Manzamine A hydrochloride 是一种具有口服活性的 β-carboline 生物碱，抑制GSK-3β和CDK-5的IC50值为 10.2 μM 和 1.5 μM。Manzamine A hydrochloride 靶向胰腺癌细胞的vacuolar ATPases并抑制自噬 (autophagy)。Manzamine A hydrochloride 具有抗疟和抗癌活性。Manzamine A hydrochloride 对HSV-1具有较强的活性。
| 生物活性 | Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specificallyGSK-3βandCDK-5withIC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A hydrochloride targetsvacuolar ATPasesand inhibitsautophagyin pancreaticcancercells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity againstHSV-1[1][2][3][4]. |
| IC50& Target[1][2][3] | GSK-3β 10.2 μM (IC50) | Plasmodium | CDK5 1.5 μM (IC50) | vacuolar ATPases | Malaria | HSV-1 |
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体外研究
(In Vitro) | Manzamine A (5-50 μM, 18 h) hydrochloride decreases tau phosphorylation, measured with ELISA[1].
Manzamine A (10 μM) hydrochloride inhibits yeastS. cerevisiaegrowth by 30%[2].
Manzamine A hydrochloride displays a few enlarged vacuoles in yeast[2].
Manzamine A (2.5-10 μM, 24 h) hydrochloride increases acidity in pancreatic cancer cells and non-malignant Vero cells[2].
Manzamine A (1 μM, 24 h) hydrochloride inhibits HSV-1 infection in SIRC cells[4].
Manzamine A hydrochloride shows antimalarial activity with an IC50of 8.0 nM (D6 clone) and 11 nM (W2 clone)[5].
Cell Viability Assay[4] | Cell Line: | SIRC cell | | Concentration: | 0.1, 0.5, 1, 2, 3, 5, and 10 μM | | Incubation Time: | 72 h | | Result: | Inhibited SIRC cell viability with an IC50of 5.6 μM. |
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体内研究
(In Vivo) | Manzamine A (50 and 100 mol/kg, p.o. or i.p.) hydrochloride inhibits the growth of the rodent malaria parasitePlasmodium bergheiin infected mice[6].
Manzamine A (8 mg/kg, i.p., daily for 8 consecutive days) hydrochloride prolongs the survival of SW mice to 20 days[7].
| Animal Model: | Plasmodium bergheiin infected mice[6] | | Dosage: | 50 or 100 mol/kg | | Administration: | Intraperitoneal injection (i.p.) or oral administration (p.o.) | | Result: | Inhibited the growth of the rodent malaria parasitePlasmodium berghei.
Prolonged the survival of highly parasitaemic mice. |
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| 分子量 | |
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| Formula | |
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| 结构分类 | - Alkaloids
- Pyridine Alkaloids
- Alkaloids
- Piperidine Alkaloids
- Alkaloids
- Indole Alkaloids
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| 来源 | |
| 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 : 5.88 mg/mL(10.05 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.7088 mL | 8.5438 mL | 17.0876 mL | | 5 mM | 0.3418 mL | 1.7088 mL | 3.4175 mL | | 10 mM | 0.1709 mL | 0.8544 mL | 1.7088 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；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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