| 體外活性 | Anticancer agent 42 (compound 10d) (0-20 μM, 4 h) exhibits a potent antitumor activity against MDA-MB-231 cells [1]. Anticancer agent 42 (10 μM, 24 h) induces G2 and S phase arrest in MDA-MB-231 cells [1]. Anticancer agent 42 (10 μM, 24 h) induces cell apoptosis by regulating the expression of apoptosis related proteins in MDA-MB-231 cells [1]. Anticancer agent 42 (0-1 μM) depolarizes mitochondrial membrane and decreases the mitochondrial membrane potential leading to apoptosis [1]. Anticancer agent 42 (0-1 μM, 24 h) induces the cells to produce a large amount of ROS [1]. Cell Viability Assay Cell Line: A549, MDA-MB-231, HeLa [1] Concentration: 0-20 μM Incubation Time: 4 h Result: Exhibited a potent activity against MDA-MB-231 with an IC 50 of 0.07 μM. Cell Cycle Analysis Cell Line: MDA-MB-231 cells [1] Concentration: 10 μM Incubation Time: 24 h Result: Induced G2 and S phase arrest in MDA-MB-231 cells; caused the percentage of MDA-MB-231 cells in G1 phase to decrease significantly (from 74.44% to 16.48%), cells in G1 phase to increase (from 16.61% to 28.47%), and in G2 phase to significantly increase (from 8.95% to 55.05%). Apoptosis Analysis Cell Line: MDA-MB-231 cells [1] Concentration: 10 μM Incubation Time: 24 h Result: Induced cell apoptosis, with apoptotic rate of 31.69%. Western Blot Analysis Cell Line: MDA-MB-231 cells [1] Concentration: 100 nM Incubation Time: 48 h Result: Increased the level of human apoptosis-related proteins (pro-caspase 3, catalase, HTRA2/Omi and p53) in MDA-MB-231 cell. Western Blot Analysis Cell Line: MDA-MB-231 cells [1] Concentration: 0, 0.035, 0.07, 0.14, 0.21 μM Incubation Time: 24 h Result: Increased caspase 9, caspase3, cytochrome C and Bax expression, but decreased Bal-2 expression with increasing concentration. |
| 體內(nèi)活性 | Anticancer agent 42 (compound 10d) (Kunming mice, 5000 mg/kg, Intragastric administration, once) has extremely low oral toxicity [1]. Anticancer agent 42 (Kunming mice, 238-600 mg/kg, IP, once) shows no obvious liver and kidney damage to mice, with an LD 50 of 374 mg/kg [1]. Anticancer agent 42 (Kunming mice, 25 mg/kg, IP, once every two days) causes mild liver and kidney damage [1]. Anticancer agent 42 (BALB/c mice, suppresses breast cancer 4T1 tumor growth, the anti-tumor effect is better combined use with CA (Cyanoacrylates), and can cross through the skin to achieve anti-tumor effects. [1]. Animal Model: Kunming mice (n=10, 5 male and 5 female) [1] Dosage: 5000 mg/kg Administration: Intragastric administration, once Result: Had extremely low oral toxicity, did not cause death in mice at 5000 mg/kg. Animal Model: Kunming mice [1] Dosage: 600, 476, 378, 300, 238 mg/kg Administration: IP, once Result: Showed no obvious liver and kidney damage to mice, with an LD 50 of 374 mg/kg. Animal Model: Kunming mice (n=3) [1] Dosage: 25 mg/kg Administration: IP, once every two days Result: Caused mild liver and kidney damage after administration, slightly increased ALT, AST and BUN of mice. Animal Model: BALB/c mice (4T1 tumor-bearing, female, eight groups, 6 mice per group) [1] Dosage: 10d (50 mg/kg) + CA; 10d (50 mg/kg) + saline; 10d (200 mg/kg) + CA Administration: Intratumoral injection, every four days (50 mg/kg); smear, every two days (200 mg/kg), for 14 days. Result: Showed obvious antitumor effect from the 8th day; had protective effects on the spleens of tumor-bearing mice; the anti-tumor effect is better when combined use with CA; can cross through the skin to achieve anti-tumor effects. |