• Natural Product Sciences
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• v.24 no.2
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• pp.82-87
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• 2018

Silymarin is the standardized extract from Silybum marianum which consists mainly of flavonoids and polyphenols. It is highly regarded for its hepatoprotective ability. Silybin B is a flavonolignan and one of the active components of silymarin. The content of silybin B in various parts of S. marianum was analyzed by HPLC-UV. Results show that the extract of seeds contain the highest amount of silybin B (7.434 mg/g DW). The petioles of S. marianum showed a low content of silybin B. This study revealed that seeds of S. marianum contain high amount of silybin B and could be a good source of the compound.

• Natural Product Sciences
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• v.12 no.3
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• pp.166-173
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• 2006

Silymarin is an antihepatotoxic substance isolated from the fruits of silybum mariamum. Possibly due to their antioxidant and membrane stabilizing properties, the compounds was shown to protect various organs and cells against a number of insults (Kvasnicka et al., 2003). Among the main silymarin components, [silybin($SB_A,\;SB_B$, isosilybin ($ISB_A,\;ISB_B$) silydianin (SD) and silychristin (SC)], silybin is the major pharmacologically active compound. Korean Pharmaceutical Codex (2nd ed.) describes silybin as the main substance of Cardus Marianus extract as supportive treatment of chronic inflammatory liver disorders. The aim of this work was to analyze silybin from various preparations containing cardus marianus extract, nicotinamide, and riboflavin (CNR). Nine commercial products were tested using reversed-phase HPLC-PDA assay. The limits of detection and quantification were $0.2\;{mu}g/ml$ and $1\;{mu}g/ml$, respectively. Calibration curve showed a good linearity ($r^2$=1.00000) in the range of $1{\sim}500\;{\mu}g/ml$ of silybin standard solutions.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.2
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• pp.151-158
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• 2009

We found that silymarin exhibited the inhibitory effect on melanogenesis in a spontaneously immortalized mouse melanocyte cell line, Mel-Ab. Silymarin is a standardized extract obtained from the dried seeds of milk thistle (Silybum marianum Gaertn.). Silymarin significantly prevented melanin production in a dose-dependent manner with an $IC_{50}$ value of 28.2 ${\mu}g/mL$ without effects on cell viability. Also, silymarin inhibited tyrosinase activity in melanocyte, while it did not affect the catalytic activity of cell-free tyrosinase. Furthermore, Western blot analysis indicated that silymarin decreased the expression of tyrosinase protein. Silybin A/B and isosilybin A/B were also able to inhibit melanin production and tyrosinase expression in protein level. Double blind study on the clinical efficacy of a cream containing 2 % silymarin showed that silymarin have a significant skin whitening effect. Therefore, this study suggests that silymarin may be useful as a natural skin whitening agent.

• Korean Journal of Pharmacognosy
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• v.38 no.2 s.149
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• pp.176-180
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• 2007

Five liglans, sauchinone (1), di-0-methyltetrahydrofuriguaiacin B (2), manassantin A (3), manassantin B (4) and saucerneol B (5), have been isolated from the MeOH extract of Saururus chinesis roots. The evaluation for protective effect of compounds 1-5 against tacrine-induced cytotoxicity in human liver-derived Hep G2 cells was conducted. Compounds 1,2, and 5 showed significant protective effects with the EC$_{50}$ values of74.2${\pm}$0.9, 111.3${\pm}$0.8,64.3${\pm}$0.8 ${\mu}$M, respectively. Silybin, one of the well-known hepatoprotective agents, used as a positive control, and also showed protective effect with an EC$_{50}$ value of 86.2${\pm}$0.5 ${\mu}$M.

• Biomolecules & Therapeutics
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• v.8 no.3
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• pp.269-275
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• 2000

Silibinin(silybin) is the active component of silymarin from Silybum marianum and has hepato-protective effect. It is water-insoluble and has low bioavailability. To improve its bioavailability, self-micro-emulsifying drug delivery system (SMEDDS) has been developed by Hanmi Pharmaceutical Company (Silyma $n^{R}$ 140 soft capsule). In this study, the pharmacokinetic profiles of Silyma $n^{R}$ were examined and compared it with a reference preparation, L Caps140 of B Pharmaceutical Company. This study was approved by Yonsei University Severance Hospital IRB(approval No. CR0004) and followed the bioequivalence test guideline of Korean FDA. Eighteen healthy adult volunteers were allocated based on 2$\times$2 Latin square cross-over design. They were given 2 capsules (each contains silymarin 140 mg (60 mg as silibinin)) of either drug at each period and crossed over after a week of drug-free washout period. Blood concentration of silibinin was measured by HPLC. The $C_{max}$ and AUC of the Silyma $n^{R}$ were 1542.0 $\pm$ 402.7 ng/ml and 3323.3 $\pm$ 824.7 ng.h/ml, respectively, and were significantly higher than those of reference preparation. The Tmax was 0.8 $\pm$ 0.3 h and significantly shorter than reference preparation. The $K_{e}$ and $T_{1}$2/ of both drugs were comparable. Percent differences in means against reference preparation were +88.3% for AUC, +222.6% for $C_{max}$, and -61.1% for $T_{max}$./.>././.>./.

• Korean Journal of Pharmacognosy
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• v.44 no.3
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• pp.209-219
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• 2013

Heat shock protein 90 (Hsp90) is a molecular chaperone that assists protein folding and contributes to the stability of various proteins. It also stabilizes a number of proteins involved in tumor growth to consider it as a promising target for the treatment of cancer. Natural products have been a rich source of agents of value in medicine, therefore discovering lead compounds from them is one of important strategy in the drug development. In this regard, geldanamycin, radicicol, novobiocin and celastrol have been utilized as leads for the development of Hsp90 inhibitory anticancer agents. This review summerizes recent findings of natural products as Hsp90 inhibitiors. The Hsp90 inhibitory activities, mode of actions on Hsp90 and cytotoxicities on human cancer cell lines of natural products including bulgarialactone B, curcumin, (-)-gambogic acid, quercetin, sansalvamide A, silybin, and withaferin A were discussed.

• Parasites, Hosts and Diseases
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• v.61 no.4
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• pp.449-454
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• 2023

Free-living amoebae (FLA) rarely cause human infections but can invoke fatal infections in the central nervous system (CNS). No consensus treatment has been established for FLA infections of the CNS, emphasizing the urgent need to discover or develop safe and effective drugs. Flavonoids, natural compounds from plants and plant-derived products, are known to have antiprotozoan activities against several pathogenic protozoa parasites. The anti-FLA activity of flavonoids has also been proposed, while their antiamoebic activity for FLA needs to be emperically determined. We herein evaluated the antiamoebic activities of 18 flavonoids against Naegleria fowleri and Acanthamoeba species which included A. castellanii and A. polyphaga. These flavonoids showed different profiles of antiamoebic activity against N. fowleri and Acanthamoeba species. Demethoxycurcumin, kaempferol, resveratrol, and silybin (A+B) showed in vitro antiamoebic activity against both N. fowleri and Acanthamoeba species. Apigenin, costunolide, (-)-epicatechin, (-)-epigallocatechin, rosmarinic acid, and (-)-trans-caryophyllene showed selective antiamoebic activity for Acanthamoeba species. Luteolin was more effective for N. fowleri. However, afzelin, berberine, (±)-catechin, chelerythrine, genistein, (+)-pinostrobin, and quercetin did not exhibit antiamoebic activity against the amoeba species. They neither showed selective antiamoebic activity with significant cytotoxicity to C6 glial cells. Our results provide a basis for the anti-FLA activity of flavonoids, which can be applied to develope alternative or supplemental therapeutic agents for FLA infections of the CNS.

• Journal of Life Science
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• v.27 no.4
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• pp.442-449
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• 2017

We analyzed the content of total phenolic and silymarin compounds of Cirsium japonicum (CJ), and its antioxidant activities and Liver protective effects were compared with those of Silybum marianum (SM). The total phenolic content in the aerial part ($97.22{\pm}5.51mg/g$) of CJ is higher than that in the underground part ($85.32{\pm}3.06mg/g$). The total silymarin content of CJ was 55.56% of SM, with the underground part ($0.47{\pm}0.03mg/g$) having higher content than the aerial part ($0.18{\pm}0.02mg/g$). The antioxidant activity of CJ was generally slightly lower than that of milk thistle, and the underground part of CJ generally had higher activity compared to the aerial part. When CJ extracts were processed at 1 mg/ml, DPPH activities were $83.76{\pm}0.60$ and $88.28{\pm}0.17%$, and FRAP activities were $77.63{\pm}0.70$ and $82.83{\pm}0.39%$ for extracts from aerial part and underground part, respectively. ABTS activities were $68.60{\pm}1.24$ and $63.41{\pm}0.57%$ for underground and aerial part respectively when extracts were processed at 0.1 mg/ml. The Liver protective effects of CJ were higher in the extracts from underground part compared to the aerial part, Liver cells were damaged by treating them with t-BHP, $H_2O_2$ and Ethanol, and then they were treated with 0.2 mg/ml CJ extracts. The survival rates of the damaged liver cells were $49.58{\pm}0.34$, $76.87{\pm}1.10$ and $71.73{\pm}0.58%$ respectively, which were higher than the cells not treated with extracts.