Saikogenin D
(Synonyms: 皂苷元 D) 目录号 : GC39053
Saikogenin D 分离自 Bupleurum chinense ，具有抗炎作用。Saikogenin D 激活环氧合酶，将花生四烯酸转化为环氧二十烷酸和二羟基二十碳三烯酸，其代谢产物继而抑制前列腺素E2 (PGE2) 的产生。 由于细胞内 Ca2+ 的释放，Saikogenin D 导致 [Ca2+]i 升高。
Cas No.:5573-16-0
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
Saikogenin D is isolated from Bupleurum chinense, has anti-inflammatory effects. Saikogenin D activates epoxygenases that converts arachidonic acid to epoxyeicosanoids and dihydroxyeicosatrienoic acids, and the metabolites secondarily inhibit prostaglandin E2 (PGE2) production. Saikogenin D results in an elevation of [Ca2+]i due to Ca2+ release from intracellular stores[1][2].
[1]. Toriniwa Y, et al. Participation of epoxygenase activation in saikogenin D-induced inhibition of prostaglandin E(2) synthesis.J Pharm Pharmacol. 2006 Jun;58(6):859-66. [2]. Kodama Y, et al. Dual effect of saikogenin D: in vitro inhibition of prostaglandin E2 production and elevation of intracellular free Ca2+ concentration in C6 rat glioma cells.Planta Med. 2003 Aug;69(8):765-7.
| Cas No. | 5573-16-0 | SDF | |
| 别名 | 皂苷元 D | ||
| Canonical SMILES | C[C@]12[C@]3(C(C=C[C@]1([H])[C@@]4([C@@]([C@@](C)([C@@H](O)CC4)CO)([H])CC2)C)=C5[C@](CO)(CCC(C)(C)C5)[C@H](O)C3)C | ||
| 分子式 | C30H48O4 | 分子量 | 472.7 |
| 溶解度 | Soluble in DMSO | 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 | 2.1155 mL | 10.5775 mL | 21.1551 mL |
| 5 mM | 0.4231 mL | 2.1155 mL | 4.231 mL |
| 10 mM | 0.2116 mL | 1.0578 mL | 2.1155 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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。
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Protective effect of saikosaponin A, saikosaponin D and Saikogenin D against Pseudomonas aeruginosa infection in mice
Int J Immunopharmacol 1990;12(5):531-7.PMID:2210914DOI:10.1016/0192-0561(90)90117-6.
Effects of saikosaponins and their genins on nonspecific resistance against Pseudomonas aeruginosa and Listeria monocytogenes infections were investigated. When mice were administered intraperitoneally (i.p.) saikosaponins one day before i.p. infection with P. aeruginosa, saikosaponins a and d induced a marked enhancement of nonspecific resistance at a dose of 10 micrograms/mouse. Also, Saikogenin D, a secondary metabolite of saikosaponin d, showed an enhancing effect. The most effective condition for enhancing the nonspecific resistance was i.p. administration of saikosaponin d one day before i.p. or intravenous (i.v.) infection with P. aeruginosa, when mice were treated i.p., i.v., or subcutaneously with saikosaponin d 1, 4 or 7 days previously. Effect of saikosaponin d was weaker than that of formalin-killed bacilli of Propionibacterium acnes and lipopolysaccharide. On the other hand, effect of saikosaponin d on enhancement of nonspecific resistance against L. monocytogenes was not seen. Effector cells participating in the enhanced protection induced by saikosaponin d may be macrophages, since macrophages were a major component in peritoneal cells obtained from mice administered i.p. saikosaponin d 1 day earlier and intracellular bactericidal activity of peritoneal macrophages against P. aeruginosa increased.
Participation of epoxygenase activation in saikogenin D-induced inhibition of prostaglandin E(2) synthesis
J Pharm Pharmacol 2006 Jun;58(6):859-66.PMID:16734988DOI:10.1211/jpp.58.6.0017.
We examined the effect of Saikogenin D on arachidonic acid metabolism in C6 rat glioma cells to clarify its anti-inflammatory mechanism. Incubation of C6 cells with Saikogenin D for 20 min resulted in the inhibition of prostaglandin E(2) production and the accumulation of an arachidonic acid metabolite that was found to be 11,12-dihydroxyeicosatrienoic acid, a metabolite of 11,12-epoxyeicosatrienoic acid. C6 cells expressed rat epoxygenase mRNAs, CYP1A1, CYP2B1 and CYP2J3, which converted arachidonic acid to epoxyeicosatrienoic acids. 11,12-Epoxyeicosatrienoic acid inhibited A23187-induced prostaglandin E(2) production and SKF-525A, an inhibitor of epoxygenase, attenuated the saikogenin D-induced inhibition of prostaglandin E(2) production in C6 cells. Furthermore, 11,12-epoxyeicosatrienoic acid and 11,12-dihydroxyeicosatrienoic acid, but not Saikogenin D, inhibited the activity of cyclooxygenase in a cell-free condition. These data suggest that Saikogenin D activates epoxygenases that rapidly convert arachidonic acid to epoxyeicosanoids and dihydroxyeicosatrienoic acids, and then the metabolites secondarily inhibit prostaglandin E(2) production.
Dual effect of Saikogenin D: in vitro inhibition of prostaglandin E2 production and elevation of intracellular free Ca2+ concentration in C6 rat glioma cells
Planta Med 2003 Aug;69(8):765-7.PMID:14531029DOI:10.1055/s-2003-42795.
To clarify the pharmacological profile of Saikogenin D, we examined the effect of Saikogenin D on prostaglandin E2 (PGE2) production and intracellular free Ca2+ concentration ([Ca2+]i) in C6 rat glioma cells. Saikogenin D (1-20 microM) inhibited PGE2 production induced by the Ca2+ ionophore A23187 in a concentration-dependent manner with the IC50 of about 3 microM. Saikogenin D did not affect the conversion of arachidonic acid into PGE2 in microsomal preparations. On the other hand, Saikogenin D elevated [Ca2+]i in a concentration-dependent manner (10-100 microM) with the EC50 value of about 35 microM in the presence or absence of extracellular Ca2+. These results suggest that Saikogenin D possesses a dual effect: an inhibition of A23187-induced PGE2 production without a direct inhibition of cyclooxygenase activity; and an elevation of [Ca2+]i that is attributed to Ca2+ release from intracellular stores.
Activation of murine peritoneal macrophages by saikosaponin a, saikosaponin d and Saikogenin D
Int J Immunopharmacol 1989;11(1):21-8.PMID:2707937DOI:10.1016/0192-0561(89)90095-7.
Macrophage activation by saikosaponins and saikogenins was investigated and compared with that by other saponins and macrophage stimulants. Saikosaponins a and d induced a marked cell accumulation in the peritoneal cavity when administered intraperitoneally. Among saikosaponins and saikogenins tested, saikosaponin d significantly activated peritoneal macrophages in terms of enhancement of phagocytic activity, increased level of cellular lysosomal enzyme (acid phosphatase), induction of cytostatic activity and expression of Ia antigen on the cell surface. The activities of saikosaponin d were much stronger than those of typical saponins ginsenoside Rg1 and glycyrrhizin and almost comparable with or somewhat weaker than those of lipopolysaccharide, a streptococcal preparation OK-432 and formalin-killed Propionibacterium acnes, indicating that saikosaponin d is a potent macrophage activator.
A new saikogenin from the roots of Bupleurum bicaule
Chin J Nat Med 2014 Apr;12(4):305-8.PMID:24863358DOI:10.1016/S1875-5364(14)60060-1.
Aim: To study the chemical constituents from the roots of Buleurum bicaule Helm (Apiaceae). Method: Silica gel, Sephadex LH-20, MPLC Rp-C18 column chromatography, and HPLC were used for isolation of compounds. The structures were elucidated on the basis of 1D- and 2D-NMR technology and HRESI-MS. Compounds were evaluated in vitro for their inhibitory ability against the proliferation of rat mesangial cells by the MTT method. Results: Twelve compounds were isolated, and their structures were identified on the basis of their spectroscopic and physico-chemical properties as 13, 28-epoxy-olean-11-en-3-one (1), saikogenin E (2), saikogenin G (3), 11α-methoxy-3β, 16β, 23, 28-tetrahydroxyolean-12-ene (4), Saikogenin D (5), prosaikogenin F (6), prosaikogenin A (7), prosaikogenin G (8), prosaikogenin D (9), laccaic acid (10b), methyl gallate (11), and ethyl gallate (12). Compounds 1, 2, 7, 8, and 10 were observed to have inhibitory activity against mesangial cell proliferationin to different degrees. Conclusion: Compound 1, 8, and 10 exhibit significant inhibitory effects on rat mesangial cell proliferation induced by Ang II.