Cycleanine 是一种高效的血管选择性Ca- 拮抗剂。Cycleanine 具有缓解疼痛、肌肉松弛和抗炎作用。Cycleanine 具有通过凋亡通路发挥抗卵巢癌作用的潜力。
| 生物活性 | Cycleanine is a potent vascular selectiveCalciumantagonist. Cycleanine has analgesic, muscle relaxant and anti-inflammatory activities. Cycleanine has potential for anti-ovariancanceracting through theapoptosispathway[1][2]. |
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体外研究
(In Vitro) | Cycleanine inhibits L-type Ca-current (ICaL) of single rat ventricular cardiomyocytes in a voltage- and frequency-dependent manner[1].
Cycleanine shows modestly less potency against human OSE cells (normal) than the cancer cells[2].
Cycleanine (20 μM; 48 hours) exhibits cytotoxicity for Ovcar-8, A2780, Igrov-1, and Ovcar-4 cell lines with IC50s ranging from 7 to 14 μM[2].
Cycleanine (20 μM; 24 hours) results in significant PARP cleavage (a marker of apoptosis)[2].
Cycleanine (20 μM; 48 hours) causes a significant increase of the population of both early and late apoptotic cells[2].
Cell Cytotoxicity Assay[2] | Cell Line: | Ovcar-8 cells, A2780 cells, Igrov-1 cells, Ovcar-4 cells | | Concentration: | 20 μM | | Incubation Time: | 48 hours | | Result: | Exhibited cytotoxicity for Ovcar-8, A2780, Igrov-1, and Ovcar-4 cell lines with IC50values of 10 μM, 7.6 μM, 14 μM, 7.2 μM, respectively. |
Western Blot Analysis[2] | Cell Line: | Ovcar-8 cells | | Concentration: | 20 μM | | Incubation Time: | 24 hours | | Result: | Induced 1.1-fold increase in PARP-1 cleavage compared with carboplatin. |
Apoptosis Analysis[2] | Cell Line: | Ovcar-8 cells | | Concentration: | 20 μM | | Incubation Time: | 48 hours | | Result: | Caused a significant increase of the population of both early and late apoptotic cells. |
Cell Cycle Analysis[2] | Cell Line: | Ovcar-8 cells | | Concentration: | 20 μM | | Incubation Time: | 48 hours | | Result: | Increased the percentage of Ovcar-8 cells in subG1. |
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体内研究
(In Vivo) | Cycleanine inhibits the KCl-induced contraction of rabbit aortic rings with an IC50of 0.8 nM[1].
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| 来源 | - Plants
- Menispermaceae
- Cissampelos pareira
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(8.03 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 1.6058 mL | 8.0289 mL | 16.0578 mL | | 5 mM | 0.3212 mL | 1.6058 mL | 3.2116 mL | | 10 mM | --- | --- | --- |
*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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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