Dehydrotumulosic acid
(Synonyms: 去氢土莫酸) 目录号 : GC38453
A triterpene with anticancer and anti-inflammatory activities
Cas No.:6754-16-1
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
Dehydrotumulosic acid is a triterpene that has been found in P. cocos and has anticancer and anti-inflammatory activities.1,2 It enhances the cytotoxicity of vincristine against multidrug-resistant KBv200 cells when used at concentrations of 12.5 or 25 ?g/ml.1 Dehydrotumulosic acid (50 mg/kg) reduces serotonin-induced hind paw edema, as well as ear edema induced by phorbol 12-myristate 13-acetate , in mice.2
1.Shan, H., Qinglin, Z., Fengjun, X., et al.Reversal of multidrug resistance of KBV200 cells by triterpenoids isolated from Poria cocosPlanta Med.78(5)428-433(2012) 2.Giner, E.M., Má?ez, S., Recio, M.C., et al.In vivo studies on the anti-inflammatory activity of pachymic and dehydrotumulosic acidsPlanta Med.66(3)221-227(2000)
| Cas No. | 6754-16-1 | SDF | |
| 别名 | 去氢土莫酸 | ||
| Canonical SMILES | C[C@]12[C@@]([C@]([C@H](C(O)=O)CCC(C(C)C)=C)([H])[C@H](O)C1)(CC=C3C2=CC[C@]4([H])[C@@]3(CC[C@H](O)C4(C)C)C)C | ||
| 分子式 | C31H48O4 | 分子量 | 484.71 |
| 溶解度 | DMSO : 33.33 mg/mL (68.76 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| 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 | 2.0631 mL | 10.3154 mL | 20.6309 mL |
| 5 mM | 0.4126 mL | 2.0631 mL | 4.1262 mL |
| 10 mM | 0.2063 mL | 1.0315 mL | 2.0631 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。
The isolation, identification and determination of Dehydrotumulosic acid in Poria cocos
Anal Sci 2002 May;18(5):529-31.PMID:12036119DOI:10.2116/analsci.18.529.
Poria cocos (Fuling), a popular Chinese medicinal (CM) herb of fungal origin, has been included in many combinations with other CM herbs for its traditionally claimed activities of inducing diuresis, excreting dampness, invigorating the spleen and tranquilizing the mind and its modern pharmacological use of modulating the immune system of the body. Dehydrotumulosic acid, one of the effective constituents of Fuling, was isolated from the chloroform-soluble material of ethanol extract of the fungus. After further purification by a high-performance liquid chromatographic method on a C18 column, the purified constituent was identified using modern analytical techniques, such as UV, 13C-NMR and EI-MS. A reversed-phase high-performance liquid chromatographic method has been developed for the determination of Dehydrotumulosic acid in Poria cocos. The determination can be accomplished in less than 50 min using methanol-acetonitrile-2% glacial acetic acid as the mobile phase at a flow rate of 1.0 mL/min, with a UV detector setting at 242 nm and testosterone propionate used as an internal standard. This assay for Dehydrotumulosic acid is simple, rapid and with good reproducibility.
High-performance liquid chromatographic method for the determination and pharmacokinetic study of Dehydrotumulosic acid in the plasma of rats having taken the traditional chinese medicinal preparation Ling-Gui-Zhu-Gan decoction
J Chromatogr B Analyt Technol Biomed Life Sci 2003 May 25;788(2):387-91.PMID:12705979DOI:10.1016/s1570-0232(02)00411-7.
A high-performance liquid chromatographic method for the determination of Dehydrotumulosic acid in plasma of rats having been administrated orally with the traditional Chinese medicinal preparation Ling-Gui-Zhu-Gan decoction was developed. Plasma samples taken from rats were acidified with hydrochloric acid and extracted with ethyl acetate. Separation of the main effective constituent Dehydrotumulosic acid was accomplished on a C(18) stationary phase and a mobile phase of methanol-acetonitrile-2% glacial acetic acid (13:12:10, v/v), with a UV detector setting at 242 nm. After validation, the method was used for preliminary investigation of the pharmacokinetic profiles of Dehydrotumulosic acid administrated in Ling-Gui-Zhu-Gan decoction.
In vivo studies on the anti-inflammatory activity of pachymic and dehydrotumulosic acids
Planta Med 2000 Apr;66(3):221-7.PMID:10821046DOI:10.1055/s-2000-8563.
Pachymic and dehydrotumulosic acids were studied in different models of acute and chronic inflammation. They proved to be active in most of the methods applied. None of them were active against arachidonic acid-induced ear edema. Dehydrotumulosic acid significantly diminished the mouse ear edema induced by ethyl phenylpropiolate, while pachymic acid was ineffective. When the putative corticoid-like mechanism of both compounds was explored, pachymic acid activity was partially abolished by the glucocorticoid receptor antagonist progesterone, but Dehydrotumulosic acid activity was not affected. In vivo experiments demonstrated the inhibition by both principles of the phospholipase A2 (PLA2)-induced extravasation. The previous report on the effects of both compounds in vitro against PLA2, together with the present in vivo results, support the idea that the inhibition of this enzyme probably constitutes their main mechanism of action.
Anti-Hyperglycemic Properties of Crude Extract and Triterpenes from Poria cocos
Evid Based Complement Alternat Med 2011;2011:128402.PMID:20924500DOI:10.1155/2011/128402.
Poria cocos, Bai Fu Ling in Chinese, is used in traditional Chinese medicine to treat diabetes. However, its claimed benefits and mechanism are not fully understood. This study aimed to investigate the effect and action of P. cocos on type 2 diabetes. We first performed phytochemical analysis on the crude extract and factions of P. cocos. P. cocos crude extract at 50 mg/kg body weight or more significantly decreased blood glucose levels in db/db mice. Based on a bioactivity-directed fractionation and isolation (BDFI) strategy, chloroform fraction and subfractions 4 and 6 of the P. cocos crude extract possessed a blood glucose-lowering effect. Dehydrotumulosic acid, dehydrotrametenolic acid, and pachymic acid were identified from the chloroform sub-fractions 4, 3, and 2, respectively. Dehydrotumulosic acid had anti-hyperglycemic effect to a greater extent than dehydrotrametenolic acid and pachymic acid. Mechanistic study on streptozocin- (STZ-) treated mice showed that the crude extract, Dehydrotumulosic acid, dehydrotrametenolic acid, and pachymic acid of P. cocos exhibited different levels of insulin sensitizer activity. However, the P. cocos crude extract and triterpenes appeared not to activate PPAR-γ pathway. Overall, the data suggest that the P. cocos extract and its triterpenes reduce postprandial blood glucose levels in db/db mice via enhanced insulin sensitivity irrespective of PPAR-γ.
Identification of Triterpene Acids in Poria cocos Extract as Bile Acid Uptake Transporter Inhibitors
Drug Metab Dispos 2021 May;49(5):353-360.PMID:33658229DOI:10.1124/dmd.120.000308.
Literature reports that Poria cocos reduces blood lipid levels; however, the underlying mechanism remains unclear. Blood lipid levels are closely related to the enterohepatic circulation of bile acids, where uptake transporters playing a significant role. P. cocos extract is commonly used in traditional prescriptions and food supplements in China. We investigated the effects of P. cocos and its five triterpene acids on bile acid uptake transporters, including intestinal apical sodium-dependent bile acid transporter (ASBT) and hepatic sodium/taurocholate cotransporting polypeptide (NTCP). Triterpene acids were fingerprinted by high-performance liquid chromatography-TripleTOF and quantified by ultraperformance liquid chromatography/tandem mass spectrometry. The inhibitory effect of P. cocos and its five major representative triterpene acids on ASBT and NTCP was investigated by in vitro assays using Xenopus oocytes expressing ASBT and NTCP. P. cocos extract exhibited significant inhibitory effects with half-maximum inhibition constants of 5.89 µg/ml and 14.6 µg/ml for NTCP and ASBT, respectively. Among five triterpene acids, poricoic acid A, poricoic acid B, and polyporenic acid C significantly inhibited NTCP function. Poricoic acid A, poricoic acid B, and Dehydrotumulosic acid significantly inhibited ASBT function. The representative triterpene acid, poricoic acid A, was identified as a competitive inhibitor of NTCP with an inhibitory constant of 63.4 ± 18.7 µM. In conclusion, our results indicate that both P. cocos extract and its major triterpenes are competitive inhibitors of ASBT and NTCP. Accordingly, it was suggested that competitive inhibition of these bile acid transporters is one of the underlying mechanisms for the hypolipidemic effect of P. cocos. SIGNIFICANCE STATEMENT: Poria cocos, a commonly used Chinese herbal medicine and food supplement, demonstrates significantly inhibitory effects on the function of apical sodium-dependent bile acid transporter and sodium/taurocholate cotransporting polypeptide. P. cocos has potential to reduce the blood lipid through inhibition of these uptake transporters in enterohepatic circulation of bile acid.