To breed a new yam cultivar of Dioscorea alata, the different and excellent germplasm resources were investigated within artificially cultivated population and some superior individuals, with a higher yield and medicinal properties, were selected. Considering results of the yield and medicinal properties during 2006-2013 cropping season, strains and lines were established and selected. As a result, the yield of the new developed cultivar (Wenshanyao No. 1, WSY01-1) reached 2217. 0 kg per 667 m2 (fresh weight) and 348.3 kg per 667 m2 (dry weight), and increased 23.8% and 23.9% comparing with control cultivars (landraces). Comparing with control cultivars, the level of polysaccharide, allantoin, and dioscin increased 36.9%, 48.3%, 20.9%, and reached 12.2%, 1.30%, 579.7 µg · g(-1), respectively. This result showed that the systematic selection method can significantly improve yield and medicinal properties of D. alata, and the developed " Wenshanyao No. 1" exhibits wide spreading prospects.
Allantoin ; analysis ; Breeding ; Dioscorea ; chemistry ; genetics ; growth & development ; Diosgenin ; analogs & derivatives ; analysis ; Polysaccharides ; analysis

OBJECTIVETo develop an HPLC method for the determination of pseudoprodioscin in Dioscorea panthaica and provide scientific basis for quality control of it and its preparation.

METHODThe analysis was carried out on a Merck Purospher STAR RP-18e column eluted with acetonitrile and water as mobile phases in gradient mode. The detection wavelength was 203 nm, and the flow rate was 1.0 mL min(-1).

RESULTThe pseudoprodioscin in D. panthaica extract was well separated. The linear range is between 0.0800-4.00 microg, r =0.9999. The average recovery and RSD are 99.9% and 2.3%, respectively.

CONCLUSIONThis method for quantitation of pseudoprodioscin in D. panthaica is simple, accurate and reliable and can be used for the quality control of D. panthaica and its preparations.

Chromatography, High Pressure Liquid ; methods ; Dioscorea ; chemistry ; Diosgenin ; analogs & derivatives ; analysis ; Drugs, Chinese Herbal ; analysis

OBJECTIVEThe aim of this study was to observe the effects of dioscin on apoptosis and on expression of PRDX1 in pancreatic cancer MiaPaCa-2 cells in vitro.

METHODSMTT assay was used to detect the growth rate among the medication groups treated with different concentrations of dioscin. The apoptosis rate was determined by annexin V-fluorescein isothiocyanate/propidium iodide double staining and flow cytometry. Western blot analysis was used to assay the expression of PRDX1 and apoptotic proteins in the cells. Reactive oxygen species (ROS) formation was measured by 2'7'-dichlorofluorescein diacetate (DCFH-DA).

RESULTSDioscin considerably inhibited the proliferation of MiaPaCa-2 cells in vitro. The inhibitory action was enhanced in a dose-dependent manner. The levels of intracellular ROS detected with DCFH-DA were highly increased after dioscin treatment. The flow cytometry analysis using annexin V-PI staining showed that compared with the apoptotic rate of control group [(3.5 ± 0.7)%], 2.5 µmol/L and 5 µmol/L dioscin induced apoptosis in (28.4 ± 0.9)% and (49.6 ± 2.7)% MiaPaCa-2 cells, and Western blot analysis showed that apoptotic proteins Bax and cleaved caspase-3 expressions were increased and antiapoptotic protein Bcl-2 expression was decreased. In addition, these effects could be blocked by antioxidant N-acetylcysteine (NAC) administration, and the apoptotic rates decreased to (10.8 ± 2.3)% and (18.8 ± 3.0)%, respectively. We further observed the decrease of PRDX1 expression after dioscin treatment. Moreover, after PRDX1 overexpression, dioscin treatment no longer induced high levels of ROS and apoptosis, and the apoptotic rate was decreased to (21.3 ± 5.9)%.

CONCLUSIONDioscin can down-regulate the PRDX1 expression, and then induces ROS-mediated apoptosis in cancer cells.

Apoptosis ; drug effects ; Diosgenin ; analogs & derivatives ; pharmacology ; Humans ; Pancreatic Neoplasms ; pathology ; Peroxiredoxins ; drug effects ; Reactive Oxygen Species ; metabolism

This study aims to investigate the molecular mechanism of polyphyllin Ⅰ(PPⅠ) inhibiting proliferation of human breast cancer cells. Human breast cancer BT474 and MDA-MB-436 cells were treated with different concentrations of PPⅠ, and then the effect of PPⅠ on cell proliferation was detected by MTT assay, trypan blue dye exclusion assay, real-time cell analysis, and clone forming assay, respectively. The apoptosis was detected by Annexin V-FITC/PI staining and then analyzed by flow cytometry. The change of mitochondrial membrane potential was detected by flow cytometry after fluorescent probe JC-1 staining. Western blot was used to detect protein expression and phosphorylation. Molecular docking was performed to detect the binding between PPⅠ and EGFR. The affinity between PPⅠ and EGFR was determined by drug affinity responsive target stability assay. The results indicated that PPⅠ inhibited the proliferation and colony formation of BT474 and MDA-MB-436 cells in a time-and concentration-dependent manner. The PPⅠ treatment group showed significantly increased apoptosis rate and significantly decreased mitochondrial membrane potential. PPⅠ down-regulated the expression of pro-caspase-3 protein, promoted the cleavage of PARP, and significantly reduced the phosphorylation levels of EGFR, Akt, and ERK. Molecular docking showed that PPⅠ bound to the extracellular domain of EGFR and formed hydrogen bond with Gln366 residue. Drug affinity responsive target stability assay confirmed that PPⅠ significantly prevented pronase from hydrolyzing EGFR, indicating that PPⅠ and EGFR have a direct binding effect. In conclusion, PPⅠ inhibited the proliferation and induced apoptosis of breast cancer cells by targeting EGFR to block its downstream signaling pathway. This study lays a foundation for the further development of PPⅠ-targeted drugs against breast cancer.
Apoptosis ; Breast Neoplasms/genetics* ; Cell Line, Tumor ; Cell Proliferation ; Diosgenin/analogs & derivatives* ; ErbB Receptors ; Female ; Humans ; Molecular Docking Simulation

OBJECTIVETo study the chemical constituents in the total saponin from Trigonellf foenum-graecum.

METHODThe compounds were isolated by column chromatography on macroporous resin and silica gel and elucidated by physical and chemical evidences and spectroscopic analysis.

RESULTTwo compounds were obtained and identifiedas methyl-protodioscin and methyl-protodeltonin.

CONCLUSIONMethyl-protodioscin and methyl-protodeltonin were isolated from this plant for the first time.

Diosgenin ; analogs & derivatives ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Saponins ; analysis ; chemistry ; isolation & purification ; Seeds ; chemistry ; Trigonella ; chemistry

Diosgenin can inhibit the growth of A375 and K562 cell lines and induce their apoptosis with an effect on pro-apoptotic members of Bcl-2 family. To study the SAR of diosgenin derivatives, and to improve the anti-tumor activity of diosgenin, a series of novel diosgenin derivatives were designed and synthesized. Their anti-tumor activities in vitro were evaluated. The results revealed that most of the new derivatives had potent effects against K562, A375 and A549 (three tumor cell lines) in vitro, and had no or less effect against H293 and L02 (two normal cell lines). Particularly, some compounds (e.g. 1, 6-8) showed excellent activities on K562 with IC50 values ranging from 1.96 to 4.35 micromol x L(-1).
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; Diosgenin ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Drug Design ; Humans

OBJECTIVETo study the effect and mechanism of methyl protodioscin (MPD), an active ingredients of yamogenin, in protecting cardiomyocytes (CMC) against anoxia/reoxygenation (A/R) injury.

METHODSCultured CMCs of neonatal SD rats were randomly divided into three groups, cells in Group A were untreated normal cells, cells in Group B and C were made to injury CMC model by A/R, and only those in Group C were treated with MPD. Levels of ATPase activity and lactate dehydrogenase (LDH) in cell membrane of CMCs were determined. Besides, the mRNA expression of sodium-calcium exchanger (NCX) in MPD treated CMCs was detected.

RESULTSAs compared with Group B, the degree of CMC injury was significantly milder and the activities of Na+ -K+ -ATPase and Ca2+ -Mg2+ -ATPase were higher in Group C after cells were treated with MPD in concentration of 10 microg/mL and 50 microg/mL. The mRNA expression of NCX in CMCs was down-regulated after MPD treatment (P < 0.05).

CONCLUSIONMPD could maintain the low calcium internal environment in CMCs by way of protecting the membranous function of Na+ -pump and Ca2+ -pump, and influencing the Ca2+ transmembrane transportation in CMCs.

Animals ; Cell Hypoxia ; Cells, Cultured ; Diosgenin ; analogs & derivatives ; pharmacology ; Myocardial Reperfusion Injury ; metabolism ; Myocytes, Cardiac ; drug effects ; metabolism ; Oxygen ; adverse effects ; Rats ; Rats, Sprague-Dawley ; Saponins ; pharmacology

AIMTo study the chemical constituents of Dioscorea parviflora.

METHODSThe chemical constituents were isolated by silica gel and RP-18 column chromatography, and their chemical structures were elucidated by IR, NMR and MS.

RESULTSEleven steroides have been isolated from EtOH extract of Dioscorea parviflora and identified as isonarthogenin 3-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranoside (I), diosgenin-diglucoside (II), prosapogenin A of dioscin (III), dioscin (IV), deltonin (V), deltoside (VI), methyl deltoside (VII), diosgenin 3-O-beta-D-glucopyranosyl (1-->3)-beta-D-glucopyranosyl-(1-->4)-[alpha-L-rhamnopyranosyl-(1-->2)]-beta-D-glucopyranoside (VIII), parvifloside (IX), methyl parvifloside (X), diosgenin (XI), and a mixture of beta-sitosterol and stigmasterol.

CONCLUSIONCompound X is a new compound. Compounds VII and X were methyl ethers of VI and IX, respectively, and may be produced during isolation. Compound I is isolated from Dioscorea L., and II, IV from Dioscorea parviflora for the first time.

Dioscorea ; chemistry ; Diosgenin ; analogs & derivatives ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry ; Saponins ; chemistry ; isolation & purification ; Steroids ; chemistry ; isolation & purification

Dioscin, a typical saponin, is widely present in the family of Dioscoreaceae, Liliaceae, Caryophyllaceae and Rosaceae, especially in Dioscoreaceae, including Discorea nipponica Makino, Dioscorea zingiberensis C. H. Wright and Dioscorea panthaica Prain et Burkill. Traditional Chinese medicine reported that dioscin plays a role in expectorant, relaxing the muscles and stimulating the blood circulation, aiding digestion and diuresis. With the development of science and technology in recent years, some new extraction and separation techniques and methods have been applied to the study of dioscin, and more and more pharmacological effects were found. Modern pharmacology studies have confirmed that dioscin had some activities on desensitization, anti-inflammatory, lipid-lowering, anti-tumor, hepatoprotection and anti-viral. After oral administration, dioscin is metabolized to diosgenin, which is the true active ingredient and is an important raw material to synthesize steroid hormone drugs. Therefore, the studies on dioscin are valueable and promising. In this review, we make a summary on the researches of dioscin including the extraction technology, separation and prepara- tion, chemical synthesis, drug metabolism, determination and pharmacological researches.
Animals ; Biological Products ; adverse effects ; chemistry ; pharmacology ; Diosgenin ; adverse effects ; analogs & derivatives ; chemistry ; pharmacology ; Humans ; Plant Extracts ; adverse effects ; chemistry ; pharmacology

The purpose of this paper is to clarify the structure-activity relationship of anti-tumor activity of diosgenin derivatives in vitro. Study has found that diosgenin can inhibit the reproduction of tumor cells by inducing apoptosis and the main target spot of this effect is Bcl-2. Based on the characteristics of pharmacophoric points' of the three-dimensional pharmacophore for Bcl-2 inhibitors, we have docked lots of diosgenin derivatives with Bcl-2, then synthesized 31 compounds of them, finally assessed the anti-tumor activity of the diosgenin derivatives in vitro against A375, A549, HepG-2 and K562. Preliminary studies of SAR have indicated that the aliphatic esters, and aromatic esters of diosgenin without F ring have no anti-tumor activity in vitro. The triazole bromides of diosgenin all achieve fairly good anti-tumor activity in vitro, and those with larger hydrophobic group have the better activity. The stronger is the hydrogen bonding interaction and dipole-dipole interaction of the heterocyclic of diosgenin and diosgenin without F ring and the acid ester of diosgenin without F ring, the better is the activity of derivatives.
Antineoplastic Agents, Phytogenic ; chemical synthesis ; chemistry ; pharmacology ; Apoptosis ; drug effects ; Cell Line, Tumor ; Diosgenin ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Humans ; Proto-Oncogene Proteins c-bcl-2 ; antagonists & inhibitors ; Structure-Activity Relationship