番石榴果实中三萜类成分研究

目的:研究番石榴果实的化学成分.方法:采用各种色谱技术分离,波谱法进行结构鉴定.结果:从番石榴果实中分离得到9个乌苏烷型三萜类化合物:乌苏酸(1),1β,3β-二羟基乌苏烷-12烯-28-酸(2),2α,3β-二羟基-12-烯-28-乌苏酸(3),3β,19α-二羟基-12-烯-28-乌苏酸(4),19α-羟基-12-烯-28-乌苏酸-3-O-α-L-阿拉伯吡喃糖(5),3β,23-二羟基-12-烯-28-乌苏酸(6),3β,19α,23-三羟基-12-烯-28-乌苏酸(7),2α,3β,19α,23-四羟基-12-烯-28-乌苏酸(8),3α,19α,23,24-四羟基-12-烯-28乌苏酸(9).结论:化合物2,5-9为首次在该植物中分离得到.     

蒲公英的现代应用

蒲公英既是一种临床常用中药,又是人们餐桌上的一种常见的食物,具有药食两用的特点,具有清热解毒,消肿散结,利湿通淋,清肝明目等功效。蒲公英内含有丰富的蛋白质、碳水化合物、氨基酸、钙铁磷锌锰等60余种微量元素,存在种类繁多的化学成分,活性成分主要为黄酮类、三萜类化合物、多糖类化合物、甾醇类化合物等,临床广泛应用于急性乳腺炎、胃炎、脾虚湿热型脂溢性脱发、扁桃体炎、胆囊炎、肝炎、肠炎等疾病的治疗。但是,对于其药理作用和作用机理还未进行系统的总结分析,临床选用困难较多。关于蒲公英毒性的研究报道较少,需要进一步深入研究;蒲公英与其他中药配伍后的化学成分变化研究欠缺,不能有效说明其机理,更好地服务临床应用;其临床疗效评价量化指标需要进一步提高;其单体的提纯也是今后努力的方向。     

Chemical Constituents of Ganoderma resinaceum

Abstract: Objective To study the chemical constituents of Ganoderma resinaceum. Methods Chemical constituents were isolated and purified by silica gel column, Sephadex LH-20, and ODS column chromatography. The structures were identified by means of physicochemical and spectral data. Results From the CHCl3 part of the fruiting bodies of this material, eight compounds were isolated. Their structures were determined to be ergosterol (1), β-sitosterol (2), ganoderic acid E (3), ganoderic acid G (4), ganoderic acid C2 (5), ganoderic acid B (6), ganoderic acid A (7), and lucidenic acid A (8). Conclusion All the compounds were obtained from this fungus for the first time.     

三萜类化合物降血糖活性及其作用机制研究进展

三萜类化合物在预防糖尿病和降血糖活性方面的研究取得了较大进展。研究发现,三萜类化合物能够通过多种途径降低血糖,包括促进胰岛素分泌,增强胰岛素敏感性,抑制蛋白酪氨酸磷酸酶1B(PTP1B),激活腺苷酸活化蛋白激酶(AMPK)促进糖摄取,减少肝脏糖原分解与糖异生,抑制α-糖苷酶、醛糖还原酶(AR)和二肽基肽酶-4(DPP-4)的活性等。本文对三萜类化合物的降血糖活性及其作用机制进行了综述,为该类化合物降血糖活性的深入研究与开发提供参考。     

桦褐孔菌三萜类化学成分研究

目的研究桦褐孔菌Inonotus obliquus子实体的化学成分。方法采用硅胶、MCI、Sephadex LH-20凝胶等柱色谱方法进行分离纯化,根据理化性质和波谱分析对化合物结构进行鉴定。结果从桦褐孔菌子实体95%乙醇提取物中分离得到13个三萜化合物和2个甾醇化合物,分别鉴定为3-羊毛甾-8,24-二烯-21-醛(1)、羊毛甾醇(2)、3β-羟基-羊毛甾-8,24-二烯-21-醛(3)、白桦脂醇(4)、桦褐孔菌醇(5)、栓菌酸(6)、3β,21-二羟基-羊毛甾-8,24-二烯(7)、齐墩果酸(8)、乌苏酸(9)、白桦脂酸(10)、桦褐孔菌素A(11)、桦褐孔菌萜D(12)、3β-乙酰氧基-11α,12α-环氧-齐墩果烷-28,13β-内酯(13)、麦角甾醇(14)、麦角甾烷-4,6,8,22-四烯-3-酮(15)。结论化合物1为1个新的三萜化合物,命名为桦褐孔菌素D;化合物9、13、15为首次从桦褐孔菌子实体中分离得到。     

人参茎叶总皂苷酸水解产物化学成分研究

目的 研究人参Panax ginseng茎叶总皂苷酸水解产物的化学成分。方法 采用硅胶柱色谱及半制备高效液相色谱等方法进行分离、纯化,通过NMR、MS等进行结构鉴定。结果 从人参茎叶总皂苷的酸水解产物中分离鉴定了34个化合物,分别为3β-乙酰氧基-12β-羟基-20(R),25-环氧达玛烷(1)、3β,6α-二乙酰氧基-12β-羟基-20(R),25-环氧达玛烷(2)、3β-乙酰氧基-6α,12β-二羟基-20(R),25-环氧达玛烷(3)、20(R)-人参二醇(4)、异去氢原人参三醇(5)、3-酮基-6α,12β-二羟基-20(R),25-环氧达玛烷(6)、达玛-(E)-20(22)-烯-3β,12β,25-三醇(7)、6α-乙酰氧基-3β,12β-二羟基-20(R),25-环氧达玛烷(8)、20(S)-原人参二醇(9)、20(R)-原人参二醇(10)、20(S)-25-乙氧基-达玛烷-3β,12β,20-三醇(11)、20(R)-人参三醇(12)、达玛-(E)-20(22),24-二烯-3β,6α,12β-三醇(13)、27-去甲基-(E,E)-20(22),23-二烯-3β,12β-二羟基达玛-25-酮(14)、3β,12β-二羟基-22,23,24,25,26,27-六去甲达玛烷-20-酮(15)、3β-乙酰氧基-6α,12β,25-三羟基-(20S,24R)-环氧达玛烷(16)、20(S)-25-乙氧基-达玛烷-3β,6α,12β,20-四醇(17)、达玛-(E)-20(22)-烯-3β,6α,12β,25-四醇(18)、达玛-(Z)-20(22)-烯-3β,6α,12β,25-四醇(19)、20(S)-达玛烷-3β,12β,20,25-四醇(20)、20(R)-达玛烷-3β,12β,20,25-四醇(21)、20(S)-原人参三醇(22)、20(R)-原人参三醇(23)、(20S,24S)-达玛烷-20,24-环氧-3β,6α,12β,25-四醇(24)、(20S,24R)-达玛烷-20,24-环氧-3β,6α,12β,25-四醇(25)、(20R,24R)-达玛烷-20,24-环氧-3β,6α,12β,25-四醇(26)、3β,6α,12β-三羟基-22,23.24,25,26,27-六去甲达玛烷-20-酮(27)、12β-羟基-20(R),25-环氧达玛烷-3β-O-β-D-吡喃葡萄糖苷(28)、20(S)-达玛烷-3β,6α,12β,20,25-五醇(29)、20(R)-达玛烷-3β,6α,12β,20,25-五醇(30)、20(R)-达玛烷-3β,6α,12β-三羟基-20,25-环氧-6-O-β-D-吡喃葡萄糖苷(31)、拟人参皂苷Rh₂(32)、20(S)-人参皂苷Rh₁(33)、20(R)-人参皂苷Rh₁(34)。结论 化合物1～3、6、8、11、17、24～26和32为首次从人参茎叶总皂苷酸水解产物中分离得到的人参三萜类化合物;首次报道化合物1、16和19的碳谱数据;32是人癌细胞增殖的抑制剂。     

Distinct Responses of Cytotoxic Ganoderma lucidum Triterpenoids in Human Carcinoma Cells

The medicinal mushroom Ganoderma lucidum is well recognized for its effective cancer‐preventative and therapeutic properties, while specific components responsible for these anticancer effects are not well studied. Six triterpenoids that are ganolucidic acid E, lucidumol A, ganodermanontriol, 7‐oxo‐ganoderic acid Z, 15‐hydroxy‐ganoderic acid S, and ganoderic acid DM were isolated and identified from an extract of the mushroom. All compounds reduced cell growth in three human carcinoma cells (Caco‐2, HepG2, and HeLa cells) dose dependently with LC50s from 20.87 to 84.36 μM. Moreover, the six compounds induced apoptosis in HeLa cells with a maximum increase (22%) of sub‐G1 accumulations and 43.03% apoptotic cells in terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay (15‐hydroxy‐ganoderic acid S treatment). Apoptosis was further confirmed by annexin‐V staining. Four of the compounds also caused apoptosis in Caco‐2 cells with maximum 9.5% increase of sub‐G1 accumulations (7‐oxo‐ganoderic acid Z treatment) and maximum 29.84% apoptotic cells in TUNEL assay (ganoderic acid DM treatment). Contrarily, none of the compounds induced apoptosis in HepG2 cells. The different responses of the three cell lines following these treatments indicated that the bioactive properties of these compounds may vary from cells of different sites of origin and are likely acting under diverse regulatory mechanisms. Copyright © 2015 John Wiley & Sons, Ltd.     

秦岭猪苓活性成分提取工艺与鉴定研究

  目的：研究秦岭猪苓三萜化合物的提取技术,并其成分进行鉴定研究  方法：以香草醛冰乙酸高氯酸为显色系统,采用紫外分光光度法测定猪苓总三萜化合物的含量;以乙醇为溶剂,采用溶剂法对三萜化合物进行提取,通过单因素试验和正交试验确定最佳提取工艺;用理化常数和波谱数据对其进行鉴定  结果：最佳提取工艺为6倍量无水乙醇,回流提取3次,每次2 h  结论：该提取工艺操作简单可行,可为猪苓药材的研究提供科学依据。     

HPLC determination of four triterpenoids in rat urine after oral administration of total triterpenoids from Ganoderma lucidum

A sensitive and simple high-performance liquid chromatography (HPLC) method was applied for the quantitative determination of four major triterpenoids (ganoderic acids C(2), B, K and H) in rat urine after oral administration of total triterpenoids from Ganoderma lucidum. The urine sample was extracted with dichloromethane-ethyl acetate (90:10) after acidification by hydrochloric acid (0.2 mol/ml). Chromatographic separation was achieved on a Zorbax SB-C(18) column (250 mm x 4.6 mm, 5 microm) at 35 degrees C, with a linear gradient of acetonitrile and 0.03% aqueous phosphoric acid (v/v), at a flow rate of 1.2 ml/min. The four triterpenoids and internal standard (hydrocortisone) were detected at a wavelength 252 nm. The within- and between-day assay coefficients of variation for the four triterpenoids in urine were less than 9% and the extraction recovery of this method was higher than 90%. Using this method, the excretion profile of the triterpenoids in rat urine after oral administration of total triterpenoids of G. lucidum was revealed for the first time.     

Antiviral triterpenoids from the medicinal plant Schefflera heptaphylla

Schefflera heptaphylla (L.) Frodin is a principal ingredient of an herbal tea formulation widely used for the treatment of common cold in southern China. An extract of the long leafstalk of the compound leaf of S. heptaphylla exhibited the most potent antiviral activity against respiratory syncytial virus (RSV). Further antiviral-guided fractionation and isolation of the leafstalk extract of S. heptaphylla led to obtain two highly active pure triterpenoids, namely 3alpha-hydroxylup-20(29)-ene-23,28-dioic acid and 3-epi-betulinic acid 3-O-sulfate, together with an inactive saponin, 3alpha-hydroxylup-20(29)-ene-23,28-dioic acid 28-O-alpha-l-rhamnopyranosyl-(1-->4)-O-beta-d-glucopyranosyl-(1-->6)-beta-d-glucopyranoside. An antiviral assay using a cytopathic effect (CPE) reduction method showed that the two triterpenoids possessed broader antiviral activity against respiratory syncytial virus (RSV) with a similar 50% inhibition concentration (IC(50)) value of 6.25 microg/mL, influenza A (H1N1) virus with IC(50) values of 25 and 31.3 microg/mL, Coxsackie B3 (Cox B3) virus with IC(50) values of 12.5 and 20 microg/mL and herpes simplex virus type 1 (HSV-1) with IC(50) values of 18.8 and 25 microg/mL, respectively, whereas the saponin did not have antiviral activity against these four viruses at a concentration of 100 microg/mL.