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排序方式: 共有74条查询结果,搜索用时 15 毫秒
1.
AIM: To study the enzyme activity of CYP2C18 variant with exon 5 skipped. METHODS: A full length CYP2C18 cDNA X1 and an exon 5 skipped variant CYP2C18 X2 were separately subcloned into mammalian expression vector pREP9 to transfect HepG2 cells. The expression of CYP2C18 mRNA in transgenic cells and human liver tissues were determined by RT-PCR. The enzyme activity of CYP2C18 to oxidate tolbutamide in postmitochondrial supernate (S9) fraction was determined by HPLC. The cytotoxicity of ifosfamide to transgenic cells was evaluated by MTT test. RESULTS: HepG2-CYP2C18 X1 cells showed strong expression of the full length CYP2C18 mRNA. On the other hand, HepG2-CYP2C18 X2 cells had only infinitesimal expression of the exon-skipped CYP2C18 as well as the full length CYP2C18, while non-transfected HepG2 cell only demonstrated an infinitesimal expression of the full length CYP2C18. The expression of CYP2C18 exons 2 to 7 was also analyzed by RT-PCR in 7 extratumoral liver tissues. Among them, 3 samples expressed on  相似文献   
2.
This study aims to investigate the protective effects of the Bauhinia championii (BC) against ischemia/reperfusion (I/R)‐induced injury in an isolated heart model. Langendorff‐perfused C57BL/6JNarl mice hearts were performed with 30 minutes ischemia and 60 minutes reperfusion by left anterior descending artery ligation. Before reperfusion, boiling water extracts of BC (10 mg/L) was pretreated for 15 minutes. During reperfusion, BC significantly decreased the occurrence of ventricular arrhythmias by lead II electrocardiogram (ECG). Electrophysiological effect of BC was further determined in isolated ventricular myocytes by whole‐cell patch clamp technique. The underlying mechanism may result from its Na+ channel blocking activity characterized with reduced rise slope of action potential and Na+ current density. Moreover, BC dramatically reduced I/R‐caused infarct size, which was accessed by 2,3,5‐triphenyltetrazolium chloride (TTC) assay. Since BC decreased I/R‐induced myoglobin release and oxidation of Ca2+‐calmodulin‐dependent protein kinase, inhibition of myocardial necroptosis may account for the protective effects of BC on myocytes lose. This study indicated that BC may prevent I/R induced ventricular arrhythmias and myocyte death by blocking Na+ channels and decreasing necroptosis, respectively. Since most of the available antiarrhythmic remedies have unwanted adverse actions, BC could be a novel candidate for the treatment of myocardial infarction and ventricular arrhythmia.  相似文献   
3.
目的 建立测定大鼠血浆中5,7,3',4 ',5'-五甲氧基黄酮浓度的HPLC法,并研究其药动学行为.方法 2组大鼠分别灌胃给予龙须藤总黄酮(给药剂量为60 mg/kg)和5,7,3',4',5'-五甲氧基黄酮(给药剂量为113 mg/kg),采用高效液相色谱法测定血浆中5,7,3',4',5'-五甲氧基黄酮的浓度,以软件DAS2.0计算药动学参数.结果 大鼠灌胃5,7,3',4',5'-五甲氧基黄酮和龙须藤总黄酮后,5,7,3',4 ',5'-五甲氧基黄酮的体内过程均符合单室模型,主要药动学参数如下:A UC0-∞分别为(5.502 ± 1.302)、(4.192±0.232) (mg·h)/L,Cmax分别为(0.689 ±0.065)、(0.758 ±0.157) mg/L,Tmax分别为(3.111 ±0.434)、(1.430±0.365)h,T1/2分别为(2.444 ±0.287)、(2.700 ±0.890)h.结论 以小剂量龙须藤总黄酮给药较单体给药时5,7,3',4',5'-五甲氧基黄酮血药浓度峰值高,吸收速率常数大,达峰时间短,龙须藤总黄酮中共存的其他成分可能有促进5,7,3',4',5'-五甲氧基黄酮吸收的作用.  相似文献   
4.
Introduction: Diabetes Mellitus has been considered an epidemic by the World Health Organization, with a high risk of morbidity and mortality. The treatment of this pathology consists in glycemic control, which can be done by oral hypoglycemic agents, insulin therapy, dietary guidance, regular physical activity, and psychosocial support. In addition, other adjuvant treatments are employed, such as phytotherapic, and one of the most used plants is Bauhinia forficata.

Areas covered: In the current review, patents using Bauhinia forficata for the Diabetes Mellitus treatment have been analyzed. There were 03 patents in WIPO, 01 in Espacenet, 01 in USPTO, and 02 in INPI.

Expert opinion: Patents on the adjuvant treatment of Diabetes Mellitus by Bauhinia forficata are discussed. Although there are some phytotherapy products containing this medicinal plant which has hypoglycemic effect here is still a need for the development of more products based on natural resources, for the treatment of this pathology, without side effects and with other benefits, to assist in the glycemia control in diabetic patients, and to improve their quality of life.  相似文献   

5.
Bauhinia scandens L. (Family: Fabaceae) is commonly used to treat cholera, diarrhea, asthma, and diabetes disorder in integrative medicine. This study aimed to screen the presence of phytochemicals (preliminary and UPLC-QTOF–M.S. analysis) and to examine the pharmacological activities of Bauhinia scandens L. stems (MEBS) stem extracts. Besides, in silico study was also implemented to elucidate the binding affinity and drug capability of the selected phytochemicals. In vivo anti diarrheal activity was investigated in mice models. In vitro, antibacterial and antifungal properties of MEBS against several pathogenic strains were evaluated using the disc diffusion method. In addition, in silico study has been employed using Discovery studio 2020, UCFS Chimera, PyRx autodock vina, and online tools. In the anti-diarrheal investigation, MEBS showed a significant dose-dependent inhibition rate in all three methods. The antibacterial and antifungal screening showed a remarkable zone of inhibition, of the diameter 14–26 mm and 12–28 mm, by MEBS. The present study revealed that MEBS has remarkable anti-diarrheal potential and is highly effective in wide-spectrum bacterial and fungal strains. Moreover, the in silico study validated the results of biological screenings. To conclude, MEBS is presumed to be a good source in treating diarrhea, bacterial and fungal infections.  相似文献   
6.
目的 考察用纤维素酶-乙醇协同提取龙须藤总黄酮的最佳提取工艺条件.方法 在单因素分析的基础上进行Box-Behnken效应面优化,以龙须藤总黄酮提取率为指标,并采用Design expert 7.0.0软件对数据进行分析.结果 纤维素酶-乙醇协同提取龙须藤总黄酮的最佳工艺条件为:每1 g药材酶用量9.13 mg、酶解时间2.06 h、酶解温度51.03℃.在优化条件下,提取率平均值为19.24%(RSD为1.68%),与预测值19.02%接近.结论 纤维素酶-乙醇协同提取龙须藤总黄酮可获得较高的提取率.  相似文献   
7.
目的研究湖北羊蹄甲〔Bauhinia glauca subsp.hupehana(Craib)T.Chen〕的化学成分。方法采用正向硅胶柱色谱、凝胶柱色谱、聚酰胺柱色谱等分离化学成分,通过理化性质和波谱数据分析鉴定化合物的结构。结果分离鉴定了5个化合物,分别为3,5,7,3′,5′-五羟基二氢黄酮醇(1)、圣草酚(2)、3-O-甲基槲皮素(3)、木犀草素(4)和黄颜木素(5)。结论化合物2和4为湖北羊蹄甲植物中首次分离;化合物1、3和5是羊蹄甲属中首次分离。  相似文献   
8.

Objectives:

Ethanol extract of the stem of Bauhinia purpurea Linn. was subjected to analgesic and anti-inflammatory activities in animal models.

Materials and Methods:

Albino Wistar rats and mice were the experimental animals respectively. Different CNS depressant paradigms like analgesic activity (determined by Eddy''s hot plate method and acetic acid writhing method) and anti-inflammatory activity determined by carrageenan induced paw edema using plethysmometer in albino rats) were carried out, following the intra-peritoneal administration of ethanol extract of Bauhinia purpurea Linn. (BP) at the dose level of 50 mg/kg and 100 mg/kg.

Results:

The analgesic and anti-inflammatory activities of ethanol extracts of BP were significant (P < 0.001). The maximum analgesic effect was observed at 120 min at the dose of 100 mg/kg (i.p.) and was comparable to that of standard analgin (150 mg/kg) and the percentage of edema inhibition effect was 46.4% and 77% for 50 mg/kg and 100 mg/kg (i.p) respectively. Anti-inflammatory activity was compared with standard Diclofenac sodium (5 mg/kg).

Conclusion:

Ethanol extract of Bauhinia purpurea has shown significant analgesic and anti-inflammatory activities at the dose of 100 mg/kg and was comparable with corresponding standard drugs. The activity was attributed to the presence of phytoconstituents in the tested extract.  相似文献   
9.

Objectives:

To evaluate the ethanolic and aqueous extracts of Bauhinia variegata Linn. for in vitro antioxidant and antihyperlipidemic activity.

Materials and Methods:

Ethanolic and aqueous extracts of the stem bark and root of B. variegata Linn. were prepared and assessed for in vitro antioxidant activity by various methods namely total reducing power, scavenging of various free radicals such as 1,2-diphenyl-2-picrylhydrazyl (DPPH), super oxide, nitric oxide, and hydrogen peroxide. The percentage scavenging of various free radicals were compared with standard antioxidants such as ascorbic acid and butylated hydroxyl anisole (BHA). The extracts were also evaluated for antihyperlipidemic activity in Triton WR-1339 (iso-octyl polyoxyethylene phenol)-induced hyperlipidemic albino rats by estimating serum triglyceride, very low density lipids (VLDL), cholesterol, low-density lipids (LDL), and high-density lipid (HDL) levels.

Result:

Significant antioxidant activity was observed in all the methods, (P < 0.01) for reducing power and (P < 0.001) for scavenging DPPH, super oxide, nitric oxide, and hydrogen peroxide radicals. The extracts showed significant reduction (P < 0.01) in cholesterol at 6 and 24 h and (P < 0.05) at 48 h. There was significant reduction (P < 0.01) in triglyceride level at 6, 24, and 48 h. The VLDL level was also significantly (P < 0.05) reduced from 24 h and maximum reduction (P < 0.01) was seen at 48 h. There was significant increase (P < 0.01) in HDL at 6, 24, and 48 h.

Conclusion:

From the results, it is evident that alcoholic and aqueous extracts of B. variegata Linn. can effectively decrease plasma cholesterol, triglyceride, LDL, and VLDL and increase plasma HDL levels. In addition, the alcoholic and aqueous extracts have shown significant antioxidant activity. By the virtue of its antioxidant activity, B. variegata Linn. may show antihyperlipidemic activity.  相似文献   
10.
湖北羊蹄甲化学成分的研究   总被引:4,自引:1,他引:3  
从湖北羊蹄甲的根中分离出3种化合物,根据其理化常数和光谱分析,分别鉴定为5,7-二羟基色原酮,香橙素和二氢槲皮素。  相似文献   
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