Echitamine chloride
(Synonyms: 氯化埃奇胺) 目录号 : GC63871
Echitamine chloride 是存在于 Alstonia 中的主要单萜吲哚生物碱，具有有效的抗肿瘤活性。Echitamine chloride 会诱导 DNA 片段化和细胞凋亡 (apoptosis)。Echitamine chloride 抑制胰腺脂肪酶 (pancreatic lipase)，IC50 为 10.92 µM。
Cas No.:6878-36-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Echitamine chloride is the major monoterpene indole alkaloid present in Alstonia with potent anti-tumour activity. Echitamine chloride induces DNA fragmentation and cells apoptosis. Echitamine chloride inhibits pancreatic lipase with an IC50 of 10.92 µM[1][2].
[1]. Ganesh Chandra Jagetia, et al. Evaluation of the Cytotoxic Effect of the Monoterpene Indole Alkaloid Echitamine In-Vitro and in Tumour-Bearing Mice. J Pharm Pharmacol. 2005 Sep;57(9):1213-9.
[2]. Ginson George, et al. Development and Validation of a New HPTLC-HRMS Method for the Quantification of a Potent Pancreatic Lipase Inhibitory Lead Echitamine From Alstonia scholaris. Nat Prod Res. 2019 Dec 24;1-5.
| Cas No. | 6878-36-0 | SDF | Download SDF |
| 别名 | 氯化埃奇胺 | ||
| 分子式 | C22H29ClN2O4 | 分子量 | 420.93 |
| 溶解度 | 储存条件 | 4°C, protect from light | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3757 mL | 11.8785 mL | 23.7569 mL |
| 5 mM | 0.4751 mL | 2.3757 mL | 4.7514 mL |
| 10 mM | 0.2376 mL | 1.1878 mL | 2.3757 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Inhibition of glycolysis and respiration of sarcoma-180 cells by Echitamine chloride
Chemotherapy 1998 May-Jun;44(3):198-205.PMID:9612610DOI:10.1159/000007115.
Malignant tumors are known to exhibit high rates of glycolytic activity leading to high production of lactic acid. Hence, neoplastic cells have elevated activity of enzymes responsible for glycolysis. Echitamine chloride, an indole alkaloid extracted from the bark of Alstonia scholaris, has been reported to have a highly promising anticancer activity against fibrosarcoma in rats. In the present study, the effect of Echitamine chloride on energy metabolism of S-180 cells is investigated to have a better understanding on the mode of action of Echitamine chloride. The effect of Echitamine chloride on the mitochondrial and cellular respiration of S-180 cells was studied. Also, the effects on glucose utilization, pyruvate utilization and lactate formation were studied on whole S-180 cells and S-180 cell-free homogenate. The levels of glycolytic enzymes such as hexokinase and lactate dehydrogenase were estimated in which particular emphasis has been laid on hexokinase which occurs both in cytosolic and particulate forms in neoplastic cells. Hence the differential effect of Echitamine chloride on the levels of total, cytosolic and particulate hexokinase has been investigated. In conclusion, Echitamine chloride affects both cellular and mitochondrial respiration, leading to reduction of the cellular energy pool and thereby resulting in the loss of viability of S-180 cells.
Antitumor effect of Echitamine chloride on methylcholonthrene induced fibrosarcoma in rats
Biochem Int 1991 Oct;25(3):491-8.PMID:1805793doi
Echitamine chloride a plant alkaloid from Alstonia scholaris has been used to examine the anticancer effects on methylcholanthrene-induced fibrosarcoma. Echitamine chloride dissolved in saline (10 mg/kg body weight) and injected subcutaneously for 20 days in fibrosarcoma rats has exhibited significant regression in tumor growth. The altered activities of plasma and liver transaminases and gamma-glutamyl transpeptidase and lipid peroxidation in fibrosarcoma have been corrected to near normal after Echitamine chloride treatment. The decreased liver glutathione content and the lowered activities of glutathione peroxidase, superoxide dismutase and catalase have also been reversed to near normals after Echitamine chloride treatment.
Evaluation of the cytotoxic effect of the monoterpene indole alkaloid echitamine in-vitro and in tumour-bearing mice
J Pharm Pharmacol 2005 Sep;57(9):1213-9.PMID:16105243DOI:10.1211/jpp.57.9.0017.
The cytotoxic effect of various concentrations of Echitamine chloride was studied in HeLa, HepG2, HL60, KB and MCF-7 cell lines in-vitro and in mice bearing Ehrlich ascites carcinoma (EAC). Exposure of various cells to different concentrations of Echitamine chloride resulted in a concentration-dependent cell killing, and KB cells were found to be most sensitive amongst all the cells evaluated. EAC mice treated with 1, 2, 4, 6, 8, 12 or 16 mg kg-1 Echitamine chloride showed a dose-dependent elevation in the anti-tumour activity, as evident by increased number of survivors in comparison with the non-drug treated controls. The highest dose of Echitamine chloride (16 mg kg-1) caused toxicity in the recipient mice, therefore 12 mg kg-1 was considered the best cytotoxic dose for its anti-tumour effect. Administration of 12 mg kg-1 Echitamine chloride resulted in an increase in the median survival time (MST) up to 30.5 days, which was 11.5 days higher than the non-drug treated control (19 days). Administration of 16 mg kg-1 Echitamine chloride to EAC mice resulted in a time dependent elevation in lipid peroxidation that reached a peak at 6 h post-treatment, whereas glutathione concentration declined in a time dependent manner and a maximum decline was reported at 3 h post-treatment. Our study demonstrated that Echitamine chloride possessed anti-tumour activity in-vitro and in-vivo.
Modulation of the impaired drug metabolism in sarcoma-180-bearing mice by Echitamine chloride
Cancer Biochem Biophys 1999 Jul;17(1-2):79-88.PMID:10738904doi
Echitamine chloride (EC), an indole alkaloid, extracted from the bark of Alstonia scholaris has got highly promising anticancer effect. The effect of this drug on the microsomal drug detoxifying system was studied in sarcoma-180 induced mice. When given sub-cutaneously at a dosage of 5 mg/kg body weight, it was able to alter the impaired drug detoxifying system which was observed in the Sarcoma-180 bearing mice. The levels of microsomal protein, Cyt-P450, Cyt-b5, NADH-Cyt-C-reductase, NADPH-Cyt-C-reductase, and glu-6 phosphatase were determined. The levels of these drug metabolizing enzymes were decreased in S-180 bearing mice. EC treatment corrected to near normal levels of these enzymes and microsomal hemeproteins. In order to understand the mechanism responsible for the decreased protein level and its normalization after treatment with EC, 3H-Phenylalanine incorporation study was carried out. From the results, it is observed that the synthesis of apoproteins is also altered in tumor-bearing animals. All these changes which were observed in tumor-bearing animals were corrected to near normal levels after treatment with EC.
The effect of seasonal variation on the antineoplastic activity of Alstonia scholaris R. Br. in HeLa cells
J Ethnopharmacol 2005 Jan 4;96(1-2):37-42.PMID:15588648DOI:10.1016/j.jep.2004.07.024.
In order to evaluate the seasonal variation as well as cytotoxicity of different fractions of Alstonia scholaris R. Br. (ASE), the HeLa cells were treated with different doses of various fractions of ASE collected in monsoon, winter and summer. The exposure of HeLa cells to different extracts prepared from the stem bark collected in monsoon, winter and summer seasons resulted in a dose dependent increase in the cell killing effect of ASE and the highest cell killing effect was observed for the extract prepared from the summer collections. Similarly, treatment of HeLa cells with different doses of various fractions of the Alstonia scholaris extract viz. residue (ASERS), steroidal (ASEST), chloroform (ASECH), petroleum ether (ASEPE), diethyl ether (ASEDE), ethyl acetate (ASEEA), n-butanol (ASENB), aqueous (ASEAQ) and Echitamine chloride (ECL) also resulted in a dose dependent decline in the cell viability, where the greatest cytotoxic effect was observed for residue (ASERS), followed by the whole extract (ASE) and chloroform (ASECH) fraction, while the least activity was observed for the steroidal (ASEST) fraction. The cytotoxicity declined ASERS > ASE > ASECH >ECL > ASEEA > ASEDE > ASEPE > ASENB > ASEAQ > ASEST in order. Our study demonstrates that the extract prepared from the summer collection, and the fractions containing the alkaloids were highly effective in cell killing. The extract of ASE was more powerful than the active principle echitamine present in ASE.