Cleistanthin B
(Synonyms: 山荷叶素O-葡萄糖苷,Diphyllin O-glucoside) 目录号 : GC64264
Cleistanthin B (Diphyllin O-glucoside) 是一种具有口服活性的芳基萘木酚素内酯糖苷。Cleistanthin B 在 Vero 细胞中表现出抗 SARS-CoV-2 作用，EC50 值为 6.51 µM。Cleistanthin B 在体内具有抗肿瘤、利尿和抗高血压的作用。
Cas No.:30021-77-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cleistanthin B (Diphyllin O-glucoside) is an orally active arylnaphthalene lignan lactone glycoside. Cleistanthin B exhibits anti-SARS-CoV-2 effects in Vero cells, with EC50 of 6.51 µM. Cleistanthin B also exhibits antitumor, diuretic and antihypertensive effects in vivo[1][2][3][4].
Cleistanthin B exhibits anti-SARS-CoV-2 effects in Vero cells, with EC50 of 6.51 µM[1].Cleistanthin B shows no cytotoxic to Vero cells in concentrations up to 100 µM[1].
Cleistanthin B (25-100 mg/kg; p.o. for 10 dys) has antitumor activity against EAC and DAL tumor mice but it is not effective against solid tumor[2].
[1]. Stefanik M, et, al. Antiviral Activity of Vacuolar ATPase Blocker Diphyllin against SARS-CoV-2. Microorganisms. 2021 Feb 25;9(3):471.
[2]. Thummar VR, et, al. Evaluation of in vivo antitumor activity of cleistanthin B in Swiss albino mice. J Tradit Complement Med. 2015 Sep 3;6(4):383-388.
[3]. Parasuraman S, et, al. Diuretic effects of cleistanthin a and cleistanthin B from the leaves of cleistanthus collinus in wistar rats. J Young Pharm. 2012 Apr;4(2):73-7.
[4]. Priyadharsini RP, et, al. Evaluation of the antihypertensive activity and alpha adrenergic receptor interaction of cleistanthins A and B. J Basic Clin Pharm. 2014 Sep;5(4):109-14.
| Cas No. | 30021-77-3 | SDF | Download SDF |
| 别名 | 山荷叶素O-葡萄糖苷,Diphyllin O-glucoside | ||
| 分子式 | C27H26O12 | 分子量 | 542.49 |
| 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 | 1.8434 mL | 9.2168 mL | 18.4335 mL |
| 5 mM | 0.3687 mL | 1.8434 mL | 3.6867 mL |
| 10 mM | 0.1843 mL | 0.9217 mL | 1.8434 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。
Diuretic effects of cleistanthin a and Cleistanthin B from the leaves of cleistanthus collinus in wistar rats
J Young Pharm 2012 Apr;4(2):73-7.PMID:22754257DOI:10.4103/0975-1483.96616.
To study the diuretic effects of cleistanthin A and Cleistanthin B, phytoconstituents were isolated from the leaves of Cleistanthus collinus in Wistar rats. The in vivo diuretic effects of cleistanthins A and B were determined according to the Lipschitz test. Prior to the experiment, the animals were fasted for 5 h and placed individually in metabolic cages. Cleistanthins A and B (12.5, 25, and 50 mg/kg) and furosemide (5 mg/kg) were suspended in 0.5% w/v carboxymethyl cellulose and administered orally. The urine was collected up to 5 h after administration and subsequently up to 24 h after administration. The acidity and urine volume were measured immediately. The urinary sodium and potassium levels were determined using a flame photometer, and the chloride level was determined by argentometric titration. The diuretic index and diuretic activity were calculated mathematically. While cleistanthins A and B showed a diuretic index of more than one, the diuretic activity of these compounds was less than one, indicating inferior activity compared with furosemide. Both cleistanthin A and B produced a significant increase in the urine volume and alterations in urinary electrolyte levels. However, the effect of the compounds was not dose dependent. Cleistanthin A and Cleistanthin B exert diuretic effects in male Wistar rats without affecting the urinary acidity.
Cleistanthin B causes G1 arrest and induces apoptosis in mammalian cells
Apoptosis 1998 Dec;3(6):413-9.PMID:14646474DOI:10.1023/a:1009658518998.
Cleistanthin B is a potential anticancer agent isolated from the tropical plant Cleistanthus collinus. We have previously shown that Cleistanthin B is clastogenic and induces micronuclei formation and chromosomal aberrations. We now show that this compound inhibits DNA synthesis in Chinese hamster ovary (CHO) cells and induces apoptosis in cervical carcinoma (SiHa) cells. Flow cytometric analysis of cleistanthin treated CHO cells revealed that they were blocked in G1. Cervical carcinoma (SiHa) cells exposed to Cleistanthin B shrank, rounded up and had condensed chromatin and fragmented nuclei. DNA isolated from cleistanthin treated cells exhibited the characteristic apoptotic ladder when electrophoresed in agarose gels. These results were confirmed by flow cytometry. Etoposide, a structurally similar compound also induced apoptosis in these cells although with a difference. Etoposide induced apoptosis after permitting cells to enter into S phase, while Cleistanthin B stopped entry of cells into S phase and subsequently drove them to apoptosis.
Biodistribution properties of cleistanthin A and Cleistanthin B using magnetic resonance imaging in a normal and tumoric animal model
Pharmacogn Mag 2012 Apr;8(30):129-34.PMID:22701286DOI:10.4103/0973-1296.96559.
Aim: To determine the biodistribution properties of cleistanthin A and Cleistanthin B in rodents using magnetic resonance imaging (MRI). Materials and methods: Cleistanthins A and B, constituents of Cleistanthus collinus Roxb., were labelled with gadolinium (Gd(3+)) directly and injected into normal and tumoric nude mice. The tissue signal intensity was measured using MRI to perform a noninvasive kinetic assay. Wistar rats were used for determination of the grayscale intensity to observe the distribution patterns of of cleistanthins A and B. Results: Cleistanthin A is kinetically more attractive to the gastrointestinal tract than is Cleistanthin B, which gets accumulated in muscular tissues of mice in greater concentrations compared with cleistanthin A. Cleistanthin B but not cleistanthin A showed tumoric affinity and exhibited a tumor kinetic attraction in tumoric mice. In rats, cleistanthin A showed greater grayscale intensities in the brain, liver, and skeletal muscles in immediate post contrast MRI images, whereas the gadolinium tagged Cleistanthin B showed higher grayscale intensities in the cardiac muscle and skeletal muscles in delayed post contrast MRI images. Conclusions: Cleistanthin A is more pharmacokinetically attractive to the gastrointestinal tract than Cleistanthin B.
Sub-chronic toxicological evaluation of cleistanthin A and Cleistanthin B from the leaves of Cleistanthus collinus (Roxb.)
Toxicol Rep 2014 Aug 19;1:596-611.PMID:28962273DOI:10.1016/j.toxrep.2014.08.006.
Objective: To investigate the toxicological effects of cleistanthin A and Cleistanthin B using sub-chronic toxicity testing in rodents. Method: Cleistanthins A and B were isolated from the leaves of Cleistanthus collinus. Both the compounds were administered orally for 90 days at the concentration of 12.5, 25 and 50 mg/kg, and the effects on blood pressure, biochemical parameters and histology were assessed. The dose for sub-chronic toxicology was determined by fixed dose method according to OECD guidelines. Result: Sub-chronic toxicity study of cleistanthins A and B spanning over 90 days at the dose levels of 12.5, 25 and 50 mg/kg (once daily, per oral) revealed a significant dose dependant toxic effect in lungs. The compounds did not have any effect on the growth of the rats. The food and water intake of the animals were also not affected by both cleistanthins A and B. Both the compounds did not have any significant effect on liver and renal markers. The histopathological analysis of both cleistanthins A and B showed dose dependent morphological changes in the brain, heart, lung, liver and kidney. When compared to cleistanthin A, Cleistanthin B had more toxic effect in Wistar rats. Both the compounds have produced a dose dependent increase of corpora amylacea in brain and induced acute tubular necrosis in kidneys. In addition, Cleistanthin B caused spotty necrosis of liver in higher doses. Conclusion: The present study concludes that both cleistanthin A and Cleistanthin B exert severe toxic effects on lungs, brain, liver, heart and kidneys. They do not cause any significant pathological change in the reproductive system; neither do they induce neurodegenerative changes in brain. When compared to cleistanthin A, Cleistanthin B is more toxic in rats.
Evaluation of in vivo antitumor activity of Cleistanthin B in Swiss albino mice
J Tradit Complement Med 2015 Sep 3;6(4):383-388.PMID:27774423DOI:10.1016/j.jtcme.2015.08.004.
To evaluate the in vivo antitumor activity of Cleistanthin B in Ehrlich's ascites carcinoma (EAC) and Dalton's ascites lymphoma (DAL) cell lines induced malignant ascites mouse models and DAL cell line induced solid tumor mouse model. All animals were injected with 2 × 106 EAC/DAL cells i.p./s.c. to induce malignant ascites and solid tumor and treated with 5-fluorouracil (5-FU) 20 mg/kg or Cleistanthin B for 10 days. Cleistanthin B was given at three doses viz. 25, 50 and 100 mg/kg. The percentage increase in life span and the overall survival in malignant ascites animals and the tumor volume in solid tumor animals were measured. The haematological parameters were assessed in all animals before and 2 weeks after the treatment. Cleistanthin B 50 mg/kg and 5-FU significantly prolonged the life span (>25%) of malignant ascites tumor bearing animals. The overall survival was significantly improved by both. Only Cleistanthin B 50 mg/kg significantly reduced the elevated WBC counts in EAC tumor bearing animals. Both 5-FU and Cleistanthin B 50 mg/kg reversed the malignancy induced increase in neutrophils and platelet counts and decrease in lymphocyte counts but not to the normal range. Only 5-FU significantly reduced the solid tumor volume. None of the three doses of Cleistanthin B was effective against the solid tumor. Cleistanthin B has antitumor activity against EAC and DAL tumor mice but it is not as effective as 5-FU. At 50 mg/kg dose Cleistanthin B exerts significant antitumor activity compared to 25 and 100 mg/kg dose. Its effect on WBC count is higher and advantageous when compared to 5-FU. But Cleistanthin B in the doses used is not effective against solid tumor.