Sibiricose A6
(Synonyms: 西伯利亚远志糖A6) 目录号 : GC37637Sibiricose A6 是从 Polygalae Radix 中分离出的一种寡糖酯,具有抗氧化活性。
Cas No.:241125-75-7
Sample solution is provided at 25 µL, 10mM.
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Sibiricose A6 is an oligosaccharide ester isolated from Polygalae Radix with potent antioxidant activity[1][2].
[1]. Ba Y, et al. Intestinal Absorption Profile of Three Polygala Oligosaccharide Esters in Polygalae Radix and the Effects of Other Components in Polygalae Radix on Their Absorption. Evid Based Complement Alternat Med. 2019 Jul 2;2019:1379531. [2]. Shi Q, et al. Indirect identification of antioxidants in Polygalae Radix through their reaction with 2,2-diphenyl-1-picrylhydrazyl and subsequent HPLC-ESI-Q-TOF-MS/MS. Talanta. 2015 Nov 1;144:830-5.
Cas No. | 241125-75-7 | SDF | |
别名 | 西伯利亚远志糖A6 | ||
Canonical SMILES | OC[C@]([C@H]1OC(/C=C/C2=CC(OC)=C(O)C(OC)=C2)=O)(O[C@H](CO)[C@H]1O)O[C@H]([C@@H]([C@@H](O)[C@@H]3O)O)O[C@@H]3CO | ||
分子式 | C23H32O15 | 分子量 | 548.49 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.8232 mL | 9.1159 mL | 18.2319 mL |
5 mM | 0.3646 mL | 1.8232 mL | 3.6464 mL |
10 mM | 0.1823 mL | 0.9116 mL | 1.8232 mL |
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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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工作液浓度: mg/ml;
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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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Indirect identification of antioxidants in Polygalae Radix through their reaction with 2,2-diphenyl-1-picrylhydrazyl and subsequent HPLC-ESI-Q-TOF-MS/MS
Talanta 2015 Nov 1;144:830-5.PMID:26452897DOI:10.1016/j.talanta.2015.07.032.
A rapid and efficient method for the identification of antioxidants in the traditional Chinese medicine Polygalae Radix (PR) by HPLC-ESI-Q-TOF-MS/MS is described. The method is based on the hypothesis that upon reaction of antioxidants with 1,1-diphenyl-2-picrylhydrazyl (DPPH), the peak areas of compounds with potential antioxidant activities in the HPLC chromatogram will be significantly reduced in comparison to the untreated sample. The identity confirmation was achieved by Q-TOF-MS/MS technique. With this method, eight components were proposed possessing potent antioxidant activity. They were identified as sibiricose A5, Sibiricose A6, sucrose monoester, polygalaxanthone III, tenuifoliside B, 3',6-disinapoylsucrose (DISS), sucrose diester, tenuifoliside C, respectively. DISS was proposed to be the most potent one. The antioxidant activity of DISS was evaluated by DPPH, ABTS radical scavenging assay and ferric-reducing antioxidant power (FRAP) assay in vitro. Vitamin C (Vc) was used as positive control substance. DISS showed moderate DPPH (DISS's IC50 value was 1024.17 μg/mL, Vc's was 294.68 μg/mL) and ABTS (IC50 324.13 μg/mL, Vc's was 117.50 μg/mL) free radical scavenging capacity and ferric-reducing antioxidant power. DISS can be used as a new source of natural antioxidant in foods and cosmetics.
UHPLC-MS/MS method for pharmacokinetic and bioavailability determination of five bioactive components in raw and various processed products of Polygala tenuifolia in rat plasma
Pharm Biol 2020 Dec;58(1):969-978.PMID:32956609DOI:10.1080/13880209.2020.1818790.
Context: Sibiricose A5 (A5), Sibiricose A6 (A6), 3,6'-disinapoyl sucrose (DSS), tenuifoliside A (TFSA) and 3,4,5-trimethoxycinnamic acid (TMCA) are the main active components of Polygala tenuifolia Willd. (Polygalaceae) (PT) that are active against Alzheimer's disease. Objective: To compare the pharmacokinetics and bioavailability of five active components in the roots of raw PT (RPT), liquorice-boiled PT (LPT) and honey-stir-baked PT (HPT). Materials and methods: The median lethal dose (LD50) was evaluated through acute toxicity test. The pharmacokinetics of five components after oral administration of extracts of RPT, LPT, HPT (all equivalent to 1.9 g/kg of RPT extract for one dose) and 0.5% CMC-Na solution (control group) were investigated, respectively, in Sprague-Dawley rats (four groups, n = 6) using UHPLC-MS/MS. In addition, the absolute bioavailability of A5, A6, DSS, TFSA and TMCA after oral administration (7.40, 11.60, 16.00, 50.00 and 3.11 mg/kg, respectively) and intravenous injection (1/10 of the corresponding oral dose) in rats (n = 6) was studied. Results: The LD50 of RPT, LPT and HPT was 7.79, 14.55 and 15.99 g/kg, respectively. AUC 0- t of RPT, LPT and HPT were as follows: A5 (433.18 ± 65.48, 680.40 ± 89.21, 552.02 ± 31.10 ng h/mL), A6 (314.55 ± 62.73, 545.76 ± 123.16, 570.06 ± 178.93 ng h/mL) and DSS (100.30 ± 62.44, 232.00 ± 66.08, 197.58 ± 57.37 ng h/mL). The absolute bioavailability of A5, A6, DSS, TFSA and TMCA was 3.25, 2.95, 2.36, 1.17 and 42.91%, respectively. Discussion and conclusions: The pharmacokinetic and bioavailability parameters of each compound can facilitate future clinical studies.
UPLC Quantitative Analysis of Multi-Components by Single Marker and Quality Evaluation of Polygala tenuifolia Wild. Extracts
Molecules 2017 Dec 20;22(12):2276.PMID:29261155DOI:10.3390/molecules22122276.
The quality control of Polygala tenuifolia Wild. is a major challenge in its clinical application. In this paper, a new strategy for the quality evaluation of P. tenuifolia extracts was verified through reverse-phase ultra-performance liquid chromatography (UPLC). The quantitative analysis of multi-components by a single marker (QAMS) was conducted with 3,6'-disinapoyl sucrose as an internal reference substance. Eight components (i.e., sibiricose A5, Sibiricose A6, glomeratose A, tenuifoliside A, tenuifoliside B, tenuifoliside C, sibiricaxanthone B, and polygalaxanthone III) were determined based on the relative correction factors. The concentrations of these components were also determined by applying a conventional external standard method. The cosine value confirmed the consistency of the two methods (cosine ratio value >0.999920). Hierarchical cluster analysis, radar plots, and discriminant analysis were performed to classify 23 batches of P. tenuifolia extracts from Shanxi, Hebei, and Shaanxi in China. Results revealed that QAMS combined with radar plots and multivariate data analysis could accurately measure and clearly distinguish the different quality samples of P. tenuifolia. Hence, QAMS is a feasible and promising method for the quality control of P. tenuifolia.
Intestinal Absorption Profile of Three Polygala Oligosaccharide Esters in Polygalae Radix and the Effects of Other Components in Polygalae Radix on Their Absorption
Evid Based Complement Alternat Med 2019 Jul 2;2019:1379531.PMID:31354847DOI:10.1155/2019/1379531.
Oligosaccharide esters, which are among the main active components of Polygalae Radix (PR), demonstrate significant pharmacological activities in the human nervous system. In our previous research, some other constituents in PR were able to improve the bioavailability of oligosaccharide esters such as sibiricose A5 (SA5), Sibiricose A6 (SA6), and 3,6'-disinapoyl sucrose (DISS), but the related components and their underlying mechanisms remain unknown. The present study aimed to investigate the intestinal absorptive profile of SA5, SA6, and DISS and the absorptive behavior influenced by the coadministration of polygalaxanthone III and total saponins of PR (TS) using an in vitro everted rat gut sac model, along with the possible mechanisms that may influence absorption. The results showed that TS could significantly enhance the absorption of SA5, SA6, and DISS monomers. Verapamil, a P-glycoprotein inhibitor, was able to elevate the absorption of SA5 and SA6, and an absorption experiment using Rho123 led us to conclude that TS influenced the absorption of SA5 and SA6 in a manner similar to that of a P-glycoprotein inhibitor. Sodium caprate, a paracellular absorption enhancer, was found to increase the absorption of SA5, SA6, and DISS. Results showed that the absorption mechanisms of SA5 and SA6 may combine active transport with paracellular passive penetration, while DISS's absorption was dominated by paracellular passive penetration. However, the relationship between polygala saponins and the absorption of SA5, SA6, and DISS by paracellular passive penetration remain to be examined. This is the direction of our future research.
[Key quality attributes of benchmark samples of famous classical formula Kaixin Powder]
Zhongguo Zhong Yao Za Zhi 2023 Jan;48(2):382-389.PMID:36725228DOI:10.19540/j.cnki.cjcmm.20220520.301.
We prepared 15 batches of Kaixin Powder benchmark samples with the decoction pieces of different batches. Further, we established the specific chromatograms and index component content determination method of Kaixin Powder benchmark samples and analyzed the peaks and similarity of the chromatograms. With sibiricose A5, Sibiricose A6, polygalaxanthone Ⅲ, 3,6'-disinapoyl sucrose, ginsenoside Rb_1, β-asarone, α-asarone, and dehydropachymic acid as index components, the index component content determination method was established and 70%-130% of the mean content of each component was set as the range. The chromatograms of 15 batches of Kaixin Powder benchmark samples had a total of 22 characteristic peaks, among which 8 peaks were identified, which represented sibiricose A5, Sibiricose A6, polygalaxanthone Ⅲ, 3,6'-disinapoyl sucrose, ginsenoside Rb_1, β-asarone, α-asarone, and dehydropachymic acid, respectively. The chromatograms shared the similarity of 0.992-0.999. The 15 batches of benchmark samples had sibiricose A5 of 0.34-0.55 mg·g~(-1), Sibiricose A6 of 0.43-0.57 mg·g~(-1), polygalaxanthone Ⅲ of 0.12-0.19 mg·g~(-1), 3,6'-disinapoyl sucrose of 1.08-1.78 mg·g~(-1), ginsenoside Rb_1 of 0.33-0.62 mg·g~(-1), β-asarone of 2.34-3.72 mg·g~(-1), α-asarone of 0.11-0.22 mg·g~(-1), and dehydropachymic acid of 0.053-0.079 mg·g~(-1). This study established the specific chromatograms and index component content determination method of Kaixin Powder benchmark samples, and the method was simple, feasible, reproducible, and stable. This study provides a scientific basis for further research on the key chemical properties of the benchmark samples and preparations of Kaixin Powder.