(Z)-Guggulsterone 是印度阿育吠陀药用植物Commiphora mukul的成分,通过引起细胞凋亡 (apoptosis) 来抑制人前列腺癌细胞的生长。 (Z)-Guggulsterone 通过抑制VEGF-VEGF-R2-Akt信号传导轴来抑制血管生成。(Z)-Guggulsterone 也是FXR拮抗剂。(Z)-Guggulsterone 可降低ACE2表达和SARS-CoV-2感染。
生物活性 | (Z)-Guggulsterone, a constituent of Indian Ayurvedic medicinal plantCommiphora mukul, inhibits the growth of human prostatecancercells by causingapoptosis. (Z)-Guggulsterone inhibits angiogenesis by suppressing theVEGF–VEGF-R2–Aktsignaling axis[1]. (Z)-Guggulsterone is also a potentFXRantagonist. (Z)-Guggulsterone reducesACE2expression andSARS-CoV-2infection[2]. |
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体外研究 (In Vitro) | (Z)-Guggulsterone (10, 20 μM; 24 or 48 hours) causes a decrease in the level of VEGF-R2 protein in HUVEC[1]. (Z)-Guggulsterone (10 μM; 24 h) reduces ACE2 and SHP levels in primary airway and intestinal organoids, and reduces SARS-CoV-2 infection in multiple cell types via FXR-mediated ACE2 regulation[2].
Western Blot Analysis[1] Cell Line: | Vascular endothelial growth factor (VEGF) | Concentration: | 10, 20 μM | Incubation Time: | 24 or 48 hours | Result: | Caused a decrease in the level of VEGF-R2 protein in HUVEC. |
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体内研究 (In Vivo) | Z-guggulsterone (oral; 1 mg; 5 times/week) results in a statistically significantly decrease in tumor volume and wet tumor weight[1].
Animal Model: | Male nude mice (5–6 weeks old) s.c. implanted with DU145 cell-containing Matrigel plugs | Dosage: | 1 mg | Administration: | Oral; 5 times/week | Result: | Resulted in a statistically significantly decrease in tumor volume and wet tumor weight. |
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来源 | - Plants
- Burseraceae
- Commiphora myrrha(Nees) Engl.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 10 mg/mL(32.01 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 3.2005 mL | 16.0026 mL | 32.0051 mL | 5 mM | 0.6401 mL | 3.2005 mL | 6.4010 mL | 10 mM | 0.3201 mL | 1.6003 mL | 3.2005 mL |
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