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Ilexsaponin B2 Sale

(Synonyms: 青皂苷B2;毛冬青皂苷B2) 目录号 : GC60199

IlexsaponinB2是从IlexpubescensHook.etArn.中分离出来的一种皂苷,也是一种有效的磷酸二酯酶5(PDE5)和PDEI抑制剂,IC50值分别为48.8μM和477.5μM。

Ilexsaponin B2 Chemical Structure

Cas No.:108906-69-0

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产品描述

Ilexsaponin B2 is a saponin isolated from the root of Ilex pubescens Hook. et Arn. Ilexsaponin B2 is a potent phosphodiesterase 5 (PDE5) and PDEI inhibitor with IC50 values of 48.8 μM and 477.5 μM, respectively[1].

[1]. Zichen Liu, et al. Rapid Screening of Potential Phosphodiesterase Inhibitors From the Roots of Ilex pubescens Hook. Et Arn. Using a Combination of Ultrafiltration and LC-MS. Evid Based Complement Alternat Med. 2017;2017:2749643.

Chemical Properties

Cas No. 108906-69-0 SDF
别名 青皂苷B2;毛冬青皂苷B2
Canonical SMILES OC([C@]12[C@]([C@](O)([C@@H](C)CC2)C)([H])C3=CC[C@@]([C@@]4([C@@](C(C)([C@@H](O[C@@]5([H])[C@@H]([C@H]([C@H](O)CO5)O)O[C@@]6([H])[C@@H]([C@H]([C@H](O)[C@@H](CO)O6)O)O[C@@]7([H])[C@@H]([C@@H]([C@@H](O)[C@H](C)O7)O)O)CC4)C)([H])CC8)C)([H])[C@]8(C)[C@]3(C)CC1)=O
分子式 C47H76O17 分子量 913.1
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Research Update

Study of Absorption Characteristics of the Total Saponins from Radix Ilicis Pubescentis in an In Situ Single-Pass Intestinal Perfusion (SPIP) Rat Model by Using Ultra Performance Liquid Chromatography (UPLC)

Molecules 2017 Nov 1;22(11):1867.PMID:29104273DOI:10.3390/molecules22111867.

In contrast to the extensively reported therapeutic activities, far less attention has been paid to the intestinal absorption of the total saponins from Radix Ilicis Pubescentis (in Chinese Mao-Dong-Qing, MDQ). This study aimed to investigate the intestinal absorption characteristics of ilexgenin A (C1), ilexsaponin A1 (C2), ilexsaponin B1 (C3), Ilexsaponin B2 (C4), ilexsaponin B3 (DC1), and ilexoside O (DC2) when administrated with the total saponins from MDQ (MDQ-TS). An UPLC method for simultaneous determination of C1, C2, C3, C4, DC1, and DC2 in intestinal outflow perfusate was developed and validated. The absorption characteristics of MDQ-TS were investigated by evaluating the effects of intestinal segments, drug concentration, P-glycoprotein (P-gp) inhibitor (verapomil), endocytosis inhibitor (amantadine) and ethylene diamine tetraacetic acid (EDTA, tight junction modulator) on the intestinal transportation of MDQ-TS by using a single-pass intestinal perfusion (SPIP) rat model, and the influence of co-existing components on the intestinal transport of the six saponins was discussed. The results showed that effective apparent permeability (Papp) of C1, C2, C3, C4, and DC2 administrated in MDQ-TS form had no segment-dependent changes at low and middle dosage levels. C1, C2, C3, D4, DC1, and DC2 administrated in MDQ-TS form all exhibited excellent transmembrane permeability with Papp > 0.12 × 10-2 cm·min-1. Meanwhile, Papp and effective absorption rate constant (Ka) values for the most saponins showed concentration dependence and saturation characteristics. After combining with P-gp inhibitor of verapamil, Papp of C2, C3, and DC1 in MDQ-TS group was significantly increased up to about 2.3-fold, 1.4-fold, and 3.4-fold, respectively in comparison to that of non-verapamil added group. Verapamil was found to improve the absorption of C2, C3, and DC1, indicating the involvement of an active transport mechanism in the absorption process. Compared with the non-amantadine added group, the absorption of C1, C2, C4, DC1, and DC2 were decreased by 40%, 71%, 31%, 53%, and 100%, respectively. Papp for the six target compounds increased up to about 1.2-2.1-fold in comparison with the non-EDTA added, respectively. The gastrointestinal transport of MDQ-TS could be greatly promoted by EDTA, and inhibited by amantadine, implying that the intestinal absorption of MDQ-TS was by passive diffusion and endocytosis process. Compared with monomer administration group, the intestinal absorption of C3, C4, DC1, and DC2 was significantly improved by co-existing components in MDQ-TS, and the non-absorbable saponins of C4, DC1, and DC2 unexpectedly showed sufficient intestinal permeability with Papp > 0.12 × 10-2 cm·min-1. This suggested that compounds orally administrated in TCM extract forms displayed unique intestinal absorption characteristics different from those of monomers, and the enhancing intestinal absorption of MDQ-TS reflected a holistic and specific view of traditional Chinese medicines (TCMs).

[A new oleanane-type triterpenoid glycoside from roots of Ilex asprella]

Zhongguo Zhong Yao Za Zhi 2017 Jul;42(13):2503-2509.PMID:28840691DOI:10.19540/j.cnki.cjcmm.20170512.005.

A new δ-oleanane-type triterpenoid glycoside, 3-O-(3-O-sulfo)-β-D-glucopyranosiduronic acid 3β-hydroxy-13(18)-oleanen- 28-oic acid 28-β-D-glucopyranosyl ester (1), along with ten known triterpenoid glycosides, rotundinoside A (2), oblonganoside M (3), 3-O-β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl 3β,19α-dihydroxy-20α- urs-12-en-28-oic acid 28-O-β-D- glucopyranosyl ester (4), Ilexsaponin B2 (5), ilexside Ⅱ (6), rotundinoside B (7), ilekudinoside B (8), ilexpublesnin E (9), ilekudinoside D (10) and ilexpernoside D (11), was isolated from the 75% ethanol extract of the roots of Ilex asprella by various chromatographic separation. Their structures were identified on the basis of MS, NMR spectroscopic analysis and chemical methods. In addition, 2-11 were isolated from I. asprella for the first time.

Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of Ilex pubescens Hook. et Arn. Using a Combination of Ultrafiltration and LC-MS

Evid Based Complement Alternat Med 2017;2017:2749643.PMID:28424739DOI:10.1155/2017/2749643.

The cyclic nucleotide phosphodiesterase (PDE) plays an important role in regulating the levels of second messenger molecules cAMP and cGMP. Various PDE inhibitors have been successfully developed into drugs for targeted diseases. In addition, PDE inhibitors can also be found in different foods and natural medicines. In this study, ultrafiltration liquid chromatography-diode-array detector-electrospray ionization-ion-trap-time-of-flight-mass spectrometry (ultrafiltration LC-DAD-ESI-IT-TOF-MS) was applied to screen PDE inhibitors from the roots of Ilex pubescens Hook. et Arn. As a result, 11 major compounds were identified in I. pubescens roots, with nine compounds as potential PDE inhibitors, among which five were further confirmed to be active against PDEI and PDE5A dose-dependently in vitro, with ilexsaponin A1 and Ilexsaponin B2 being the strongest. HPLC quantification of these bioactive compounds suggested that they are major components in the plant. The results demonstrate that ultrafiltration LC-DAD-ESI-IT-TOF-MS is an efficient method for rapid screening of PDE inhibitors from natural medicines.