• Korean Journal of Pharmacognosy
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• v.37 no.1 s.144
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• pp.33-36
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• 2006

The quantitative analytical method for the content of dioscin in Dioscorea rhizoma using a high performance liquid chromatography(HPLC) system was established for its quality control. After extracting Discorea rhizoma flour with ethanol, dioscin was separated though an ODS column with a flow rate of 1.0ml/min of acetonnitril-methanol-0.01 M phosphate buffer (pH 5.0)(6:3:1, v/v%), and the amount of dioscin was detected at 210nm. Relation time of dioscin in HPLC chromatogram were about $7.45{\pm}0.34\;min$ and calibration curve showed good linearity at concentrations from 0.1 to 2.0 mg/ml of dioscin. When 5 commercial Dioscorea rhizoma flours were analyzed by HPLC, the peak for dioscin was well separated from others in ethanol extract of Dioscorea rhizoma, and the amount of dioscin was in the range from 0.076 to 0.142(w/w)%.

• Korean Journal of Pharmacognosy
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• v.32 no.2 s.125
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• pp.153-156
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• 2001

The methods for isolation and quantitative determination of dioscin, a spirostanol triglycoside, from the roots of Smilax china have been developed. Isolation of dioscin was achieved by silica gel and RP-18 chromatography. The HPLC method used for quantitative determination of dioscin enabled the standardization of the crude drug. It suggests that the content of dioscin in Smilax china should be above 0.01%.

• Mass Spectrometry Letters
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• v.4 no.3
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• pp.55-58
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• 2013

Dioscin is a biologically active steroidal saponin with anticancer and hepatoprotective effects. A rapid, selective, and sensitive liquid chromatographic method with electrospray ionization tandem mass spectrometry was developed for the quantification of dioscin in rat plasma. Dioscin was extracted from rat plasma using ethyl acetate at acidic pH. The analytes were separated on a Halo C18 column using gradient elution of acetonitrile and 0.1% formic acid and detected by tandem mass spectrometry in selected reaction monitoring mode. The standard curve was linear ($r^2$ = 0.998) over the concentration range of 1-100 ng/mL. The lower limit of quantification was 1.0 ng/mL using 50 ${\mu}L$ of plasma sample. The coefficient of variation and relative error for intra- and inter-assay at four QC levels were 1.3 to 8.0% and -5.4 to 10.0%, respectively. This method was applied successfully to the pharmacokinetic study of dioscin after oral administration of dioscin at a dose of 29.2 mg/kg in male Sprague-Dawley rats.

• Korean Journal of Pharmacognosy
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• v.20 no.2
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• pp.76-82
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• 1989

Five known diosgenin glycosides have been isolated from the MeOH extract of Smilax china rhizomes and characterized as prosapogenin A of dioscin, dioscin, gracillin, methyl protogracillin, methyl protodioscin and its corresponding 22-hydroxy analog. This is the first isolation of the former four compounds from this plant. ${\beta}-Sitosterol\;glucoside$ was also isolated and identified.

• Archives of Pharmacal Research
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• v.17 no.4
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• pp.218-222
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• 1994

The natural product, spirostanol glycoside dioscin, was shown to directly inactivate human pleural fluid phospholipase $A_2{\;}(PLA_2)$ Inactivation was dose, and time dependent. The $IC_{50}$ was estimated at 18 .mu.M and virtually complete inactivation of the enzyme occurred at 50 .mu.M. Using Michaelis-Menten kinetics, dioscin inactivated the enzyme by a competitive inhibitory manner, the apparent Ki value was $6.9{\times}10_{-4}$. Reversibility was studied directly by dialysis method, the inhibition was reversible. Additioin of excess $Ca^{2+}$ concentration up to 8 mM did not antagonize the inhibitory activity of dioscin. Inactivation of several kinds of $PLA_2$ by dioscin is due to interaction with the active site of $PLA_2$ and may be a useful adjunt in the theraphy of inflammatory diseases.

• Korean Journal of Plant Resources
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• v.21 no.6
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• pp.444-448
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• 2008

An adventitious root formation protocol from Smilax china L. was established for in vitro production of dioscin, a steroidal saponin having various bioactivities such as anticancer, antifungal, antiviral, and antiobesity. Optimal medium for root initiation from leaf explant was MS medium containing $30\;g{\cdot}L^{-1}$ of sucrose supplemented with $1.0\;mg{\cdot}L^{-1}$ kinetin + $2.0\;mg{\cdot}L^{-1}$ NAA. The induction of adventitious roots from in vitro initiated root segments was most favorable to MS liquid medium with $0.1\;mg{\cdot}L^{-1}$ kinetin + $2.0\;mg{\cdot}L^{-1}$ NAA. Among the 20 different adventitious roots originated from different plants, strain No. 10 was selected based on production ability of dioscin, and its stability through the successive suspension culture. The maximum growth stage of adventitious roots was noticed at 5 weeks after subculture while that of dioscin production in the adventitious root was at 7 weeks after subculture in suspension culture system. These results provide that suspension culture of adventitious roots of Smilax china L. have a potential for in vitro mass production of dioscin.

• Journal of Microbiology and Biotechnology
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• v.20 no.6
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• pp.1011-1017
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• 2010

A novel dioscin-glycosidase that specifically hydrolyzes multi-glycosides, such as 3-O-${\alpha}$-L-($1{\to}4$)-rhamnoside, 3-O-${\alpha}$-L-($1{\to}2$)-rhamnoside, 3-O-${\alpha}$-L-($1{\to}4$)-arabinoside, and ${\beta}$-D-glucoside, on diosgenin was isolated from the Absidia sp.d38 strain, purified, and characterized. The molecular mass of the new dioscin-glycosidase is about 55 kDa based on SDS-PAGE. The dioscin-glycosidase gradually hydrolyzes either 3-O-${\alpha}$-L-($1{\to}4$)-Rha or 3-O-${\alpha}$-L-($1{\to}2$)-Rha from dioscin into 3-O-${\alpha}$-L-Rha-${\beta}$-D-Glc-diosgenin, further rapidly hydrolyzes the other ${\alpha}$-L-Rha from 3-O-${\alpha}$-L-Rha-${\beta}$-D-Glc-diosgenin into the main intermediate products of 3-O-${\beta}$-D-Glc-diosgenin, and subsequently hydrolyzes these intermediate products into aglycone as the final product. The enzyme also gradually hydrolyzes 3-O-${\alpha}$-L-($1{\to}4$)-arabinoside, 3-O-${\alpha}$-L-($1{\to}2$)-rhamnoside, and ${\beta}$-D-glucoside from [3-O-${\alpha}$-L-($1{\to}4$)-Ara, 3-O-${\alpha}$-L-($1{\to}4$)-Rha]-${\beta}$-D-Glc-diosgenin into diosgenin as the final product, exhibiting significant differences from previously reported glycosidases. The optimal temperature and pH for the new dioscin-glycosidase is $40^{\circ}C$ and 5.0, respectively. Whereas the activity of the new dioscin-glycosidase was not affected by $Na^+$, $K^+$, and $Mg^{2+}$ ions, it was significantly inhibited by $Cu^{2+}$ and $Hg^{2+}$ ions, and slightly affected by $Ca^{2+}$ ions.

• BMB Reports
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• v.40 no.6
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• pp.1016-1020
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• 2007

In this study, dioscin was isolated from Dioscoreae Rhizoma (DR), which is the rhizome of Dioscorea batatas DECNE. that inhabits broad areas of Korea and Japan. To determine whether dioscin induced growth hormone (GH) release, we evaluated its induction effects on GH release both in vitro and in vivo. The 70% methanol extract of DR, and its n-hexane and n-BuOH fractions, induced rat GH (rGH) release in rat pituitary cells 10-fold, 8-fold, and 5-fold higher than the control ($0.36{\pm}0.02 nM$), respectively (p < 0.05 each). The dioscin-induced rGH release of the cells was concentration-dependent and its $ED_{50}$ was $1.14{\times}10^{-5} M$. Within 90 minutes after intravenous administration of $10{\mu}g$/kg (p < 0.05 at $t_{max}$), dioscin caused the greatest increase in rGH concentration ($C_{max}$) in the rat plasma ($34.16{\pm}14.10 ng/ml$) (n = 4), which was twice as high as the control group ($12.88{\pm}3.29 ng/ml$) (n = 27).

• Journal of Plant Biotechnology
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• v.32 no.3
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• pp.217-223
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• 2005

Effects of growth regulators on growth of adventitious roots and accumulation of steroidal saponins, such as dioscin, prosapogenin A and prosapogenin C, in cultures of Dioscorea nipponica were determined. The maximum growth of adventitious roots was observed in MS medium supplemented with 30 g/L sucrose and 1.0 mg/L NAA. Addition of BA in combination with NAA appeared to be no effective in the growth of adventitious roots. Among the twenty different adventitious roots formed from different seeds, strain No. 10 was selected based on production ability of dioscin, and its stability through the successive liquid culture. During the first 4 weeks of incubation, contents of steroidal saponins in adventitious roots were negligible but the contents were markedly increased at 5 weeks of incubation. Dioscin and prosapogenin C content in IBA-treated adventitious roots were significantly higher than those in NAA-treated roots. However, content of prosapogenin A was not significantly different among NAA or IBA level. Results provide that liquid culture of adventitious roots of D. nipponica have a potential for mass production of dioscin including prosapogenin A and prosapogenin C.

• Korean Journal of Pharmacognosy
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• v.24 no.3
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• pp.187-191
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• 1993

Three compounds were isolated from the rhizomes of Dioscorea quinqueloba and identified as $diosgenin\;3-O-{\alpha}_-L-rhamnopyranosyl(1{\rightarrow}2)-{\beta}-_D-glucopyranoside$, dioscin and gracillin by chemical and spectroscopic means.