Advances in Pharmacological Studies of Calycosin-7-O-β-D-glucoside

The isoflavone compound Calycosin-7-O-β-D-glucoside (CG) is an active monomer component extracted from the dry roots of the leguminous plant Astragalus mongolicus and Astragalus. It is also one of the main active ingredients in the Astragalus that is a commonly used traditional herb. CG has obvious effects of anti-oxidation, anti-virus, inhibition of melanin formation, and immunosuppression. With the advancement of modern technology, it has become a pivotal subject that the adjuvant therapy or even substitute for the synthetic drug of monomer of Chinese herb in medical field. In recent years, with the deepening of research on the mechanism of action of CG, which has been found that its pharmacological effects are very extensive, such as the anti-tumor effect and the effect on cerebrovascular diseases of CG. This review summarizes the pharmacological effects and the latest research progress of CG.

HPLC法测定不同产地功劳木中3个有效成分

目的测定功劳木中3,4,5-三甲氧基苯酚-1-O-β-D-葡萄糖苷(1)e、rythro-syringoylglycerol-8-O-β-D-glucoside(2)、5,5'-二甲氧基落叶松脂醇-4'-O-β-D-葡萄糖苷(3),为功劳木质量控制提供科学依据。方法采用高效液相色谱法,依利特Hypersil-C18柱(4.6 mm×250 mm,5μm);流动相为乙腈-水(14∶86);检测波长280 nm;体积流量1 mL/min;柱温25℃。结果化合物12,,3分别在0.12～2.40μg(r=0.999 5),0.20～4.00μg(r=0.999 6),0.07～1.40μg(r=0.999 6)与峰面积Y线性关系良好,平均加样回收率依次为100.3%,98.8%,97.2%(n=6)。结论该方法快速,简单,重复性好,适用于同时测定功劳木中化合物12,3,。

A Novel Lignan Glucoside from Forsythia suspensa Vahl

从连翘果实中分离得到了五个单体化合物，根据理化性质和光谱分析鉴定为：对－羟基苯乙酸［ｐ－ｈｙｄｒｏｘｙｐｈｅｎｙｌａｃｅｔｉｃａｃｉｄ］（１），（＋）松脂素－β－Ｄ－葡萄糖甙［（＋）ｐｉｎｏｒｅｓｉｎｏｌ－β－Ｄ－ｇｌｕｃｏｓｉｄｅ］（２），（＋）表松脂素－４－β－Ｄ－葡萄糖甙［（＋）ｅｐｉｐｉｎｏｒｅｓｉｎｏｌ－４－β－Ｄ－ｇｌｕｃｏｓｉｄｅ］（３），（＋）松脂素单甲基醚－β－Ｄ－葡萄糖甙［（＋）ｐｉｎｏｒｅｓｉｎｏｌｍｏｎｏｍｅｔｈｙｌｅｔｈｅｒ－β－Ｄ－ｇｌｕｃｏｓｉｄｅ］（４），连翘甙［ｐｈｉｌｙｒｉｎ］（５）。其中３未见文献报道。

Two new compounds derived from bufalin

The biotransformation of bufalin by cell suspension cultures of Platycodon grandifiorus was investigated and two new biotransformed products were obtained, which was 3-epi-telocinobufagln and 3-epi-bufalin-3-O-β-D-glucoside.

Inhibitory Effects of 2,3,4',5-tetrahydroxystilbene-2-O-β-D-glucoside on Angiotensin Ⅱ-Induced Proliferation of Vascular Smooth Muscle Cells

Objective：To investigate the effect of 2,3,4’,5-tetrahydroxystilbene-2-0- p-D-glucoside（TSG）,an active component extracted from the root of Polygonum multiflorum,on angiotensin Ⅱ（Ang Ⅱ）-induced proliferation of cultured rat vascular smooth muscle cells（VSMCs） and to identify the potential mechanism.Methods：Cell proliferation and cell cycle were determined by cell counting,5-bromo-2’-deoxyuridine incorporation assay,proliferating cell nuclear antigen protein expression and flow cytometry.Levels of phosphorylated extracellular signal-regulated kinase 1/2（ERK1/2）,mitogenic extracellular kinase 1/2（MEK1/2） and Src in VSMCs were measured by Western blot.The expression of c-fos,c-jun and c-myc mRNA were measured by reverse transcription polymerase chain reaction（RT-PCR）.Intracellular reactive oxygen species（ROS） was measured by fluorescence assay.Results：TSG significantly inhibited Ang Ⅱ-induced VSMCs proliferation and arrested cells in the G1/S checkpoint（P〈0.05 or P〈0.01）.TSG decreased the levels of phosphorylated ERK1/2,MEK1/2 and Src in VSMCs（P〈0.05 or P〈0.01）.TSG also suppressed c-fos,c-jun and c-myc mRNA expression（P〈0.05 or P〈0.01）.In addition,the intracellular ROS was reduced by TSG（P〈0.01）.Conclusions：TSG inhibited Ang Ⅱ-induced VSMCs proliferation.Its antiproliferative effect might be associated with down-regulation of intracellular ROS,followed by the suppression of the Src-MEK1/2-ERK1/2 signal pathway,and hence,blocking cell cycle progression.

Beneficial effects of anthocyanins against diabetes mellitus associated consequences——A mini review

Anthocyanins(ACN) are water-soluble pigments, belonging to flavonoids, and are present in almost all fruits, and vegetables at varying concentration. About 635 ACN were distinguished based on the position and number of methoxyl and hydroxyl moieties in the basic structure of ACN. Pelargonidin, cyanidin, delphinidin, malvidin, peonidin, and petunidin are extensively studied anthocyanidins. The absorption, bioavailability, metabolism, pharmacokinetics, molecular mechanism, and analytical techniques of several phytochemicals were described. The biological benefits(antidiabetic, anti-neuro-disorder, anti-cardiovascular diseases, antigastrointestinal diseases, and disorders) of flavonoids and ACN have been reported. Several in vitro, and in vivo reports demonstrated that ACN-rich plant extracts ameliorate the diabetesassociated consequences by reducing the glucose absorption, ROS production, oxidative stress, glomerular angiogenesis, lipid synthesis, and FoxO1 and adipose triglyceride lipase expressions, and improve the insulin secretion, insulin sensitivity, glucose tolerance, glucose uptake, glucose consumption, antioxidant activity. The literature search was made in Scopus, Google Scholar, PubMed using the keywords "anthocyanin" and "diabetes". The documents were carefully checked for the relevance to the current manuscript and the selection was made without any chronological restriction. The present manuscript summarizes the updated reports on antihyperglycemic properties of ACN.

A new flavone glycoside from Cancrinia discoidea(Ledeb.) Poljak

A new flavone glucoside,selagin-7-O-（6″-O-acetyl-）-β-D-glycoside,has been isolated from Cancrinia discoidea（Ledeb.） Poljak.Its structure was identified by spectroscopic methods,2D NMR and MS.Compounds exhibited activity of anti-inflammatory in vitro.

Bioactivity‑Guided Isolation of Totarane‑Derived Diterpenes from Podocarpus neriifolius and Structure Revision of 3‑Deoxy‑2α‑hydroxynagilactone E

Bioactivity-guided phytochemical investigation of Podocarpus neriifolius D.Don.(Podocarpaceae)has led to the isolation of one new(2)and three known(1,3,and 4)B-type podolactones,along with three totarane-type diterpenes(5-7).Their structures were determined by interpretation of High Resolution ElectroSpray Ionization Mass Spectrometry(HRESIMS)and 1D and 2D NMR data,and comparison with the values reported in the literature.The structure of compound 1,previously identifed as 3-deoxy-2α-hydroxynagilactone E(8),was revised as its 2β-epimer,which has been reported recently as a new compound.All of the isolates were evaluated for their antiproliferative activity against a panel of four human cancer cell lines,namely,ovarian(OVCAR3),breast(MDA-MB-231),colon(HT-29),and melanoma(MDA-MB-435),and compounds 1 and 3 were found to be cytotoxic with IC_(50) values in the low micromolar range for most of the cell lines used.The major compound,inumakilactone A(3),was further tested in vivo using the HT-29,MDA-MB-435,and OVCAR3 cells in a murine hollow fber model,for the frst time.

过山蕨水提物的化学成分分离鉴定

目的:过山蕨为铁角蕨科过山蕨属植物过山蕨(Camptosorus sibiricus)的地上全草部位,是一种民间常用药,目前关于过山蕨的生物活性研究主要集中在过山蕨总黄酮上,对其化学成分的研究尚有不足,药效成分也不能完全确认。该实验对过山蕨的化学成分进行系统分离,从药效物质基础的角度探寻其作为过山蕨补充药物来源的可能性,为进一步的药理活性和充分开发利用过山蕨植物资源提供物质基础和科学依据。方法:采用硅胶柱,ODS开放柱,Sephadex LH-20柱以及反相高效液相色谱法对过山蕨水提物进行化学成分的分离。根据其理化性质和波谱数据鉴定化合物结构。结果:分离得到10个化合物,分别鉴定为(7E)-9-hydroxymegastigma-4,7-dien-3-on-9-O-β-D-glucoside (1),bridelionoside F (2),(3R,5S,6S,7E,9S)-megastigman-7-ene-3,5,6,9-tetrol 9-O-β-D-glucopyranoside(3),(6S,7E,9R)-roseoside(4),(3S,5S,6R,9R)-3-hydroxy-5,6-epoxy-β-ionol-9-O-β-glucopyranoside(5),6,9-dihydroxy-4,7-megastigmadien-3-one(6),elaphoside A(7),ptelatoside-A(8),n-butyl-α-β-Dfructofuranoside(9),dibutylphthalate(10)。结论:首次从过山蕨属中分离得到化合物1~10,以上化合物的发现进一步丰富了过山蕨的化学成分组成,为综合开发和利用过山蕨植物资源提供前期的实验基础。

A New Phenolic Glucoside from Paeonia lactiflora

Objective To study the chemical constituents from EtOAc extracts of Paeonia lactiflora.Methods Compounds were isolated by various chromatographic techniques and structures were elucidated on the basis of spectral analysis.Results Seventeen compounds were obtained and their structures were identified as 1,2,6-benzenetriol-1-O-α-D-glucoside(1),paeoniflorin(2),4-methylpaeoniflorin(3),albiflorin(4),paeonidanin(5),benzoylpaeoniflorin(6),4-methylbenzoylpaeoniflorin(7),benzoylalbiflorin(8),paeonidanin A(9),galloylalbiflorin(10),debenzoylalbiflorin(11),4’,5-dihydroxyflavanone-7-O-β-D-glucoside(12),5,7-dihydroxy flavanone-4’-O-β-D-glucoside(13),(+)-catechin(14),gallic acid(15),vanillic acid(16),and 1,2,3-benzenetriol(17).Conclusion Compound 1 is a new compound named paeoniphenoside.Compounds 12 and 13 are firstly obtained from genus Paeonia L.,and compounds 5 and 9 are isolated from P.lactiflora for the first time.

Two New Sesquiterpenoid Glucosides from the Aerial Parts of Saussurea involucrate

Two new sesqulterpenoid glucosides, namely α-hydroxycostic acid 6-β-D-glucopyranoside （compound 1） and 11 βH-11,13-dlhydrodehydrocostuslactone 8α-O-（6＇-acetyl）-β-D-glucopyranoside （compound 2）, along with 11 known sesqulterpenoids （compounds 3-13） were isolated from the aerial parts of Saussurea involucrate （Kar. et Kir.） Sch.- BIp. The structures of the new sesquiterpenoid glucosides were established by one- and two-dimensional nuclear magnetic resonance and mass spectrometry analysis.

Screening and Identifying Hepatotoxic Components in Polygoni multiflori Radix and Polygoni multiflori Radix Praeparata

Objective: In this study, the hepatotoxic components of Polygoni multiflori Radix and Polygoni multiflori Radix Praeparata(known as Heshouwu [HSW] and Zhiheshouwu [ZHSW] in China, respectively) were screened, isolated, and identified. Materials and Methods: The ethanol extracts of HSW and ZHSW were separated into 80 fractions according to their polarity in the preparation liquid phase. Chang liver cell line was used to screen the toxic components of HSW and ZHSW in vitro. The obtained toxic mixture was further collected, isolated, and identified to confirm the hepatotoxic compounds of HSW and ZHSW. Results: The identifid hepatotoxic compounds include 2,3,5,4’-tetrah ydroxystilbene-2-O-β-D-glucoside, emodin, physcion-8-O-β-d-glucoside, physcion, and citreorosein, the fist two among them were the main components of HSW and ZHSW. After processing of HSW, the contents of 2,3,5,4’-tetrahydroxystilbene-2-O-β-D-glucoside and emodin in ZHSW were signifiantly decreased. Conclusions: The traditional processing with herb has signifiant effects on the components, especially the toxic components, in the extract of HSW and is an effective method to reduce its toxicity.

New Isoflavonoid Glycosides from the Rhizomes of Iris leptophylla Lingelsh.

Two new isoflavonoid glucosides, 5-hydroxy-6,7-methylenedioxy-isoflavone-4＇-O-D-glucopyranosyl （2→〉l）-L-rhamnoside （irilone-bioside） （compound 1） and 5,4＇-methoxy-6,7-methylenedioxyisoflavone-3＇-O-β-D-glucoside （irisleptophyllidin） （compound 2）, together with five known compounds, nigricanin- 4＇-O-β-D-glucoside （compound 3）, irifloside （compound 4）, irigenin （compound 5）, 5, 3＇, 4＇-trimethoxy-6,7-methylenedioxyisoflavone （compound 6）, and nigricanin （compound 7） were isolated from the alcoholic extract of rhizomes of Iris leptophylla Lingelsh. Their structures were elucidated by spectroscopic methods.