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Protogracillin Sale

(Synonyms: 原纤细薯蓣皂甙) 目录号 : GC44731

A steroid saponin

Protogracillin Chemical Structure

Cas No.:54848-30-5

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1mg
¥679.00
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5mg
¥3,059.00
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10mg
¥5,428.00
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产品描述

Protogracillin is a steroid saponin originally isolated from T. terrestris. It is cytotoxic to K562 cells (IC50 = 3.3 µM).

Chemical Properties

Cas No. 54848-30-5 SDF
别名 原纤细薯蓣皂甙
Canonical SMILES C[C@@]1([C@]([C@@H]2C)([H])[C@](O[C@]2(O)CC[C@@H](C)CO[C@@H]([C@@H]([C@@H](O)[C@@H]3O)O)O[C@@H]3CO)([H])C4)[C@]4([H])[C@@](CC=C5[C@@]6(CC[C@H](O[C@@](O[C@H](CO)[C@@H](O)[C@@H]7O[C@]([C@@H]([C@@H](O)[C@@H]8O)O)([H])O[C@@H]8CO)([H])[C@@H]7O[C@@](O[C@@H
分子式 C51H84O23 分子量 1065.2
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 0.9388 mL 4.694 mL 9.3879 mL
5 mM 0.1878 mL 0.9388 mL 1.8776 mL
10 mM 0.0939 mL 0.4694 mL 0.9388 mL
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Research Update

Methyl Protogracillin (NSC-698792): the spectrum of cytotoxicity against 60 human cancer cell lines in the National Cancer Institute's anticancer drug screen panel

Anticancer Drugs 2001 Jul;12(6):541-7.PMID:11460001DOI:10.1097/00001813-200107000-00008.

Methyl Protogracillin (NSC-698792) was a furostanol saponin isolated from the rhizome of Dioscorea collettii var. hypoglauca (Dioscoreaceae), a Chinese herbal remedy for the treatment of cervical carcinoma, carcinoma of urinary bladder and renal tumor for centuries, in our previous studies. In order to systematically evaluate its potential anticancer activity, methyl Protogracillin was tested for its cytotoxicity in vitro against 60 human cancer cell lines in the National Cancer Institute (NCI)'s anticancer drug screen. As a result, it was found that methyl Protogracillin was cytotoxic against all the tested cell lines from leukemia and solid tumors in the NCI's human cancer panel; it showed particular selectivity against one colon cancer line (KM12), one central nervous system (CNS) cancer line (U251), two melanoma lines (MALME-3M and M14), two renal cancer lines (786-0 and UO-31) and one breast cancer line (MDA-MB-231) with GI50< or =2.0 microM. The selectivity between these seven most sensitive lines and the least sensitive line (CCRF-CEM) ranged from 26- to 56-fold. In the same cancer subpanel, selectivity more than 15-fold was observed between MDA-MB-231 and MCF-7, NCI-ADR-RES, BT-549 in breast cancer. From a general view of the mean graph, CNS cancer is the most sensitive subpanel, while ovarian cancer and renal cancer are the least sensitive subpanels. Based on an analysis of the COMPARE computer program with methyl Protogracillin as a seed compound, no compounds in the NCI's anticancer drug screen database have similar cytotoxicity patterns (mean graph) to that of methyl Protogracillin, indicating a potential novel mechanism of the anticancer action involved.

Paris polyphylla: chemical and biological prospectives

Anticancer Agents Med Chem 2014;14(6):833-9.PMID:24917072DOI:10.2174/1871520614666140611101040.

Paris polyphylla J.E. Smith is extensively used in traditional systems of Indian and Chinese medicines mainly for its anticancerous property. The national and international demand for P. polyphylla is constantly increasing and most of the supplies come from wild. Illegal and unscientific exploitation coupled with habitat destruction decreases the natural population of the herb, as a consequence this species comes under vulnerable category. Restoration and conservation of the natural population of this potential herb is prerequisites. This article aims to provide an overview on chemical and biological prospective of P. polyphylla. Secondary metabolites such as daucosterol, polyphyllin D, β -ecdysterone, Paris saponins I, II, V, VI, VII, H, dioscin, oligosaccharides, heptasaccharide, octasaccharide, trigofoenoside A, Protogracillin, Paris yunnanosides G-J, padelaoside B, pinnatasterone, formosanin C and 20-hydroxyecdyson saponins have been isolated from P. polyphylla. Several biological activities such as anticancerous, antitumor, cytotoxic, anthelmintic, antimicrobial, antiangiogenic, immunostimulating, contractile and hemostatic have also been reported. Consequently, this review will be helpful to the researcher and scientist for further research.

[Quality control of Dioscoreae Nipponicae Rhizoma based on fingerprint and quantitative analysis]

Zhongguo Zhong Yao Za Zhi 2020 Oct;45(20):4949-4956.PMID:33350268DOI:10.19540/j.cnki.cjcmm.20200615.201.

Dioscoreae Nipponicae Rhizoma, the dried rhizoma of Dioscorea nipponica, has been widely used in traditional Chinese medicines. According to the different of the growth and cultivation patterns, Dioscoreae Nipponicae Rhizoma can be divided into two species, the wild Dioscoreae Nipponicae Rhizoma and the cultivated Dioscoreae Nipponicae Rhizoma. In this paper, an accurate and reliable fingerprint of Dioscoreae Nipponicae Rhizoma was established based on HPLC coupled with evaporative light scattering detector(ELSD). A total of 6 common peaks were marked, and the similarity of the Dioscoreae Nipponicae Rhizoma samples was above 0.950. The results indicated that the established fingerprint could be used for quality evaluation of Dioscoreae Nipponicae Rhizoma. Moreover, an HPLC coupled with ELSD method was developed for simultaneous quantitative analysis of six steroidal saponins, including protodioscin, Protogracillin, methyl protodioscin, pseudoprotodioscin, dioscin and gracillin in wild Dioscoreae Nipponicae Rhizoma and cultivated Dioscoreae Nipponicae Rhizoma samples. Furthermore, chemometrics analysis such as principal component analysis and partial least squares discriminant analysis were performed to compare and discriminate wild Dioscoreae Nipponicae Rhizoma and cultivated Dioscoreae Nipponicae Rhizoma samples based on the quantitative data. The results indicated that the contents of steroidal saponins were notably different between the wild and cultivated Dioscoreae Nipponicae Rhizoma, and protodioscin and Protogracillin were significant to effectively discriminate the wild and cultivated Dioscoreae Nipponicae Rhizoma samples, and these two compounds could be recognized as chemical markers. In conclusion, this present study might provide useful data and acceptable analysis method for identification and quality evaluation of Dioscoreae Nipponicae Rhizoma.

Antineoplastic agents. II. Four furostanol glycosides from rhizomes of Dioscorea collettii var. hypoglauca

Planta Med 1997 Apr;63(2):161-5.PMID:17252340DOI:10.1055/s-2006-957636.

During activity-guided fractionations to screen for antineoplastic agents, further studies by means of preparative HPLC led to the isolation of four known furostanol saponins: protoneodioscin, protodioscin, protoneogracillin, Protogracillin, along with their corresponding artifacts: methyl protoneodioscin, methyl protodioscin, methyl protoneogracillin, and methyl Protogracillin, from the rhizomes of Dioscorea collettii var. hypoglauca. Among them, protoneodioscin, protodioscin, and protoneogracillin are first reported from the title plant. The structures of the compounds were established on the basis of chemical evidence and spectral analysis (1H-NMR, 13C-IMMR, 1H-1H COSY, HMQC, HMBC, and FAB-MS). These eight compounds all caused morphological abnormality of Pyricularia oryzae mycelia. They also showed cytotoxic activities against the cancer cell line of K562 in vitro as antineoplastic agents.

Screening and identification of lipase inhibitors extracted from Dioscorea nipponica Makino by UV-vis and HPLC coupled to UPLC-Q-TOF-MS/MS

Int J Biol Macromol 2023 Mar 1;230:123427.PMID:36706882DOI:10.1016/j.ijbiomac.2023.123427.

Dioscoreae nipponica Makino (D. nipponica) as the rhizome of dioscoreaceae rich in steroidal saponins, has been reported to have the hypolipidemic effects etc. However, it is still unclear which exact active components are primary responsible for the beneficial effects. This study was conducted to fish out the lipase inhibitors from D. nipponica, and evaluate the inhibitory activity on porcine pancreatic lipase (PPL) through in vitro kinetic assay using p-nitrophenyl palmitate as substrate. Accordingly, the ethanolic extract was subjected to D101 macroporous resin purification for spectrophotometric screening, high performance liquid chromatography (HPLC) separation and structural characterization by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry. Through orlistat validation, the PPL inhibitory activity and IC50 value of the extract were respectively 68.34 ± 1.47 % and 107.05 μg/mL under the optimized inhibition conditions. From 6 steroidal saponins identified, the inhibitory components named the protodioscin, Protogracillin, dioscin and gracillin were fished out by grouping separation and HPLC analysis. Furthermore, dioscin and gracillin with the parent structure of diogenin were confirmed as the major inhibitors by virtue of stability tests based on transformation of protodioscin and Protogracillin. Finally, the inhibitory mechanism of the major inhibitors toward PPL was further clarified by kinetic analysis and molecular docking analysis. The proposed method not only revealed the PPL inhibitory components in D. nipponica, but also provided an effective approach to hierarchical screening of PPL inhibitors from natural plants.