Protective effects of total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja on STZ-stimulated INS-1 cells through regulating of autophagy and apoptosis

OBJECTIVE To explore the protective effects of total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja on STZ-stimulated INS-1 cells through regulating of autophagy and apoptosis.METHODS INS-1cells were cultured in media containing 3n M STZ and different doses of total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja.The proliferation of cells was examined by MTT assay,ROS content were detected by fluorescence enzyme label.The levels of superoxide dismutase(SOD),glutathione peroxidase(GSH-Px),hydrogen peroxidase(CAT),malondialdehyde(MDA)were also measured by colorimetry.The activities of caspase-3,9 were also observed by Caspase colorimetric assay kit in each group.The expressions of Bcl-2 m RNA and Bax m RNA were detected by Real time PCR,protein expression of LC3-Ⅱand PARP were detected by Western blotting.RESULTS Compared with the control group,total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja could promote the proliferation of INS-1 cells no matter with STZ or not when its concentration lower than 25μg·m L-1;but when its concentration higher than 100μg·m L-(1use individually)or 50μg·m L-1(combined use),total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja might significantly inhibite the growth of the cells whether STZ existed or not.Total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja(6.25,12.5,25μg·m L-1)might inhibit INS-1cell apoptosis,decrease intra-cellular ROS contents,improve the s upernatant liquid SOD,GSH-PX,CAT activities,decrease MDA level,promote INS-1 cell secreting insulin,decrease the protein expressions of autophagy protein LC3Ⅱand apoptosis regulating protein cleaved PARP protein,up-regulate the anti-apoptotic protein Bcl-2 m RNA expression,down-regulate the pro-apoptotic protein Bax m RNA expression and Bcl-2and Bax,reduce the activity of caspase-9 and caspase-3(P<0.05 or P<0.01).CONCLUSION Total triterpenoids extracts from Cyclocarya paliurus(Batal.)Iljinskaja has good protective effect on STZ-stimulated INS-1cells.It can inhibit STZ injured INS-1 cells to overproduce ROS production,enhance endogenous antioxidant enzymes(GSH-Px,SOD,CAT activities),reduce the expression of autophagy protein LC3Ⅱand apoptosisregulating protein cleaved PARP,up-reglute the antiapoptosis protein Bcl-2 expression,down-regulate the pro-apoptotic protein Bax expression,decrease the caspase-9 and caspase-3 activities,and improve the INS-1cell survival rate,and then play a protective effect on damaged INS-1 cells.

Optimization of Extraction Process and Determination of Total Triterpenoids from Semen Trichosanthis by Response Surface Methodology

[Objectives] To optimize the extraction process and determine the total triterpenoids from Semen Trichosanthis.[Methods]The Box-behnken response surface methodology was applied to optimize the extraction conditions of total triterpenoids in Semen Trichosanthis.And the spectrophotometry was used to determine the content of total triterpenoids in Semen Trichosanthis.[Results] The optimal extraction conditions were solid to liquid ratio of 40∶ 1,ultrasonic time of 20 min,and ultrasonic power of 100 W.Under these conditions,the content of total triterpenoids in Semen Trichosanthis was significantly different among the 10 production areas,among which the No.9 production area(Anhui 1) had the highest total triterpenoids content of 45.71 mg/g,while No.7 production area(Shandong) had the lowest total triterpenoids content of 15.22 mg/g.[Conclusions]The Box-behnken response surface methodology is reliable for the extraction of total triterpenoids in Semen Trichosanthis,and the spectrophotometry is proper for determining the content of total triterpenoids in Semen Trichosanthis.There are large differences in the content of total triterpenoids in Semen Trichosanthis produced in different areas.

Immediate-release Mechanism of Dehydrotrametenolic Acid and Dehydroeburicoic Acid in Poriae Cutis Total Triterpenoids Tablets Based on Liquid-solid Compact Technique

[Objectives]To study the immediate-release mechanism of dehydrotrametenolic acid and dehydroeburicoic acid in Poriae Cutis total triterpenoids tablets by liquid-solid compacts technique.[Methods] Taking dehydrotrametenolic acid and dehydroeburicoic acid as indicators,differences in dissolution were compared between liquid-solid compressed tablets and crude drug of total triterpenoids in Poriae Cutis;crude drug,powder of liquid-solid compressed tablets and excipients of liquid-solid compressed tablets were characterized by differential scanning calorimetry( DSC).[Results]Liquid-solid compact technique could significantly improve dissolution rate of dehydrotrametenolic acid and dehydroeburicoic acid. The total dissolution rate of dehydrotrametenolic acid and dehydroeburicoic acid in Poriae Cutis total triterpenoids tablets was 92%,t50( time for 50% total dissolution rate) and t_D( time for 63. 2% total dissolution rate) were 11. 18 min and 22. 71 min; the total dissolution rate of dehydrotrametenolic acid and dehydroeburicoic acid in crude drug of total triterpenoids was 29%,and t50 and t_D were231. 06 min and 359. 23 min. DSC showed that there was no mutual interaction between excipients and total triterpenoids in Poriae Cutis; on the DSC curve for powder of liquid-solid compressed tablets,the absorption peak vanished completely,indicating that the drug exists in the amorphous form in the liquid-solid powder.[Conclusions] Liquid-solid compact technique can increase the dissolution rate of total triterpenoids in Poriae Cutis and allow rapid release of poorly water soluble drugs.

Effects of Different Decolorants on Retention Rate of Total Triterpenes in Fruit and Rattan Stems of Schisandra chinensis(Turcz.) Baill

This study was to investigate the decoloration effects of activated clay, activated carbon, diatomite, Ca group bentonite, kaolin, activated aluminum oxide, magnesium oxide and attapulgite. Ultraviolet-visible spectroscopywas adopted to de- tect the absorbanees of the extracts of Schisandra chinensis fruit and rattan stems, the contents of total triterpenoids in S. chinensis fruit and rattan stems were deter- mined, and the decoloration rate and the retention rate of total triterpenoids of S. chi- nensis fruit and rattan stems were calculated. The results indicated that, attapulgite exhibited the best decoloration effect on the extract of S. chinensis fruit, with a de- coloration rate up to 60.47%, activated carbon exhibited a better decoloration effect on the extract of S. chinensis rattan stems, with a decoloration rate up to 69.24%, and they had relatively higher retention rates of total triterpenoids. In the eight de- colorants, attapulgite showed the best decoloration effect on the extract of S. chi- nensis fruit, and activated carbon exhibited the best decoloration effect on the ex- tract of S. chinensisrattan stems.

Total triterpenes from fruits of Chaenomeles speciosa(Sweet) Nakai protect against indomethacin-induced gastric mucosal injury: involvement of TFF1-mediated EGF/EGFR and apoptotic pathways

OBJECTIVE Gastric ulcers affect people of all ages and half of the world's population,which is being considered as the new"plague of the 21st century".As is well known,gastric mucosa is known as the first guard to protect the stomach from ulcer injury,while the aetiology of gastric ulcer is relative to imbalances between gastric mucosal protective and aggressive factors.Therefore,reducing or eliminating the aggressive factors,returning to the balance of between mucosal protective and aggressive factors,and then restoring the normal functional of gastric mucosal barrier could be crucial for treating the gastric ulcer.The fruits of Chaenomeles speciosa(TCS),also known as"mugua",might be processed into edible and health care derived products,and used as a commonly used traditional medicine in China for thousands of years.In China folk,there is a saying that"apricot one benefit,pear two benefits,mgua hundred benefits",so it has a"hundred-benefit"fruit reputation.Tujia nationality inhabitants in Southwestern China should have rheumatic diseases and peptic ulcers for living in the damp environments and bingeing on spicy and pungent foods.For the exis⁃tence of the fruit derived products of Chaenomeles speciosa as their complementary foods or snacks,the habit makes them rarely suffer from the two kinds of diseases.Enlightened by these,we had investigated the structure-activity rela⁃tionships,screened out CSTT with gastroprotective activity.Our previous studies demonstrated that TCS owned effec⁃tively therapeutic effects on gastric ulcer patients and animals,and further confirmed that TFF1 and apoptotic pathway were closely interrelated with its exerting gastroprotection.However,its underlying molecular mechanisms involved have not been fully elucidated.The current study was to further investigate its protective effect on indomethacin(IND)-damaged RGM-1 cells and rats and its underlying mechanisms through modulating TFF1-mediated EGF/EGFR and apoptotic pathways.METHODS The gastroprotection of TCS was evaluated with IND-induced gastric lesions model in RGM-1 cells and rats.In vitro,the proliferation,migration,mitochondrial viability and apoptosis were assessed,In vivo,ulcer index,ulcer inhibition rate,gastric juice acidity,gastric wall mucus(GWM),histopathology of gastric mucosa were detected.The gastroprotective effects of TCS through the TFF1-mediated EGFR/EGFR and apoptotic pathways were presented and measured by qRT-PCR and Western blotting assays.RESULTS TCS had gastroprotective function,which was related to the amelioration in promoting IND-damaged RGM-1 cell proliferation and migration,hoisting gastric juice acidity and GWM,improving ulcer index and ulcer inhibition rate,attenuating the hemorrhage,edema,epithelial cell loss and inflammatory cell infiltration of gastric mucosa,upregulating proliferation cell nuclear antigen,Bcl-2,Bcl-xl mRNA and TFF1,EGF,p-EGFR,p-Src,pro-caspase-3,pro-caspase-9 protein expressions,mitochondrial viability,mitochondrial cytochrome C concentration and p-EGFR/EGFR,p-Src/Src,Bcl-2/Bax,Bcl-xl/Bad ratioes,downregulating Bax,Bad,Apaf-1 mRNA and cleaved-caspase-3,cleaved-caspase-9,cleaved-PARP-1 protein expressions,cytosol cytochrome C concentration.CONCLUSION TCS′s gastroprotective effect was closely connected with boosting TFF1 expression,acti⁃vating TFF1-mediated EGF/EGFR pathway,thus restraining mitochondrial-dependent apoptosis,which provided new insights into interpreting its underlying mechanism and promised to act as a candidate drug to treat gastric mucosal injury.

响应面法优化提取瓜蒌皮中总三萜的研究

目的 探讨用醇提法提取瓜蒌皮中总三萜化合物。方法 以瓜蒌皮为研究对象,以乙醇为溶剂,采用紫外分光光度法对瓜蒌皮中总三萜化合物的含量进行测定。通过单因素实验研究液固比、提取温度、提取时间、乙醇浓度对总三萜提取率的影响,在单因素实验的基础上,采用Box-Behnken Design响应面分析法研究乙醇提取的最佳工艺条件。结果 冷凝回流提取的最佳条件为液固比51 mL/g,乙醇浓度83%、提取时间70 min、提取温度90℃;在此工艺条件下,总三萜的最佳提取率为2.324%。结论 研究结果与预测值基本一致,因此该模型可靠。

凌霄花总三萜的超声辅助提取工艺优化

目的 优化凌霄花总三萜类化合物的超声辅助提取工艺。方法 以总三萜提取率为评价指标,考察料液比、乙醇浓度、超声时间、超声功率等因素对提取率的影响,采用单因素试验和正交试验优化提取工艺。结果 凌霄花总三萜的最佳提取工艺为:料液比1/40(g·mL^(-1)),乙醇浓度60%,超声时间40min,超声功率100W。该条件下,凌霄花总三萜平均提取率为4.11%。结论 本研究优化了凌霄花总三萜的超声辅助提取工艺,该工艺稳定,提取效率较高,适合该药材三萜类化学成分的提取。

响应面法优化超声辅助提取蕨麻总三萜工艺研究

目的:优化超声辅助提取蕨麻总三萜工艺条件研究。方法:在单因素试验基础上,利用响应面法评估液料比、提取时间、提取温度对总三萜提取得率的影响。结果:超声辅助提取最佳工艺参数为液料比20∶1 mL/g,提取时间63 min,提取温度60℃,蕨麻总三萜提取得率可达4.73%±0.01%。结论:响应面法优化提取工艺切实可行,操作简单,总三萜含量高,可为蕨麻进一步开发利用提供依据。

星点设计-效应面法优化超声提取桂籽中三萜化合物的工艺研究

目的本研究以桂籽为原材料,采用星点设计(CCD)-效应面法(RSM)等多种方法优化桂籽总三萜(OFSTT)的提取工艺及其含量测定研究。方法采用单因素、Plackett-Burman(PB)、最陡爬坡和CCD-RSM实验,建立各因素与响应值之间的数学模型,确定OFSTT的最佳超声提取工艺。结果通过单因素试验,得到了关于桂籽总三萜含量变化的趋势线,进一步利用PB实验筛选出对OFSTT产生显著影响的因素(提取功率、液料比及提取次数),通过最陡爬坡实验设计出极值点,以此作为效应面设计的中心点,采用星点设计-效应面法优化了OFSTT提取工艺的最佳提取工艺条件:乙醇溶剂分数60%,液料比25∶1(mL/g),提取温度65℃,提取功率325W,提取时间30min,提取3次;该条件下OFSTT的提取率为7.251%,实际值与预测值的偏差为2.05%。结论本研究采用CCD-RSM实验优化了OFSTT的提取工艺,该工艺稳定,提取率较高,实际值与预测值吻合度高,为后续桂籽三萜类物质进一步结构鉴定及生物活性作用研究提供参考价值。

牛樟芝总三萜提取工艺优化及其抗氧化活性研究

牛樟芝是我国台湾特有的珍稀药食两用真菌,含有丰富活性成分,具有抗癌、抗肿瘤和保肝等多种药理作用,三萜类化合物被认为是牛樟芝中的重要药用物质,不同提取工艺对牛樟芝总三萜得率影响不同.为探究牛樟芝总三萜最佳提取工艺及其抗氧化活性.选取不同提取溶剂、温度、时间、液料比,采用单因素试验方法和正交试验方法探究不同因素对牛樟芝总三萜得率的影响,并通过高效液相色谱(HPLC)分析不同溶剂提取工艺之间的成分差异,比较分析其抗氧化活性.结果表明,牛樟芝总三萜提取最佳工艺为:二氯甲烷为提取溶剂、液料比1∶320 g·mL^(-1)、45℃提取5 h.在此条件下,牛樟芝总三萜得率为10.16±0.077 6%,通过HPLC分析,所得粗提物成分丰富且具有较好的抗氧化活性,其中DPPH清除能力的IC50值达0.137 6,总还原能力达58.03%.通过对牛樟芝提取工艺优化显著提高了牛樟芝总三萜得率,为牛樟芝活性成分提取、化合物分离及开发利用提供理论参考.

超临界CO_2萃取灵芝子实体中的三萜类成分

目的:筛选超临界CO2萃取灵芝子实体中三萜类成分的最佳工艺条件。方法:采用RP-HPLC测定灵芝酸B的含量、可见分光光度法测定灵芝总三萜含量,设计正交试验优化超临界CO2萃取灵芝子实体中三萜类成分的工艺条件。结果:超临界CO2萃取灵芝子实体中三萜类成分的最佳工艺条件:萃取压力为25 MPa,萃取温度为45℃,萃取时间为1.5 h,夹带剂(95%乙醇)用量为3 mL.g-1。结论:超临界CO2萃取灵芝子实体中三萜类成分具有萃取效率高、萃取时间短、操作简单等优点,其方法可靠,切实可行。

超声辅助提取青钱柳叶总三萜化合物研究

以青钱柳叶为原料,以乙醇为溶剂,超声辅助提取总三萜化合物。对提取液乙醇体积分数、料液比和提取时间3个主要因素进行单因素和正交优化实验,并对提取级数和正丁醇萃取次数进行探索。结果表明:体积分数为65%乙醇提取液、1:12料液比、30min提取时间为优化参数,优化条件下得率为9.19%;乙醇溶液2级提取和正丁醇2次等体积萃取,总三萜化合物提取较为完全。

大孔树脂吸附纯化青钱柳叶三萜化合物

为得到纯度较高的青钱柳叶三萜化合物,采用大孔树脂吸附法对青钱柳叶三萜粗提物进行纯化研究。静态吸附实验结果表明,AB-8树脂对青钱柳叶三萜化合物吸附、解吸性能较好,比饱和吸附量为77.49mg/g,解吸率为85.44%,总回收率可达72.01%。AB-8树脂动态吸附-解吸实验表明:上柱流速增大,吸附率呈降低趋势;随着上柱液质量浓度增大,吸附率先升后降;95%乙醇洗脱效果较好,10BV为合理用量;随着洗脱流速增大,洗脱液峰浓度降低,洗脱率减小,综合考虑以1.5mL/min较为适宜。经AB-8树脂纯化后,三萜类物质纯度可达44.30%。

泽泻总三萜提取物对大鼠泌尿系草酸钙结石形成的影响

目的研究泽泻总三萜提取物对大鼠尿草酸钙结石形成的影响,从而确认泽泻抗泌尿系结石的活性成分。方法在实验的28d内给予乙二醇及阿法骨化醇诱导雄性SD大鼠泌尿系草酸钙结石形成。造模的同时分别给予不同剂量的泽泻总三萜提取物,分别为205.2、68.4及22.8mg/kg。实验结束时,检测各组大鼠体重,血尿素氮(BUN)、肌酐(Cr)、P、Ca2+、Mg2+含量,24h尿量,尿pH值,24h尿Ca2+、Mg2+、尿草酸(Ox)的分泌量,右肾系数,肾Ca2+、Mg2+含量;显微镜下观察肾组织切片中草酸钙结晶沉积及病理变化,评价泽泻总三萜对泌尿系结石形成的影响。结果乙二醇及阿法骨化醇诱导的泌尿系草酸钙结石大鼠血BUN、Cr、24h尿Ox、尿Ca2+分泌量、肾Ca2+含量及右肾系数明显升高,肾Mg2+含量明显下降。泽泻总三萜提取物能降低泌尿系结石大鼠的血BUN、Cr、24h尿Ca2+含量、肾Ca2+含量及右肾系数水平,增加24h尿量及肾组织Mg2+含量。肾组织病理学检查可知泽泻总三萜能减少大鼠肾组织内草酸钙晶体的沉积,改善肾脏组织的损伤情况。结论泽泻总三萜提取物可以有效抑制乙二醇及阿法骨化醇诱导的大鼠泌尿系草酸钙结石的形成,泽泻总三萜是泽泻抗泌尿系结石的活性成分。

夏枯草总三萜调控ERK、TGF-β1/Smad通路对肝纤维化大鼠的保护作用研究

目的研究夏枯草总三萜(TTP)对四氯化碳(CCl4)致肝纤维化大鼠的保护作用及其分子机制。方法 SD大鼠随机分为正常组、模型组、TTP(25、50、100 mg·kg-1)组和阳性对照组(秋水仙碱0.1 mg·kg-1),除正常组外,其余各组分别于大鼠背部皮下注射CCl40.1 ml·(100 g)-1,每周2次,连续12周,自造模第5周起开始给药,各给药组分别给予相应的药物,正常组、模型组给予等体积的溶媒,每天1次。实验结束后,比色法测定血清中丙氨酸氨基转氨酶(ALT)、天冬氨酸氨基转移酶(AST)含量;放免法测定透明质酸(HA)、Ⅲ型前胶原(PCⅢ)、Ⅳ型胶原(CⅣ)含量;同时取固定部位肝组织,苏木精伊红染色(HE)、Masson染色观察肝纤维化程度;制备100 g·L-1肝匀浆,进行丙二醛(MDA)、超(过)氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GSH-Px)、羟脯氨酸(Hyp)含量测定;RT-PCR法检测α-SMA、Procollagen I、Smad2、Smad3和Smad7 mRNA表达;Western blot法检测pERK蛋白表达。结果与模型组相比,TTP(25、50、100 mg·kg-1)给药组不仅能降低肝纤维化大鼠ALT、AST、HA、CⅣ、PCⅢ、Hyp水平,改善肝脏病变程度,降低MDA水平,增强SOD以及GSH-Px活性,还可抑制肝组织中α-SMA、Procollagen I、Smad2、Smad3及p-ERK表达,升高Smad7表达。结论夏枯草总三萜对CCl4诱导的肝纤维化大鼠具有较好的保护作用,其机制可能与下调p-ERK表达,调控TGF-β1/Smad信号通路有关。

树舌灵芝总三萜提取工艺优化及其抗氧化作用研究

以树舌灵芝为原料,研究总三萜的提取工艺及其抗氧化性。选择料液比、乙醇浓度、超声温度和超声时间进行单因素实验,在单因素实验基础上,采用Box-Behnken试验设计,以树舌灵芝总三萜得率为响应值进行响应面分析,确定最优工艺参数为:料液比1∶20(g/m L),乙醇浓度70%,超声温度55℃,超声时间60 min。在此工艺条件下进行5次验证性实验,树舌灵芝总三萜的提取得率平均值为1.75%。并通过测定DPPH的清除率、羟基自由基的清除率以及总还原力,研究其抗氧化活性。

响应面试验优化苹果渣总三萜超声提取工艺

利用超声波提取技术结合响应面分析法对富士苹果渣中总三萜的提取工艺进行优化。选择苹果渣粉碎粒度、液固比、乙醇体积分数、超声时间和超声温度进行单因素试验,在此基础上采用Plackett-Burman因素筛选设计对影响超声波提取苹果渣总三萜的因素进行试验,筛选出影响显著的因素;然后根据Box-Behnken试验设计原理,选取三因素三水平,以苹果渣总三萜得率为响应值进行响应面分析,确定最优工艺参数。结果表明:PlackettBurman设计筛选出粉碎粒度、液固比和乙醇体积分数为对苹果渣总三萜得率有显著影响的因素;通过响应面分析,确定苹果渣总三萜最优提取工艺为粉碎粒度100目、液固比12∶1(m L/g)、提取溶剂为无水乙醇、超声时间20 min、超声温度40℃,在此条件下富士苹果渣总三萜的得率为(7.10±0.01)%。

扁担藤总黄酮和总三萜提取工艺及抗氧化研究

目的:研究扁担藤总黄酮和总三萜的提取工艺及抗氧化活性。方法:采用正交试验优化扁担藤中总黄酮和总三萜的最佳提取工艺,并采用FRAP法、水杨酸法和ABTS法测定其抗氧化能力。结果:扁担藤总黄酮提取的最佳条件为70%乙醇在70℃超声波提取3次,每次1 h;总三萜提取的最佳条件为60%乙醇在70℃微波提取2次,每次5 min。与对照品抗坏血酸和茶多酚相比较,富含黄酮的扁担藤的Fe3+还原抗氧化能力和清除ABTS+.能力均大于茶多酚,但清除OH.的能力均小于二者。结论:超声法提取总黄酮和微波法提取总三萜效果最好,扁担藤具有一定的抗氧化性能。

夏枯草总三萜对四氯化碳致急性肝损伤大鼠的保护作用

目的研究夏枯草总三萜(TTP)对大鼠急性肝损伤的保护作用。方法 60只SD大鼠随机均分为对照组、模型组、TTP(62.5、125、250 mg/kg)3个剂量组和联苯双酯(200mg/kg)组。各给药组及联苯双酯组预防给药6 d,第6天给药结束后腹腔注射50%CCl4(2 ml/kg)诱导大鼠急性肝损伤模型,观察TTP对大鼠血清中丙氨酸氨基转移酶(ALT)、天门冬氨酸氨基转移酶(AST)水平的影响以及对肝匀浆中丙二醛(MDA)、超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GSH-Px)水平的影响;肝组织HE染色;RT-PCR法、West-ern blot法检测肝组织细胞色素P4502E1(CYP2E1)表达。结果 TTP各剂量组可降低急性肝损伤大鼠血清中ALT、AST活性,降低肝匀浆MDA的水平,升高SOD、GSH-Px的水平,抑制肝组织中CYP2E1的表达;同时,病理组织学检查结果显示TTP各剂量组大鼠肝组织病变程度明显减轻。结论TTP对CCl4致大鼠急性肝损伤具有一定的保护作用,其机制可能与抗机体脂质过氧化、抑制CYP2E1表达有关。

番石榴叶总三萜对2型糖尿病大鼠的降血糖和血脂作用

目的:探讨番石榴叶总三萜(TTPGL)对2型糖尿病大鼠血糖及血脂的影响。方法:采用高糖高脂饮食加腹腔注射小剂量链脲佐菌素(STZ,35 mg.kg-1)方法建立2型糖尿病大鼠模型。将造模成功的糖尿病大鼠随机分为5组:糖尿病模型组,TTPGL低、中、高剂量组(60、120、240 mg.kg-1),罗格列酮阳性对照组(3 mg.kg-1)。另取12只正常大鼠设为正常对照组。给药组每天灌胃给药1次,连续给药6周;模型组和正常对照组则给予同体积的生理盐水灌胃。给药6周后,采用葡萄糖氧化酶法测定大鼠的空腹血糖(FBG);放射免疫法测定空腹胰岛素(FINS),并计算胰岛素敏感指数(ISI);酶联免疫法测定大鼠的甘油三酯(TG)、总胆固醇(TCH)、游离脂肪酸(FFA)和糖化血红蛋白(GHb);果糖胺法测定糖化血清蛋白(GSP);Western blotting检测脂肪组织过氧化物酶体增殖物激活受体γ(PPARγ)的表达情况。结果:与正常对照组相比,糖尿病模型组血脂、FBG以及GHb显著升高,FINS及ISI显著下降,脂肪细胞PPARγ蛋白表达水平降低。与模型组相比,TTPGL中、高剂量组大鼠的FBG和GSP显著降低,FINS以及ISI显著升高,脂肪组织PPARγ蛋白的表达水平升高(P<0.01或P<0.05);此外,TTPGL能显著降低糖尿病大鼠血脂水平,TG、TCH和FFA含量均明显降低(P<0.01或P<0.05)。结论:TTPGL能显著降低2型糖尿病大鼠的血糖和血脂水平,明显改善糖尿病动物的糖脂代谢紊乱,升高血清胰岛素水平,提高胰岛素敏感指数;其抗糖尿病作用机制可能与其增加PPARγ蛋白的表达有关。