflammation-related cytokine including prostaglandin E₂ (PGE₂), interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), and nitric oxide (NO) in the edematous paw tissue were determined by enzyme linked immunosorbent assay (ELISA). Moreover, effect of CPZ on chronic inflammation was observed through granuloma formation in rats subjected to cotton pellet implantation.

Results

CPZ (340, 170, and 85 mg/kg for mice, p.o.) not only decreased the DMB-induced ear vasodilatation but also attenuated capillary permeability under acetic acid challenge in mice. And the significant inhibition on carrageenan-induced paw edema was observed. Further more, the ELISA results showed that CPZ (170, 85, and 42.5 mg/kg for rats, p.o.) could up-regulate the level of IL-1β in the edema paw tissue of rats significantly while down-regulate that of PGE₂, but no apparent effect on TNF-α or NO was observed in the test. Besides, CPZ had a certain degree of restraining effect on the cotton pellet-induced granuloma formation in rats and the highest dose of 170 mg/kg even showed a significant suppression on it.

Conclusion

The above results indicated that CPZ possessed a potent anti-inflammatory activity, which is indicated to be closely associated with its regulation on IL-1β and PGE₂ thereby mediating the inflammatory response acting at an appropriate level.     

Regulation effects on abnormal glucose and lipid metabolism of TZQ-F,a new kind of Traditional Chinese Medicine

Aim of the study

Based on the recipe of the traditional anti-diabetic formula TZQ, we developed TZQ-F, a new formula including 8 fractions isolated from Red Paeony root, Mulberry leaf, Lotus leaf, Danshen root and Hawthorn leaf with a good quality assurance. The study was aimed at fraction preparation and effects of the fractions on abnormal glucose and lipid metabolism.

Materials and methods

The active fractions were obtained by macroporous resin, ion-exchange resin and polyamide resin column chromatographies. HPLC analyses were used for quality control. In vitro mechanism study included DPPH radical scavenging, AGEs formation inhibition, α-glucosidase inhibition and lipase inhibition, and rats on high-fat diet were used for in vivo study.

Results

In vitro mechanism study showed that among the 8 fractions, three of them had inhibition effects on intestinal disaccharase, three with inhibition effects on lipase, and five with effects of free radical scavenging. In vivo study showed that after 4 weeks of treatment, TZQ-F significantly decreased the levels of serum total cholesterol, TG, glucose, LDL-C and HDL-C in rats on high-fat diet. Consistent with the in vitro and in vivo results, histology study demonstrated that TZQ-F alleviated hepatic steatosis induced by high-fat diet.

Conclusions

TZQ-F possesses the potential regulation effects on abnormal glucose and lipid metabolism.     

Antifungal activity of Brazilian medicinal plants involved in popular treatment of mycoses

A survey of medicinal plants used to treat common mycoses was done in the Curituba district, Sergipe State, Brazil. One hundred inhabitants were interviewed by health agents and traditional healers. Four different plants were the most cited (more than 50% of the citations): Ziziphus joazeiro, Caesalpinia pyramidalis, Bumelia sartorum and Hymenea courbaril. The aqueous extracts obtained following traditional methods and using different parts of these plants, were submitted to drop agar diffusion tests for primary antimicrobial screening. Only the water infusion extract of Ziziphus joazeiro and Caesalpinea pyramidalis presented a significant antifungal activity against Trichophyton rubrum, Candida guilliermondii, Candida albicans, Cryptococcus neoformans and Fonsecaea pedrosoi, when compared to the antifungal agent amphotericin B. The minimal inhibitory concentration (MIC) of the bioactive extracts was evaluated by the microdilution method. Best activity with a MIC of 6.5 microg/ml for both extracts was observed against Trichophyton rubrum and Candida guilliermondii. Ziziphus joazeiro and Caesalpinea pyramidalis extracts presented also low acute toxicity in murine models. The present study validates the folk use of these plant extracts and indicates that they can be effective potential candidates for the development of new strategies to treat fungal infections.     

常用藏药“蒂达”(藏茵陈)基原物种药用合理性及资源利用价值评价

目的:对“蒂达”各品种不同基原植物药用合理性及其资源利用价值作出评价.方法:采用HPLC指纹图谱共有特征峰、结合SPSS聚类分析方法,评价“蒂达”不同品种基原植物的成分组成相似性.结果:“蒂达”不同品种涉及的来源有龙胆科獐牙菜属、花锚属、扁蕾属及肋柱花属共15种1变种33个样品,指纹图谱全谱相似度较差;以10个共有峰成分的相对面积聚类,其基原植物可分别聚为4个组;上述4个属的属间成分组成差异较大;其中獐牙菜属不同种间成分组成变化较大,而其他各属种间成分组成相似度较高.结论:上述龙胆科4属植物均含有具有保肝利胆生物活性的环烯醚萜类、(山)酮类及三萜类成分,藏医学将其归为“蒂达”一类药材使用具有一定的物质基础;鉴于“蒂达”类药材不同基原各品种间在成分组成上差异较大,分别制定各品种的HPLC指纹图谱,是鉴别和控制各品种质量的有效手段,可有效控制各基原品种质量.     

乌拉尔甘草HMGR基因cDNA的克隆与序列分析

目的:对乌拉尔甘草3.羟基-3-甲基戊二酰辅酶A还原酶(3-hydroxy-3methylglutary CoA reductase,HMGR)的cDNA克隆并进行序列分析.方法:根据NCBI数据库中的豆科其他物种HMGR的cDNA保守区设计引物,利用同源扩增和cDNA末端快速扩增技术从甘草根中获得目的基因;利用BLAST进行序列比对,ORF Finder寻找开发阅读框,Prosite分析蛋白质的基本结构域,Clustal x比对已有HMGR的氨基酸序列,并构建进化树.结果:得到1个全长为1 842 bp的HMGR的cDNA序列,含有1 722 bp的开放阅读框(open reading frame,ORF),编码573个氨基酸,具有HMGR家族的特异序列,推测的氨基酸序列与豌豆、蒺藜苜蓿的氨基酸序列一致性分别为84%,76%.结论:对甘草HMGR基因的cDNA进行了克隆,为进一步研究3-羟基-3-甲基戊二酰辅酶A在甘草酸生物合成途径中的作用提供了理论依据.