乌索酸药理作用研究进展

乌索酸为五环三萜类药合物,资源广,毒性低、具有广泛的生物活性。有抗肿瘤、抗氧化、抗肝炎、抗炎抑菌,降血脂1抗溃疡等作用。尤其抗肿瘤、抗氧化、抗肝炎作用显,有望成为抗肿瘤,抗肝炎药物。     

薄层扫描法测定祛浊胶囊中熊果酸的含量

用薄层扫描法测定祛浊胶囊中熊果酸的含量。方法　以氯仿-醋酸乙酯-冰醋酸(5∶3∶0 .1)为展开剂,λS=5 30nm,λR=70 0nm。结果　平均回收率为97 .10 %,RSD =0 . 83%。结论　该方法简便,准确,可用于控制该产品的质量     

均匀设计在熊果酸提取工艺中的应用

采用均匀设计对连翘中熊果酸的提取工艺进行考察,以乙醇浓度、提取时间、液固比、提取次数为考察因素,采用U7(7)4表进行实验,根据多元回归方程得到最佳提取工艺为:乙醇浓度为75%,其加入量为原料的7倍,提取2次,每次60 min.     

HPTLC evaluation of oleanolic acid and ursolic acid from the methanol extract of Wattakaka volubilis

ObjectiveTo find out the secondary metabolites present in the methanol extract of Wattakaka volubilis (W. volubilis).MethodsHigh performance thin layer chromatography method for the quantification of triterpenoids in soxhlet methanol extract of W. volubilis is described by densitometric scanning. The linear regression data from the calibration curve was plotted over the range of 10–25 μg/mL, r² = 0.992 46, 0.950 42 respectively. A mixture of toluene: methanol (9:1) was used as mobile phase for oleanolic acid were petroleum ether: chloroform: ethyl acetate: methanol (4:1:0.1:0.1) were used for ursolic acid.ResultsThe results showed that the presence of oleanolic acid and ursolic acid in methanol extract. The content found to be 218.30 ng and 509.99 ng/10 mg of extract.ConclusionFor conclusion, above study scientifically validated as a useful traditional medicine with the identification of bioactive secondary metabolites.     

高效液相色谱法测定治咳川贝枇杷露中熊果酸的含量

目的：建立治咳川贝枇杷露中熊果酸含量测定方法。方法：采用高效液相色谱法,使用Cosmosil-C18（250 mm×4.6 mm,5μm）为色谱柱;甲醇∶水∶冰醋酸∶三乙胺（90∶10∶0.03∶0.06）为流动相;流速为1.0 ml·min^-1;柱温为室温（25℃）,检测波长为215 nm。结果：样品中熊果酸在16-80μg·ml-1浓度范围内呈线性关系,r=0.999 5（n=5）,加样回收率为98.67%,RSD为1.22%（n=6）。结论：本法简便、准确、可靠、专属性强、重复性好、可作为治咳川贝枇杷露中熊果酸的含量测定。     

Ursolic Acid-Induced Elevation of Serum Irisin Augments Muscle Strength During Resistance Training in Men

Ursolic acid (UA), a type of pentacyclic triterpenoid carboxylic acid purified from natural plants, can promote skeletal muscle development. We measured the effect of resistance training (RT) with/without UA on skeletal muscle development and related factors in men. Sixteen healthy male participants (age, 29.37±5.14 years; body mass index=27.13±2.16 kg/m²) were randomly assigned to RT (n=7) or RT with UA (RT+UA, n=9) groups. Both groups completed 8 weeks of intervention consisting of 5 sets of 26 exercises, with 10~15 repetitions at 60~80% of 1 repetition maximum and a 60~90-s rest interval between sets, performed 6 times/week. UA or placebo was orally ingested as 1 capsule 3 times/day for 8 weeks. The following factors were measured pre-and post-intervention: body composition, insulin, insulin-like growth factor-1 (IGF-1), irisin, and skeletal muscle strength. Body fat percentage was significantly decreased (p<0.001) in the RT+UA group, despite body weight, body mass index, lean body mass, glucose, and insulin levels remaining unchanged. IGF-1 and irisin were significantly increased compared with baseline levels in the RT+UA group (p<0.05). Maximal right and left extension (p<0.01), right flexion (p<0.05), and left flexion (p<0.001) were significantly increased compared with baseline levels in the RT+UA group. These findings suggest that UA-induced elevation of serum irisin may be useful as an agent for the enhancement of skeletal muscle strength during RT.     

民族药青刺尖抗炎活性成分的初步研究

目的结合抗炎药效学的筛选实验,研究青刺尖抗炎活性部位中的化学成分。方法95%乙醇提取,系统溶剂法及硅胶柱色谱分离,用化学和1HNMR1、3CNMR等光谱学方法鉴定化合物。结果分离并鉴定了正三十四烷醇(Ⅰ)和熊果酸(Ⅱ)两个化合物。结论化合物Ⅰ和Ⅱ为首次从青刺尖中分得。     

Ursolic acid restores sensitivity to gemcitabine through the RAGE/NF-κB/MDR1 axis in pancreatic cancer cells and in a mouse xenograft model

Gemcitabine (GEM) is a first-line drug for pancreatic cancer therapy, but GEM resistance is easily developed in patients. Growing evidence suggests that cancer chemoprevention and suppression are highly associated with dietary phytochemical and microbiota composition. Ursolic acid (UA) has anti-inflammatory and anticancer effects; however, its role in improving cancer drug resistance in vivo remains unclear. In this study, the aim was to explore the role of UA in managing drug resistance-associated molecular mechanisms and the influence of gut microbiota. The in vitro results showed that receptor for advanced glycation end products (RAGE), nuclear factor kappa B p65 (NF-κB/p65), and multidrug resistance protein 1 (MDR1) protein levels were significantly increased in GEM-resistant pancreatic cancer cells (named MIA PaCa-2 ^GEMR) compared to MIA PaCa-2 cells. Downregulation of RAGE, pP65, and MDR1 protein expression not only was observed following UA treatment but also was seen in MIA PaCa-2 ^GEMR cells after transfection with a RAGE siRNA. Remarkably, the enhanced effects of UA coupled with GEM administration dramatically suppressed the RAGE/NF-κB/MDR1 cascade and consequently inhibited subcutaneous tumor growth. Moreover, UA could increase alpha diversity and regulate the composition of gut microbiota, especially in Ruminiclostridium 6. Taken together, these results provide the first direct evidence of MDR1 attenuation and chemosensitivity enhancement through inhibition of the RAGE/NF-κB signaling pathway in vitro and in vivo, implying that UA may be used as an adjuvant for the treatment of pancreatic cancer in the future.     

熊果酸对活化T细胞功能的影响

目的 研究熊果酸在体外对活化的人T细胞功能的影响,探讨其作为免疫调节药物开发的可能性和提供相关实验数据.方法 无菌采集和分离正常人外周血淋巴细胞,以不同浓度的熊果酸和PHA/PMA刺激T细胞,用MTT法检测细胞的增殖反应,ELISA法检测细胞因子IFN-γ、IL-2、GM-CSF、IL-4的峰值浓度.结果 熊果酸对淋巴细胞的活化和增殖无显著影响(P＞0.05);熊果酸抑制IFN-γ、IL-2、GM-CSF的分泌,并呈剂量依赖性(P＜0.05),而对IL-4的分泌影响较小,无统计学意义(P＞0.05).结论 熊果酸抑制活化的T细胞分泌Th1型细胞因子,抑制T细胞的功能,熊果酸有可能作为治疗某些自身免疫性疾病天然药物成分.     

熊果酸对人骨肉瘤MG63细胞的影响

目的 探讨熊果酸(UA)对人骨肉瘤MG63细胞的影响作用及其机制.方法 体外培养骨肉瘤MG63细胞,应用浓度为10、20、50、100 μmol/L的熊果酸干预骨肉瘤MG63细胞,噻唑蓝(MTT)比色法检测细胞的增殖,逆转录-聚合酶链反应(RT-PCR)技术检测细胞中骨形态发生蛋白(BMP)-2和BMP-6的mRNA的表达,并应用蛋白印记技术检测相应蛋白的表达水平.结果 熊果酸干预组的肿瘤细胞增殖被明显抑制,72 h时100 μmol/L组的增殖活性为(0.25±0.03),而10μmol/L组的增殖活性为(0.86±0.10),差异有统计学意义(P＜0.05),各浓度组在24、48、72 h时的增殖活性差异均有统计学意义(P＜0.05);BMP-2和BMP-6 mRNA和蛋白的表达水平在实验组和对照组间差异均有统计学意义(P＜0.05),而两对照组之间差异无统计学意义(P＞0.05).结论 熊果酸能够抑制骨肉瘤MG63细胞的增殖,并能够促进细胞中BMP-2和BMP-6的表达.