紫红獐牙菜中紫药甙的结构

紫红獐牙菜(Swertia punicea Hemsl)系龙胆科(Gentianaceae)獐牙菜属植物。分布于去南、四川、贵州、湖北、湖南等省。民间全草入药,具清肝利胆,除湿清热功效,治急性黄疸型肝炎,胆囊炎等。国内外至今尚未见有关其化学成分的报道。我们从紫红獐牙菜乙醇提取物中分得五个(口山)酮类成分,经光谱分析及化学反应,鉴定为芒果甙(mangiferin,1,3,6,7-四羟基(口山)酮-2-C-β-D-吡喃葡萄糖甙,Ⅰ),bellidifodin(1,5,8-三羟基-3-     

大籽獐牙菜中大籽獐牙菜甙的结构

本文报道从大籽獐牙菜Swertia macrosperma C.B.Clark的全草中分离得到的另外四个化合物Ⅰ～Ⅳ。经光谱及化学方法鉴定,化合物Ⅰ是一种咖啡酸双糖酯类化合物,其结构为反式咖啡酸-1-O-芦丁糖酯(trans caffeic acid-1-O-rutinose ester),系首次从天然界得到的一种新化合物,命名为大籽獐牙菜甙(swertiamacroside);化合物Ⅱ～Ⅳ为已知的(口山)酮衍生物,分别鉴定为芒果甙(mangiferin,Ⅱ),bellidifodin(Ⅲ)及bellidifodin-8-O-β-D-glucopyranoside(Ⅳ)。     

超临界CO2萃取川东獐牙菜总员(口山)酮的工艺优化

目的 优化超临界CO2萃取川东獐牙菜总(口山)酮的工艺.方法 以去甲基雏菊叶龙胆酮和总(口山)酮含量为指标,用正交试验法优选.结果 川东獐牙菜总山酮萃取的最佳工艺条件为:萃取温度40 ℃,萃取压力30 MPa,萃取时间80 min,夹带剂为95%乙醇.结论 采用超临界CO2萃取法提取脂溶性成分具有速度快、效率高和无污染的特点,工艺简便易行.     

狭叶獐牙菜的两个新环烯醚单萜甙

本文报道狭叶獐牙菜(Swertia angustifolia)中两个新的环烯醚单萜甙的结构。分别命名为狭叶獐牙菜苦甙(angustiamarin,Ⅰ)和狭叶獐牙菜甙(angustioside,Ⅱ),此外还鉴定了獐牙菜甙(sweroside,Ⅲ),獐牙菜苦甙(swertiamarin,Ⅳ)和表优士特莫甙(epi-eustomoside,Ⅴ)。     

川东獐牙菜总酮指纹图谱研究

目的建立川东獐牙莱总口山酮指纹图谱测定方法。方法采用反相高效液相色谱法测定川东獐牙菜总口山酮指纹图谱，色谱柱为Hypersil C18柱（150mm×4．6mm，5μm），流动相为甲醇-水（54：46），流速1．3mL／min，检测波长338nm，柱温20℃。结果建立了川东獐牙菜总咄酮样品指纹图谱，确立了11个特征共有峰，10批样品的相似度均在0．9以上。结论所用方法简便、快速、重现性好，可作为川东獐牙菜总口山酮的一项质量控制指标。     

11种獐牙菜及近缘植物中有效成分的高效液相色谱测定

建立了獐牙菜中3种苦味甙,即獐牙菜苦甙(swertiamarin)、獐牙菜甙(sweroside)、龙胆苦甙(gentiopicroside)及一种　酮甙──獐牙菜　酮甙(swertianolin)的高效液相色谱定量分析方法(μ-BondpakC₁₈柱,水—甲醇—异丙醇—四氢呋喃=65:30:5:1作流动相);对11种獐牙菜及近缘植物椭圆叶花锚、坚龙胆进行了含量测定,并对他们之间的异同进行了比较。     

彝药布高兹尔化学成分的分离和结构鉴定（Ⅱ）

本文继续报道Veratrills baillonii Franch根中分离得到的另外两个(口山)酮成分。现经光谱、理化常数鉴定,已确定为:1-羟基-2,3,5,6-四甲氧基(口山)酮(Ⅶ)及1-羟基-3,4,6-三甲氧基-7-0-β-D-吡喃葡萄糖基(口山)酮(Ⅷ)。此外,尚自乙醇提取液中分离并检出3个环烯醚萜类化合物,经聚酰胺薄膜层析,并与龙胆苦甙、獐牙菜苦甙等标准品对照,其中之一已初步确定为龙胆苦甙。     

云南民族药斜茎獐牙菜的实验研究(摘要)

斜茎獐牙菜(Swertia Patens Burk)为龙胆科獐牙菜属植物,又名金沙青叶胆、小儿腹痛草,彝药名“落孺疴”其意为苦得很,我省彝族人民用其全草治疗消化不良、腹痛、牙痛、沿用历史已久。我们对该植物进行了实验研究,从其全草中分离得到齐墩果酸及獐牙菜苦甙。本所实验证明:齐墩果酸对大鼠由四氯化碳引起的肝损伤有保护作用;獐牙菜苦甙有明显的解除平滑肌痉挛作用。近三年来,我所对斜茎獐牙菜的植物学、生药学、有效成分的提取、分离、结构鉴定、药理、毒理等方面进行了研究,其中主要有效成分——獐牙菜苦甙作为解止痛新药已于1983年12月     

紫红獐牙菜中紫药苦甙的结构

继续报道从紫红獐牙菜Sivertia punicea Hemsl,全草中分得的另八个化合物(Ⅰ～Ⅷ)的结构,经光谱解析,I的结构推定为6′-O-β-D-吡喃葡萄糖基獐牙菜甙(6′-O-β-D-glucopyranosylsweroside,Ⅰ),为一新的裂环环烯醚萜甙类化合物,命名为紫药苦甙(swertiapunimarin),Ⅱ～Ⅷ的结构分别鉴定为獐牙菜甙(sweroside,Ⅱ)、獐牙菜苦甙(swertiamarin,Ⅲ)、齐墩果酸(oleanolic acid,Ⅳ)、胡萝卜甙(daucosterol.Ⅴ)、β-谷甾醇(B-sitosterol,Ⅵ)、2,3-二羟基-1,4-苯二甲酸(2,3-dihydroxy-1,4-benzodicarboxylic acid,Ⅶ)及methylswertianin.以上均首次从该植物中得到。     

乌棒子甙甲和甙乙的分离鉴定

从远志科植物乌棒子(Polygala caudata Rehd et Wils)的根皮和茎皮中分得四种(口山)酮类成分和一种甾醇甙,分别鉴定为优(口山)酮(Ⅰ),豆甾醇葡萄糖甙(Ⅱ),乌棒子甙甲(wubangziside A,Ⅲ),乌棒子甙乙(wubangziside B,Ⅳ)和芒果甙(Ⅴ)。本文报道两种新(口山)酮甙乌棒子甙甲和甙乙的结构测定以及三种已知化合物的鉴定工作。     

The effect of gamma-hexachlorcyclohexane on rat liver lysosomes.

(1). An intraperitoneal injection of gamma-HCH (40 mg/kg, ld₅₀) was shown to induce a significant release of three lysosomal enzymes—acid phosphatase, β-glucosidase and cathepsin D—in rat livers already 1 hr after administration of the agent. From 1 hr up to 24 hr of the observation period the release of selected lysosomal hydrolases consistently increased. In contrast to the biochemical findings, the morphological changes including, hepatic necrosis and fatty infiltration, were established only 24 hr after gamma-HCH treatment. (2). The in vitro studies on the latency of two lysosomal enzymes—acid phosphatase and β-glucosidase—in the rat liver lysosome-rich suspension treated with gamma-HCH, showed that the concentrations of 10^?5 M, 10^?4 M and 10^?3 M significantly decreased latency of both enzymes. However, acid phosphatase and β-glucosidase, exhibited differential responses to the in vitro effect of gamma-HCH, which might be due to the differential affinities of these enzymes for the lysosomal matrix. The above mentioned concentrations of gamma-HCH did not significantly change the activities of acid phosphatase, β-glucosidase and cathepsin D in vitro. (3). No significant alterations were observed in the total activities of enzymes studied after in vivo and in vitro administered gamma-HCH. (4). The present study suggests that gamma-HCH exerts its effect on rat liver lysosomes by modifying the structural properties of the lysosomal membrane.     

Picroliv and its Components Kutkoside and Picroside I Protect Liver Against Galactosamine-Induced Damage in Rats

Abstract: D-Galactosamine (800 mg/kg, intraperitoneally) caused significant decrease in the activities of 5′-nucleotidase, glucose-6-phosphatase and cytochrome P450 and increase in activities of γ-glutamyl transpeptidase, succinate dehydrogenase, acid phosphatase and acid ribonuclease in liver after 24 hr. The levels of RNA, protein and glycogen decreased while total lipids, phospholipids, cholesterol and lipid peroxides increased. It also increased the serum levels of transaminases, alkaline phosphatase and bilirubin while protein concentration decreased significantly. Oral administration of Picroliv (12 mg/kg/day for 7 days), a standardised iridoid glycoside fraction of Picrorhiza kurroa, significantly prevented the biochemical changes in liver and serum of galactosamine-toxicated rats. Kutkoside (12 mg/kg/day for 7 days) also protected against changes in most of the hepatic and serum constituents studied. Another iridoid glycoside from Picroliv, Picroside I, at the same dose level could only prevent toxicant-induced changes in acid phosphatase, phospholipids and lipid peroxides in liver and alkaline phosphatase in serum. Mixture of Picroside I and Kutkoside in the ratio of 1:1.5 at 12 mg/kg dose elicited lesser response than Picroliv.     

Hepatoprotective activity of Stereospermum suaveolens against CCl4-induced liver damage in albino rats

The present study aims to evaluate the hepatoprotective activity of Stereospermum suaveolens DC (Bignoniaceae). Hepatoprotective activity is studied by carbon tetrachloride (CCl₄)-induced liver damage in albino rats. The degree of protection in this activity has been measured by using biochemical parameters such as serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT), alkaline phosphatase (ALP), total bilirubin, LDL-cholesterol and SOD, CAT, GSH, total thiols, NO, and lipid peroxidation in liver tissue homogenate. The results suggest that the methanol stem bark extract of Stereospermum suaveolens at the doses 125, 250, and 500?mg/kg and reference standard Liv-52 treated group produced significant (p <0.001) hepatoprotection against CCl₄-induced liver damage by decreasing the activities of serum enzymes, bilirubin and lipid peroxidation. The extract significantly (p <0.001) increased levels of SOD, CAT, GSH and total thiols, as compared to control group. Histopathological studies further substantiate the protective effect of the extract. It was concluded that methanol stem bark extract of Stereospermum suaveolens showed effective hepatoprotective activity.     

Antioxidant Defense System Induced by a Methanol Extract of Caesalpinia bonducella. in Rat Liver

ABSTRACT

The antioxidant defense system dramatically controls hepatocellular carcinoma induced by N.-nitrosodiethylamine (NDEA). In order to assess the anticarcinogenic activity of a methanol extract of Caesalpinia bonducella. (MECB) leaves containing flavonoids and triterpenoids, the antioxidant defense system has been evaluated. The effect of MECB on lipid peroxidation end-product malondialdehyde (MDA), enzymatic antioxidants such as superoxide dismutase (SOD) and catalase (CAT), and nonenzymatic antioxidants glutathione (GSH), vitamin E, and vitamin C levels were analyzed in the liver of control and experimental animals. Serum was also analyzed for transaminase activity (SGOT and SGPT), alkaline phosphatase (SALP), bilirubin, total protein, and uric acid. Depletion of all these antioxidants was recorded in cancer conditions. These deleterious effects are controlled by the administration of MECB. After drug administration, there was a marked increase in antioxidant levels and a dramatic decrease in lipid peroxidation levels. MECB also produced a protective effect by decreasing the activity of serum enzymes, bilirubin, and increased the protein and uric acid levels. From the above results, it can be concluded that the observed anticarcinogenic properties of MECB may also be explained by its strong antioxidant capacity and capability to induce an in vivo. antioxidant system.     

Antihepatotoxic activity of debelalactone,a new oxirano-furanocoumarin from Phyllanthus debilis

The whole plant of Phyllanthus debilis (Euphorbiacae) afforded a new oxirano-furanocoumarin, characterized as 5-hydroxy-7-methoxy-furanocoumarin-9(14)-cyclohex-12(13)-oxirano-11-one (1), named as debelalactone. Debelalactone exhibited a significant antihepatotoxic activity by reducing the elevated levels of serum enzymes such as serum glutamate oxaloacetate transaminase (SGOT) by 59.14%, serum glutamate pyruvate oxaloacetate transaminase (SGPT) by 61.84%, and alkaline phosphatase (ALP) by 85.93%; while the total protein (TP) levels were increased by 110.35%, when compared with standard drug silymarin that have decreased SGOT by 77.03%, SGPT by 69.67%, ALP by 93.18%, and increased TP levels by 100.48%, respectively, against CCl₄-induced toxicity in Wistar rats. These biochemical observations were also supplemented by histopathological examinations of the liver sections.     

Effect of Mangiferin,a Naturally Occurring Glucosylxanthone,on Reproductive Function of Rats

Female albino rats, treated with mangiferin at daily doses of 5 mg/100 g ip for 3 days during mid-gestation, showed complete fetal resorption. Administration of a mangiferin-Cu²⁺ (1:1) complex, along with mangiferin, attenuated the effect of mangiferin and restored the completion of gestation in 60% of the rats. The mother rats that completed gestation successfully did not show any post-natal abnormality, and the litters born were also normal. Mangiferin treatment of non-gestating female rats caused little or no changes in their organ weights. However, changes in the protein and protein-DNA ratios of several organs were statistically significant. Mangiferin also modified the ascorbic acid retention capacity of adrenal glands of male rats in vitro. These findings are appraised in view of mangiferin as a potential antifertility agent.     

Rifampicin induced hepatotoxicity in rats: Protective effect of picrolive effect of picroliv

Rifampicin, an anti-tubercular drug, at 100 mg/kg (122 μmol) body weight (daily single ip injection for 6 days) caused changes in most of the biochemical parameters of the liver and serum in rats, 24 h after the last injection. These included significant increase in the activities of hepatic γ-glutamyl transpeptidase, acid ribonuclease, acid phosphatase and decrease in the activity of succinate dehydrogenase. The levels of RNA, total proteins, bilirubin, total lipids, phospholipids, cholesterol, lipid peroxides in liver and bilirubin in serum increased while hepatic glycogen and serum proteins decreased. At a lower dose (50 mg/kg; 61 μmol/kg) the changes were less as compared to 100 mg/kg dose. When Picroliv (12 mg/kg body weight), a standardized iridoid glycoside mixture of Picrorhiza kurroa was administered simultaneously with rifampicin, most of the biochemical changes in liver and serum were prevented. These results indicate protective effect of Picroliv against rifampicin-induced hepatotoxicity in rats. © 1994 Wiley-Liss, Inc.     

Mangiferin and its aglycone,norathyriol, improve glucose metabolism by activation of AMP-activated protein kinase

Context: Mangiferin has been reported to possess antidiabetic activities. Norathyriol, a xanthone aglycone, has the same structure as mangiferin, except for a C-glucosyl bond. To our best knowledge, no study has been conducted to determine and compare those two compounds on glucose consumption in vitro.

Objective: In this study, the effects of norathyriol and mangiferin on glucose consumption in normal and insulin resistance (IR) L6 myotubes were evaluated. Simultaneously, the potential mechanism of this effect was also investigated.

Materials and methods: Normal or IR L6 myotubes were incubated with norathyriol (2.5?～?10?μM, 0.625?～?2.5?μM), mangiferin (10?～?40?μM, 2.5?～?10?μM) or rosiglitazone (20?μM) and/or 0.05?nM insulin for 24?h, respectively. The glucose consumption was assessed using the glucose oxidase method. Immunoblotting was performed to detect protein kinase B (PKB/Akt) and AMP-activated protein kinase (AMPK) phosphorylation in L6 myotubes cells.

Results: Norathyriol and mangiferin treatment alone increased the glucose consumption 61.9 and 56.3%, respectively, in L6 myotubes and made additional increasing with 0.05?nM insulin. In IR L6 myotubes, norathyriol treatment made increasing with or without insulin, mangiferin treatment also made increasing but only when co-treated with insulin. Immunoblotting results showed that norathyriol and mangiferin produced an increase of 1.9?- and 1.8-fold in the phosphorylation levels of the AMPK, but not in Akt.

Discussion and conclusion: Our findings suggest that norathyriol and mangiferin could improve the glucose utilization and insulin sensitivity by up-regulation of the phosphorylation of AMPK. Norathyriol may be considered as an active metabolite responsible for the antidiabetic activity of mangiferin.     

Hypolipidemic and hypoglycemic activities of a oleanolic acid derivative from <Emphasis Type="Italic">Malva parviflora</Emphasis> on streptozotocin-induced diabetic mice

One new oleanolic acid derivative, 2α,3β,23α,29α tetrahydroxyolean-12(13)-en-28-oic acid (1) was isolated from the aerial parts of Malva parviflora. Their structure was characterized by spectroscopic methods. The hypolipidemic and hypoglycemic activities of 1 was analyzed in in streptozotocin (STZ)-nicotinamide-induced type 2 diabetes in mice (MD) and type 1 diabetes in streptozotocin-induced diabetic mice (SD). Triterpene was administered orally at doses of 20 mg/kg for 4 weeks. Organ weight, body weight, glucose, fasting insulin, cholesterol-related lipid profile parameters, glutamate oxaloacetate transaminase (SGOT), glutamate pyruvate transaminase (SGPT), serum alkaline phosphatase (SALP), glucokinase, hexokinase, glucose-6-phosphatase activities and glycogen in liver were measured after 4 weeks of treatment. The results indicated that 1 regulate glucose metabolism, lipid profile, lipid peroxidation, increased body weight, glucokinase and hexokinase activities inhibited triglycerides, total cholesterol, low density lipoproteins level, SGOT, SGPT, SALP, glycogen in liver and glucose-6-phosphatase. In addition, improvement of insulin resistance and protective effect for pancreatic β-cells, also 1 may changes the expression of pro-inflammatory cytokine (IL-6 and TNF-α levels) and enzymes (PAL2, COX-2, and LOX). The results suggest that 1 has hypolipidemic and hypoglycemic, anti-inflammatory, activities, improve insulin resistance and hepatic enzymes in streptozotocin-induced diabetic mice.     

Biochemical Changes Induced in Liver and Serum of Aflatoxin B1‐Treated Male Wistar Rats: Preventive Effect of Picroliv

Abstract: Administration of aflatoxin B₁ to rats (2 mg/kg intraperitoneally) caused significant increase in the activities of γ‐glutamyl transpeptidase, 5′‐nucleotidase, acid phosphatase, acid ribonuclease as well as content of lipid peroxides in liver after six weeks. However, the activities of succinate dehydrogenase, glucose‐6‐phosphatase, catalase, superoxide dismutase, glutathione‐S‐transferase, glutathione peroxidase and glutathione reductase in liver were decreased. The levels of glycogen and reduced glutathione were also decreased. There were significant elevations in the levels of serum transaminases, phosphatases (acid and alkaline), dehydrogenases (sorbitol, lactate and glutamate) and bilirubin following aflatoxin B₁ administration. Picroliv (25 mg/kg/day orally for six weeks), an iridoid glycoside isolated from the roots and rhizomes of Picrorhiza kurroa, significantly prevented the biochemical changes induced by aflatoxin B₁.