Bonannione A (6-Geranylnaringenin; Mimulone) 是一种异戊二烯类黄酮，一种口服有效的蛋白酪氨酸磷酸酶 1B (PTP1B) 抑制剂，IC50为 14 μM。Bonannione A 触发半胱天冬酶依赖性细胞凋亡。Bonannione A 通过 p53 介导的 AMPK/mTOR 通路诱导自噬。Bonannione A 显示出抗炎、抗自由基和抗癌活性。
| 生物活性 | Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potentprotein tyrosinephosphatase1B (PTP1B)inhibitor with anIC50of 14 μM. Bonannione A triggers caspase-dependentapoptosis. Bonannione A inducesautophagythrough p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity[1][2][3]. |
体外研究
(In Vitro) | 6-香叶草基柚皮素 (0-80 μM; 12, 24 小时) 在癌细胞系中以剂量和时间依赖性方式显着抑制细胞增殖[2]。
6-香叶草基柚皮素 (0-60 μM; 24 小时) 在 A549 细胞中触发半胱天冬酶依赖性细胞凋亡。6-香叶草基柚皮素增加凋亡亚 G1 期细胞的积累和 G2/M 期细胞的数量[2]。
6-香叶草基柚皮素 (60 μM; 24 小时) 在 A549 细胞中触发自噬而不损害自噬通量[2]。
6-香叶草基柚皮素 (60 μM; 24 小时) 显着降低 p53 和磷酸化 mTOR 的水平[2]。
Cell Proliferation Assay[2] | Cell Line: | Human lung cancer A549, breast cancer MCF-7, colon cancer HCT116 and osteosarcoma U2OS cells | | Concentration: | 20, 40, 60, 80 μM | | Incubation Time: | 12, 24 h | | Result: | Significantly inhibited cell proliferation in a dose- and time-dependent way in these cancer cell lines. |
Apoptosis Analysis[2] | Cell Line: | A549 cells | | Concentration: | 0-60 μM | | Incubation Time: | 24 h | | Result: | Annexin V/PI-positive cells were markedly increased in a dose- and time-dependent way.
Induced apoptosis through caspase-3 activation and PARP cleavage. |
Cell Cycle Analysis[2] | Cell Line: | A549 cells | | Concentration: | 0-60 μM | | Incubation Time: | 24 h | | Result: | Increased accumulation of cells at the apoptotic sub-G1 phase in a dose-dependent manner.
The number of cells at G2/M phase also increased in a dose-dependent manner. |
Cell Autophagy Assay[2] | Cell Line: | A549 cells | | Concentration: | 60 μM | | Incubation Time: | 24 h | | Result: | Remarkably increased ATG7 and LC3-II protein levels in a dose-dependent way, but Beclin-1 level was slightly augmented. |
Western Blot Analysis[2] | Cell Line: | A549 cells | | Concentration: | 60 μM | | Incubation Time: | 0-24 h | | Result: | Remarkably decreased the levels of p53 and phospho-mTOR.
Significantly increased whereas the levels of phospho-AMPK and phospho-Acetyl-CoA Carboxylase (ACC), an AMPK substrate. |
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体内研究
(In Vivo) | 6-香叶草基柚皮素 (25 mg/kg; 灌胃; DSS 前 48 和 24 小时，随后每 24 小时一次; 持续 5 天) 改善结肠炎的症状并延迟其发作[3]。
| Animal Model: | Male Wistar rats (180-220 g)[3] | | Dosage: | 25 mg/kg | | Administration: | Gavage; 48 and 24 h prior to DSS (10% (w/v)) and every 24 h on the following days; for 5days | | Result: | Ameliorated the symptoms of colitis and delayed their onset.
Showed the low DAI on the last day of the experiment. |
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| 来源 | - Plants
- Scrophulariaceae
- Paulownia tomentosa(Thunb.) Steud.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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