芸苔素内酯作用机制 - Medchemexpress - MCE中国

1、Product Data SheetBrassinolideCat. No.: HY-N0273CAS No.: 72962-43-7分式: CHO分量: 480.68作靶点: Apoptosis作通路: Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (208.04 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.0804 mL 10.4

2、019 mL 20.8039 mL5 mM 0.4161 mL 2.0804 mL 4.1608 mL10 mM 0.2080 mL 1.0402 mL 2.0804 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液

3、可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.20 mM); Clear solution此案可获得 2.5 mg/mL (5.20 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均

4、匀。2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.20 mM); Clear solution此案可获得 2.5 mg/mL (5.20 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Brassinolide种主 的植物长调节剂，可调节植物细胞伸长。IC & Target plant gr

5、owth modulator1体外研究 Brassinolide is a plant sterol first isolated from pollen of rape (Brassica napus L.). Brassinolide can induce a time andconcentration-dependent cytotoxicity in PC-3 cells. The mode of cell death appears to be predominately apoptosis, asshown by flow-cytometric analysis, fluoresc

6、ence and transmission electron microscopes. Caspase-3 activity isobviously increased after Brassinolide treatment. Western blot studies indicate that treatment with Brassinolidetriggered a time-dependent decrease in the expression of anti-apoptotic protein Bcl-2, which suggests thatBrassinolide can

7、induce cytotoxicity in PC-3 cells by triggering apoptosis. Brassinolide might therefore be a promisingcandidate for the treatment of prostate cancer1. Brassinolide is a plant growth modulator, on multidrug resistance(MDR) of human T lymphoblastoid cell line CCRF-VCR 1000 which is obtained by progres

8、sively addition of vincristine(VCR) to sensitive CCRF-CEM cells, and to explore preliminarily the mechanism of reversing action. After treatment ofBrassinolide under the concentration of 0.001-10 g/mL, the resistance of CCRF-VCR is reversed partly with thereversing folds respectively as 4.4-11.6. Th

9、e intracellular accumulation of rhodamine 123 is significantly reduced in theresistant cells. After treatment of Brassinolide, the accumulation increased, the level of fluorescent dye is situatedbetween resistant cells and sensitive cells. No alteration of the catalytic activity of topoisomerase II

10、is found amongthree groups. The level of protein expression of p53 in resistant cells is higher than that of sensitive cells. AfterBrassinolide treatment, the expression of p53 in CCRF-VCR cells restored to the level of sensitive cells. Brassinolidecan effectively reverse the resistance of CCRF-VCR

11、cells by inhibiting the effusion of drug transported by P-glucoprotein. To down regulate the abnormal expression of p53 maybe one of the mechanisms of reversing MDR forBrassinolide2.PROTOCOLCell Assay 2 MTT method is used to detect the resistant factor of resistant cell line and the reversing fold a

12、fter addition ofBrassinolide. The intracellular accumulation of rhodamine 123, a fluorescent dye transported by P-glycoprotein isdetected by flow cytometry, the catalytic activity of topoisomerase II is assessed by Sulliven method to find the effectof Brassinolide on resistance. The protein expressi

13、on of p53 is measured using Western blotting in the sensitive cellsand resistant cells to explore the effect of Brassinolide2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Wu YD, et al. Brassinolide, a plant sterol from pollen of Brassica

14、 napus L., induces apoptosis in human prostate cancer PC-3 cells. Pharmazie. 2007May;62(5):392-5.2. Xian LJ, et al. Reversing effect of brassinolide on multidrug resistance of-CCRF-VCR1000 cells and a preliminary investigation on its mechanisms. Yao XueXue Bao. 2005 Feb;40(2):117-21.McePdfHeightPage 2 of 3 www.MedChem