Timosaponin AIII 可抑制乙酰胆碱酯酶（AChE）的活性，其IC50值为 35.4μM。
Cas No.:41059-79-4
Sample solution is provided at 25 µL, 10mM.
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Timosaponin AIII inhibits the activity of acetylcholinesterase (AChE), with IC50 value of 35.4μM[1]. Timosaponin AIII is a bioactive steroid saponin isolated from A. asphodeloides. Timosaponin AIII has shown multiple pharmacological activities and has been developed as an anticancer agent[2].
In vitro，Timosaponin AIII presented cytotoxicity effects in various kinds of cancer cells including breast cancer, hepatocellular cancer, cervical cancer, colon cancer, and so on. Timosaponin AIII inhibited cell viability of BT474, MDA-MB-231, HepG2, HeLa, HCT-116 with IC50s of 2.5µM, 2µM, 15.41µM, 10µM, 5.5µM, respectively[3-6].
In vivo, treatment with Timosaponin AIII (7.5mg/kg; i.p.; 3 times per week for 3 weeks) dramatically restricted tumor growth in MHCC97L tumor bearing nude mice[7]. Oral administration of free Timosaponin AIII (6.8 mg/kg) in healthy male SD rats, the Cmax, Tmax, AUC0-t, and T1/2 of Timosaponin-AIII were 18.2±3.1ng/mL, 2.3±0.57h, 150.5±29. ng·h/mL, and 4.9±2.0h, respectively[8].
References:
[1] Lee, Bomi, Kangsik Jung, and Dong-Hyun Kim. "Timosaponin AIII, a saponin isolated from Anemarrhena asphodeloides, ameliorates learning and memory deficits in mice." Pharmacology Biochemistry and Behavior 93.2 (2009): 121-127.
[2] Liu, Zhaowen, et al. "The potential role of timosaponin-AIII in cancer prevention and treatment." Molecules 28.14 (2023): 5500.
[3] Kang, You-Jin, et al. "Cytotoxic and antineoplastic activity of timosaponin A-III for human colon cancer cells." Journal of natural products 74.4 (2011): 701-706.
[4] Gergely, Joseph E., et al. "Timosaponin A‐III inhibits oncogenic phenotype via regulation of PcG protein BMI1 in breast cancer cells." Molecular carcinogenesis 57.7 (2018): 831-841.
[5] Nho, Kyoung Jin, Jin Mi Chun, and Ho Kyoung Kim. "Induction of mitochondria-dependent apoptosis in HepG2 human hepatocellular carcinoma cells by timosaponin A-III." Environmental toxicology and pharmacology 45 (2016): 295-301.
[6] Sy, Lai-King, et al. "Timosaponin A-III induces autophagy preceding mitochondria-mediated apoptosis in HeLa cancer cells." Cancer research 68.24 (2008): 10229-10237.
[7] Wang, Ning, et al. "A novel mechanism of XIAP degradation induced by timosaponin AIII in hepatocellular carcinoma." Biochimica et Biophysica Acta (BBA)-Molecular Cell Research 1833.12 (2013): 2890-2899.
[8] Liu, Zhirui, et al. "Comparative pharmacokinetics of timosaponin B-II and timosaponin A-III after oral administration of Zhimu–Baihe herb-pair, Zhimu extract, free timosaponin B-II and free timosaponin A-III to rats." Journal of Chromatography B 926 (2013): 28-35.
Timosaponin AIII可抑制乙酰胆碱酯酶（AChE）的活性，其IC50值为 35.4μM[1]。Timosaponin AIII是从水百合属植物A. asphodeloides中分离出的一种具有生物活性的甾体皂苷。Timosaponin AIII已显示出多种药理活性，并被开发为一种抗癌药物[2]。
在体外实验中，Timosaponin AIII对乳腺癌、肝细胞癌、宫颈癌、结肠癌等多种癌症细胞均表现出细胞毒性作用。Timosaponin AIII抑制了BT474、MDA-MB-231、HepG2、HeLa、HCT-116等细胞的细胞活力，其IC50值分别为2.5μM、2μM、15.41μM、10μM、5.5μM[3-6]。
在体内实验中，用Timosaponin AIII（7.5mg/kg；腹腔注射；每周3次，共3周）治疗MHCC97L荷肿瘤的裸鼠，显著抑制了肿瘤生长[7]。在健康雄性SD大鼠中口服游离的Timosaponin AIII（6.8mg/kg），其Cmax、Tmax、AUC0-t和T1/2分别为18.2±3.1ng/mL、2.3±0.57h、150.5±29. ng·h/mL和4.9±2.0h[8]。
| Cell experiment [1]: | |
Cell lines | HeLa |
Preparation Method | Cells (8×103 per well) were seeded in supplemented culture medium (100μL/well) in 96-well plates and incubated for 24h. Then the medium was replaced with a Timosaponin AIII-containing medium, and the cells were further incubated for 24 to 48h. All experiments were run in parallel with controls (0.2% DMSO) and the cell viabilities were evaluated by MTT assays. |
Reaction Conditions | 0-20µM; 24 to 48h |
Applications | Timosaponin AIII inhibited HeLa cell viability in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female nude mice |
Preparation Method | Female nude mice subcutaneously received 1×107 MHCC97L cells on its right flank. One week after injection, mice were randomized into two groups. One of which received 7.5mg/kg Timosaponin AIII three times per week through intraperitoneal injection for 3 weeks while the other received PBS. Tumor growth and body weight were monitored three times per week. At the end of the study, the mice were sacrificed with overdose of phenobarbital (200mg/kg). Tumor was dissected out and subjected to histological analysis. |
Dosage form | 7.5mg/kg; i.p.; 3 times per week for 3 weeks |
Applications | In tumor bearing nude mice treated with Timosaponin AIII (7.5mg/kg/2 days) while tumor growth was dramatically restricted. |
References: | |
| Cas No. | 41059-79-4 | SDF | |
| 别名 | 知母皂苷A-III,Xilingsaponin A; Zhi-mu saponin | ||
| 化学名 | Xilingsaponin A; Zhi-mu saponin | ||
| Canonical SMILES | O[C@@H]1[C@@H]([C@@H](O[C@H](CO)[C@@H]1O)O[C@H]2C[C@H]3[C@@](CC2)(C)[C@H]4[C@H](CC3)[C@@H](C5)[C@@](CC4)(C)[C@H]([C@H]6C)[C@@H]5O[C@]76OC[C@@H](C)CC7)O[C@@H]([C@@H]([C@H]8O)O)O[C@H](CO)[C@H]8O | ||
| 分子式 | C39H64O13 | 分子量 | 740.43 |
| 溶解度 | ≥ 27.2mg/mL in DMSO | 储存条件 | Store at 2-8°C,protect from light |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3506 mL | 6.7528 mL | 13.5057 mL |
| 5 mM | 270.1 μL | 1.3506 mL | 2.7011 mL |
| 10 mM | 135.1 μL | 675.3 μL | 1.3506 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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