• Journal of Microbiology and Biotechnology
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• 제16권5호
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• pp.667-672
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• 2006

Tyrosinase is an enzyme that catalyzes the biosynthetic pathway of melanin pigments participating in the coloring of skin, hair, and eyes, and is widely distributed in nature. The inhibitory compounds of tyrosinase have been extensively used as a cosmetic agent with a skin-whitening effect. In this paper, several plant extracts were screened using Melan-a cells for the melanin biosynthesis inhibition activity, and Idesia polycarpa was selected. A melanin biosynthesis inhibitor was isolated from I. polycarpa fruits by activity-guided fractionation, and the inhibitor was identified as 6-hydroxy-2-[[[(1-hydroxy-6-oxo-2-cyclohexenl-yl)carbonyl]oxy]methyl]phenyl$\beta$-D-glucopyranoside (idescrapin) by comparing it with reported spectral data. Idescarpin $(IC_{50}=8{\mu}g/ml)$ reduced melanin content compared with the vehicle. In addition, the inhibitory activity of idescarpin for melanin synthesis is mediated by decreasing tyrosinase protein rather than directly inhibiting the tyrosinase activity. These results suggest that idescarpin isolated from I. polycarpa fruits may be used as a skin-whitening agent.

• Advances in Traditional Medicine
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• 제7권2호
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• pp.141-149
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• 2007

Madhuca indica has been used ethnomedically in Indian folks. In the present study we have investigated anti-inflammatory, anti-ulcer and hypoglycaemic effect of ethanolic extract (EE) and crude alkaloid extract of Madhuca indica seed cake on albino rats. The study showed that the EE had a significant, dose dependent anti-edematogenic, anti-ulcerogenic and hypoglycaemic activity, whereas the crude alkaloid extract exhibited a significant only. Both the extracts possess dose dependent inhibitory activity on carrageenan-induced edema, inhibiting prostaglandins or mediators involved in prostaglandin synthesis, the second phase of inflammation. The EE was significantly effective in protecting pylorus-ligation-induced gastric ulcers at a higher dose level. The active principle of EE seems to be a selective inhibitor of the COX II (prostaglandin synthesis) without important effect on COX I since, EE exhibited both anti-edematogenic and anti-ulcerogenic effect. The EE was effective in reducing the plasma glucose level in normal albino rats in a dose dependent manner, producing hypoglycaemic effect by stimulating the release of insulin from the ${\beta}-cells$ and/or increasing the uptake of glucose from the plasma.

• 대한의생명과학회지
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• 제15권3호
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• pp.179-185
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• 2009

In our previous report, we showed that $PPAR{\gamma}$ does not influence adipogenesis in females with functioning ovaries, indicating that $PPAR{\gamma}$ activity on adipogenesis is associated with sex-related factors. Among the sex-related factors, estrogen has been recognized as a major factor in inhibiting adiposgenesis in females. Thus, we hypothensized that $17{\beta}$-estradiol (E) inhibits 3T3-L1 cell adipogenesis by preventing $PPAR{\gamma}$ activity. E decreased triglyceirde accumulation in differentiated 3T3-L1 cells compared with control group. E also decreased the expression of $PPAR{\gamma}$ mRNA as well as $PPAR{\gamma}$ dependent adipocyte-specific genes, such as adipocyte fatty acid binding protein and tumor necrosis factor $\alpha$. In addition, E not only decreased luciferase reporter activity by $PPAR{\gamma}$, but also transfection of estrogen receptor $\alpha$ ($ER{\alpha}$) or $ER{\beta}$ led to decreases in $PPAR{\gamma}$ reporter gene activation. Moreover, E-activated ERs significantly decreased the luciferase reporter gene activation induced by $PPAR{\gamma}$ transfection, suggesting that estrogen-activated ERs inhibit $PPAR{\gamma}$-dependent transactivation. Accordingly, our results demonstrate that E inhibits the action of $PPAR{\gamma}$ on adipogenesis through E activated ER, providing evidence that lack of estrogen may potentiate $PPAR{\gamma}$ action on adipogenesis.

• Asian Pacific Journal of Cancer Prevention
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• 제13권4호
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• pp.1097-1104
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• 2012

Background/Aim: Pristimerin isolated from Celastrus and Maytenus spp can inhibit proteasome activity. However, whether pristimerin can modulate cancer metastasis is unknown. Methods: The impacts of pristimerin on the purified and intracellular chymotrypsin proteasomal activity, the levels of regulator of G protein signaling 4 (RGS 4) expression and breast cancer cell lamellipodia formation, and the migration and invasion were determined by enzymatic, Western blot, immunofluorescent, and transwell assays, respectively. Results: We found that pristimerin inhibited human chymotrypsin proteasomal activity in MDA-MB-231 cells in a dose-dependent manner. Pristimerin also inhibited breast cancer cell lamellipodia formation, migration, and invasion in vitro by up-regulating RGS4 expression. Thus, knockdown of RGS4 attenuated pristimerin-mediated inhibition of breast cancer cell migration and invasion. Furthermore, pristimerin inhibited growth and invasion of implanted breast tumors in mice. Conclusion: Pristmerin inhibits proteasomal activity and increases the levels of RGS4, inhibiting the migration and invasion of breast cancer cells.

• Advances in Traditional Medicine
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• 제6권3호
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• pp.167-173
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• 2006

A growing body of evidence supports lipid peroxidation as having a role in the pathogenesis of liver disease. Although the probable cause of damage to human hepatocytes may be multifactorial, free radicals have been implicated in a variety of liver diseases, particularly in the presence of iron overload and toxic substances such as ethanol. Consequently, antioxidants, particularly those of plant origin such as flavonoids, may help to reduce the risk of developing these diseases. Silybum (S.) marianum, a medicinal plant widely used in traditional European medicine for the treatment of liver disorders, was evaluated for antioxidant activity. Thin layer chromatography and High Performance Liquid Chromatography analyses of crude extract of the plant confirmed the presence of a number of flavonoids reported in the literature. The antioxidant activity of these flavonoids was measured through inhibition of lipid peroxidation and 1, 1-diphenyl-2- picrylhydrazyl radical scavenging. The crude plant extract showed marked antioxidant activity in both assays. These results suggest that S. marianum contains flavonoids with antioxidant activity, capable of inhibiting or scavenging free radicals, thus supporting its traditional use as a hepatoprotective agent.

• 동의생리병리학회지
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• 제17권5호
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• pp.1321-1324
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• 2003

To produce anti-malarial drugs, natural products were extracted from 18 species of marine algae by various mechanical methods. Twelve species of marine algae were found to have antiplasmodial activity by inhibiting the growth of the chloroquine-resistant Plasmodium falciparum strain FCR-3 with EC/sub 50/ values less than 100 ㎍/㎖. The methanol extract of Neoholmeria japonica had the strongest antiplasmodial activity with EC/sub 50/ value of 62 ㎍/㎖.

• 한국미생물·생명공학회지
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• 제24권5호
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• pp.624-629
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• 1996

The ethanol extracts from Angelica gigas Nakai and Angelica acutiloba Kitagawa were fractionated to diethyl ether and aqueous partitions. Both partitions had strong antimutagenic effect on the MNNG (N-methyl-N-nitro-N-nitrosoguanidine) by Ames mutagenicity test. Diethyl ether fractions exhibited the greatest antimutagenic effect suppressing the mutagenicity of MNNG with inhibition of 78-80%. The ethanol extracts from both species showed the inhibitory effect on the growth of several human cancer cell lines. Especially, the diethyl ether fraction from ethanol extracts was most effective on human hepatocellular carcinoma cells, inhibiting 90-95% of cell growth. However, the aqueous fractions had least inhibition activity on many cancer cells. There was little cytotoxicity on human normal liver cell by ethanol extracts. Diethyl ether fraction from Angelica gigas Nakai ethanol extract had cytotoxicity less than 20% on human normal liver cells, compared with that from Angelica acutiloba Kitagawa ethanol exract. The adding of 0.5 (g/l) of diethyl ether fractions of Angelica gigas Nakai or Angelica acutiloba Kitagawa increased immune activity by enhacing human B and T cells up to three to four times. It was proven that diethyl ether fraction (0.7 g/1) from Angelica gigas Nakai could control blood pressure by suppressing angiotensin converting enzyme activity up to 98%. From TLC, it was appeared that both of diethyl ether partitions had umbelliferon, known to one of active substances from Angelica gigas Nakai and Angelica acutiloba Kitagawa.

• BMB Reports
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• 제49권9호
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• pp.502-507
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• 2016

To examine the effect of TBMS1on breast cancer metastasis, and investigate the potential mechanism by which Tubeimoside-1 (TBMS1) inhibits the CXCR4 expression in breast cancer cells. The expression of CXCR4 in breast cancer cell lines was determined by immunoblotting and real-time PCR. The effect of TBMS1 on NF-κB binding activity was evaluated by EMSA assay and ChIP analysis. Cell proliferation and invasion were analyzed by MTT assay and transwell invasion assay, respectively. The effect of TBMS1 on breast cancer metastasis was further evaluated in a metastasis model of nude mice. TBMS1 suppressed the expression of CXCR4 through inhibition of NF-κB binding activity. TBMS1 inhibited CXCL12-induced invasion in breast cancer cells, while ectopic expression of CXCR4 abolished the inhibitive activity of TBMS1. TBMS1 suppressed breast cancer metastasis in the metastatic model of nude mice. TBMS1 suppressed the CXCR4-mediated metastasis of breast cancer by inhibiting NF-κB binding activity.

• Parasites, Hosts and Diseases
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• 제47권4호
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• pp.377-380
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• 2009

Growing patterns of pediculocidal drug resistance towards head louse laid the foundation for research in exploring novel anti-lice agents from medicinal plants. In the present study, various extracts of Pongamia pinnata leaves were tested against the head louse Pediculus humanus capitis. A filter paper diffusion method was conducted for determining the potential pediculocidal and ovicidal activity of chloroform, petroleum ether, methanol, and water extracts of P. pinnata leaves. The findings revealed that petroleum ether extracts possess excellent anti-lice activity with values ranging between 50.3% and 100% where as chloroform and methanol extracts showed moderate pediculocidal effects. The chloroform and methanol extracts were also successful in inhibiting nymph emergence and the petroleum ether extract was the most effective with a complete inhibition of emergence. Water extract was devoid of both pediculocidal and ovicidal activities. All the results were well comparable with benzoyl benzoate (25% w/v). These results showed the prospect of using P. pinnata leave extracts against P. humanus capitis in difficult situations of emergence of resistance to synthetic anti-lice agents.

• Biomolecules & Therapeutics
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• 제22권1호
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• pp.55-61
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• 2014

Panax ginseng is a medicinal herb that is used worldwide. Its medicinal effects are primarily attributable to ginsenosides located in the root, leaf, seed, and flower. The flower buds of Panax ginseng (FBPG) are rich in various bioactive ginsenosides, which exert immunomodulatory and anti-inflammatory activities. The aim of the present study was to assess the effect of 18 ginsenosides isolated from steamed FBPG on the transcriptional activity of NF-${\kappa}B$ and the expression of tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$)-stimulated target genes in liver-derived cell lines. Noticeably, the ginsenosides $Rk_3$ and $Rs_4$ exerted the strongest activity, inhibiting NF-${\kappa}B$ in a dose-dependent manner. SF and $Rg_6$ also showed moderately inhibitory effects. Furthermore, these four compounds inhibited the TNF-${\alpha}$-induced expression of IL8, CXCL1, iNOS, and ICAM1 genes. Consequently, ginsenosides purified from steamed FBPG have therapeutic potential in TNF-${\alpha}$-mediated diseases such as chronic hepatic inflammation.