Girinimbine (Girinimbin) 是一种咔唑类生物碱，具有多种生物学作用。Girinimbine 可诱导细胞凋亡 (apoptosis)，具有抗锥虫、抗血小板活性、抗菌活性、抗炎、抗氧化和抗肿瘤活性。
| 生物活性 | Girinimbine (Girinimbin) is a carbazole alkaloid with a variety of biological effects. Girinimbine can induceapoptosis, and has antitrypanosomal, antiplatelet activity, antibacterial activity, anti-inflammatory, antioxidant and antitumor activities[1][2][3]. |
体外研究
(In Vitro) | Girinimbine (1-400 μM; 24-72 h) decreases the viability of HepG2 cells in 24, 48 and 72 h with IC50values of 61 μM, 56 μM, and 40 μM respectively. Girinimbine (10-100 μM; 24-48 h) increase of LDH leakage in both concentration- and time-dependent manner in HepG2 cells[1].
Girinimbine (56 μM; 24-48 h) treatment results in DNA fragmentation and elevates levels of caspase-3 in HepG2 cells[1].
HepG2 cells[1].
Girinimbine (56 μM; 12-48 h) treatment also displays a time-dependent accumulation of the Sub-G0/G1 peak (hypodiploid) and caused G0/G1-phase arrest[1].
Girinimbine shows a potent antitrypanosomal activitywith an IC50value of 10.16 μg/mL[3].
Cell Viability Assay[1] | Cell Line: | HepG2 cells | | Concentration: | 1 μM, 10 μM, 50 μM, 100 μM, 200 μM | | Incubation Time: | 24 h, 48 h and 72 h | | Result: | Inhibited the proliferation of HepG2 cells in vitro in a dose- and time-dependent manner. |
Apoptosis Analysis[1] | Cell Line: | HepG2 cells | | Concentration: | 56 μM | | Incubation Time: | 24 h, 48 h | | Result: | Showed typical morphological features of apoptosis. |
Cell Cycle Analysis[1] | Cell Line: | HepG2 cells | | Concentration: | 56 μM | | Incubation Time: | 12 h, 24 h, 48 h | | Result: | Induced G0/G1-phase arrest in HepG2 cells. |
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体内研究
(In Vivo) | Girinimbine (10-100 mg/kg; orally gavage; once) pretreatment helps limit total leukocyte migration, and reduced pro-inflammatory cytokine (IL-1β, TNF-α) levels in the peritoneal fluid[2].
In vivo in zebrafish embryos, Girinimbine (20 μg/mL; 24 hours) shows significant distribution of apoptotic cells in embryos[2].
| Animal Model: | Male ICR mice (25-35 g) treated with carrageenan[2] | | Dosage: | 10 mg/kg, 30 mg/kg, and 100 mg/kg | | Administration: | Orally gavage; once | | Result: | Helped limit total leukocyte migration, and reduced pro-inflammatory cytokine levels in the peritoneal fluid. |
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| 结构分类 | - Alkaloids
- Indole Alkaloids
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| 来源 | - Plants
- Rutaceae
- Murraya koenigii(L.) Spreng
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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) |
