• 약학회지
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• 제42권6호
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• pp.634-638
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• 1998

The effects of MeOH extracts from 88 herbal medicines on monoamine oxidase (MAO) acitivity were investigated. MAO was purified from mouse brain and its activity was determined by fluorospectrophotometer using kynuramine as a substrate. The $K_m\;and\;V_{max}$ values (n=4) of MAO were $78.2{\pm}4.0\;{\mu}M$ and $0.65{\pm}0.05$ nmol/min/mg protein, respectively. Four MeOH extracts from Melilotus sauvelolens, Eupatorium lindleyanum Bupleurum longiradiatum and Sorbaria sirbiforia showed a strong inhibitory effect with less than $100{\mu}g/ml$ in their $IC_{50}$ values on MAO activity. Six MeOH extracts including Agastache rugosa showed a mild inhibitory effect with 100~200${\mu}$g/ml in their $IC_{50}$ values. Twenty-two MeOH extracts including Melandryum seoulense exhibited a week inhibition of MAO activity with 200~300${\mu}$g/ml in their $IC_{50}$ values.

• Natural Product Sciences
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• 제24권2호
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• pp.93-98
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• 2018

Medicinal plants are potential sources of anticancer agents screening. A large number of phytochemicals, including triterpenoids, have been reported to have significant cytotoxic effects on cancer cells. From the fruits of Ligustrum japonicum Thunb., thirteen triterpenoids (1 - 13) were isolated and evaluated for their cytotoxic activity against Hela and HL-60 cells. As results, 8 (oleanolic acid) showed significant effects on Hela with $IC_{50}$ values of $5.5{\mu}M$, and moderate effects on HL-60 cells with $IC_{50}$ values of $55.9{\mu}M$. Meanwhile, 10 (oleanderic acid) and 11 ($3{\beta}$-acetoxy-urs-12-en-28-oic acid) exhibited moderate inhibitory effects on Hela with $IC_{50}$ value of 55.0 and $68.8{\mu}M$, respectively. Moreover, 10 showed cytotoxic effect on HL-60 cell line with $IC_{50}$ value of $63.9{\mu}M$. To our knowledge, this is the first report that oleanderic acid was isolated from L. japonicum and investigated in cytotoxic effects on Hela and HL-60 cells.

• Advances in Traditional Medicine
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• 제8권1호
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• pp.86-92
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• 2008

The aim of the study was to evaluate in vitro antioxidant and cytotoxic activities of the methanolic extracts of leaves of Solanum sisymbrifolium, Solanum anguivi multiflora, Solanum barbisetum and Solanum jasminoides. In the in vitro antioxidant screening using ABTS [2,2'-azino-bis (3-ethylbenzo-thiazoline-6-sulphonic acid) diammonium salt] method, the methanol extracts of Solanum jasminoides, Solanum barbisetum and Solanum anguivi multiflora exhibited potent antioxidant activity with $IC_{50}$ values 31.25 $\pm$ 0.35, 40.33 $\pm$ 0.57 and 54.33 $\pm$ 0.57 ${\mu}g$/ml, respectively. Solanum barbisetum also showed potent activity in DPPH [1,1-diphenyl-2-picryl hydrazyl] method with an $IC_{50}$ value of 55.33 $\pm$ 1.66 ${\mu}g/ml. In the cytotoxicity studies, the methanol extract of Solanum barbisetum exhibited moderate activity against Vero, HEp-2, HeLa and A-549 cell lines with $IC_{50}$ values in the range of 83.30 - 127.30 ${\mu}g$/ml. Solanum anguivi multiflora extract also showed moderate activity against Hep-2 cell line with $IC_{50}$ value of 80.13 ${\mu}g$/ml. Solanum barbisetum possessing both the activities requires further investigation.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1998년도 Advances in Ginseng Research - Proceedings of the 7th International Symposium on Ginseng -
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• pp.216-223
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• 1998

Cyclic nucleotide phosphodiesterases (PDEs) represent the unique enzymatic system degrddinf cAMP and cGMP which play a major role in the regulation of cell physiology. To investigate a possible molecular mechanism of ginsenosides, their activities were evaluated on PDEs which are recently described is new therapeutic targets. PDEs are classified into 7 families according to their genes (PDEI to PDE7) and are differently distributed in tissues. The IC50 values of ginsenosides were determined on PDEI to PDE 5 chromatographically isolatetl from bovine aorta. The results show that total ginseng saponin extract preferentially inhibits PDE 1 and PDE4 at concentrations nearby 200 ug/ml. Protopanaxadiol (PPD) fraction acts preferentially on PDE4 with and IC50 value of 100 nlml and inhibits also PDEI and PDE5 at 14 to 2 fold higher concentrations, respectively. Protopanaxatriol (PPT) fraction preferentially inhibits PDE 1 with and IC50 value of 170 ug/ml. Compound Rgl, originated from PPT fraction, and RC3 (5) represent the most active compounds towards PDE 1 with IC50 values around 80 UM. However Rg3 (R), epimer of Rgl (5) has no effect on the various PDEs tested, excepted on PDE3 rich is sligthly sensitive Compound Rbl, originated from PPD, acts on both PDEI and PDE4. It if two fold less active than Rgl and Rg3 (5) on PDEI. Taken together, these results mainly suggest that PDEI and PDE4 inhibitions could be a molecular mechanism which would participate in ginsenoside mechanisms, especially the effect of PPD on blood vessel and on CNS.

• Archives of Pharmacal Research
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• 제28권2호
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• pp.190-194
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• 2005

In our search for monoamine oxidase (MAO) inhibitors from natural resources, we found that the methanol extract of the roots of Sophora flavescens showed an inhibitory effect on mouse brain monoamine oxidase (MAO). Bioactivity-guided isolation of the extract yielded two known flavonoids, formononetin (1) and kushenol F (2), as active compounds along with three inactive compounds, oxymatrine (3), trifolirhizin (4), and ${\beta}$-sitosterol (5). Formononetin (1) and kushenol F (2) showed significant inhibitory effects on MAO in a dose-dependent manner with $IC_{50}$ values of 13.2 and $69.9\;{\mu}M$, respectively. Formononetin (1) showed a slightly more potent inhibitory effect against MAO-B ($IC_{50}:\;11.0\;{\mu}M$) than MAO-A ($IC_{50}:\;21.2\;{\mu}M$). Kushenol F (2) also preferentially inhibited the MAO-B activity than MAO-A activity with the $IC_{50}$ values of 63.1 and $103.7\;{\mu}M$, respectively.

• Natural Product Sciences
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• 제16권2호
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• pp.68-74
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• 2010

Phytochemical investigation on the ethyl acetate and n-butanol fractions of Moutan Cortex resulted in the isolation and characterization of a new monoterpene glycoside (3) and twenty known monoterpene glycosides (1, 2, 4-21). The structure of 3 was determined by spectroscopic data interpretation and physico-chemical properties. Compounds 1 and 8 presented a remarkable inhibitory activity against lipoxygenase-1 (LOX-1) with $IC_{50}$ values of 45.2 and $37.5\;{\mu}M$, respectively. Compounds 9, 10, 13, 18, 19, and 21 showed significant 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging effect with $IC_{50}$ values of 9.8, 25.5, 6.4, 15.2, 18.7, and $23.7\;{\mu}M$, respectively. Benzoylpaeoniflorin (8), which exhibited the highest inhibitory effect with an $IC_{50}$ value of $37.5{\pm}0.7{\mu}M$, was further analyzed the inhibition kinetics by Lineweaver-Burk plots. Results indicated that 8 is a non-competitive inhibitor, and the kinetic parameter values were estimated to be ($31.04\;{\mu}M$, Ki), ($0.29\;{\mu}M/min$, $V_m$), and ($48.50\;{\mu}M$, $K_m$).

• Journal of Radiation Protection and Research
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• 제25권4호
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• pp.183-190
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• 2000

본 연구에서는 천연 약용작물 추출물을 대상으로 하여 산화적 스트레스 하에서 상피세포암 세포 생장억제의 상승효과를 검색하였다. 한국인 호발암인 간암, 위암 및 대장암 등에 효과가 있다고 보고된 총 51 종의 천연 약용작물을 선정하여 메탄올 추출물 시료를 제조하고 , 과산화수소에 의해 유도된 산화적 스트레스 하에서 이 추출물의 암세포생장억제상승효과를 검색하였다. 사용된 51종의 시료 중 27 시료가 다양한 정도의 활성을 나타내었다. 활성이 나타난 27 시료 중 고련피, 곽향, 노나무, 도인, 방기, 백두웅, 백화사설초, 전호, 오미자, 조각자, 천궁의 11시료에서 산화적 스트레스 부가시 $IC_{50}$ 값이 50% 이상 감소되었으며, 다른 16 시료엣 50-25%의 $IC_{50}$ 값의 감소가 나타났다. 우수한 상승효과를 나타낸 11 시료는 산화적 스트레스에 용량 의존적인 상승효과를 나타내었다. 그 중 가장 우수한 상승효과를 나타낸 시료는 노나무(Catalpa ovata)로서 과산화수소수 75 및 100 uM을 가하여 산화적 스트레스를 부가하였을 때 각각 61 및 28%의 $IC_{50}$ 값의 감소를 초래하였다. 그 외 고련피, 곽향, 도인, 백두옹, 오미자 등이 우수한 효과를 나타내었다.

• Natural Product Sciences
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• 제18권1호
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• pp.47-51
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• 2012

Among 38 Vietnamese medicinal plant extracts investigated for their ${\alpha}$-glucosidase inhibitory activity, 35 extracts showed $IC_{50}$ values below $250{\mu}g/mL$. The MeOH extracts of the heartwood of Oroxylum indicum, the seeds of Caesalpinia sappan, and the fruits of Xanthium strumarium exhibited strong ${\alpha}$-glucosidase inhibitory activity with $IC_{50}$ values less than $50{\mu}g/mL$. Fractionation of the MeOH extract of the heartwood of O. indicum led to the isolation of oroxylin A (1), oroxyloside (2), hispidulin (3), apigenin (4), ficusal (5), balanophonin (6), 2- (1-hydroxymethylethyl)-4H,9H-naphtho[2,3-b]furan-4,9-dione (7), salicylic acid (8), p-hydroxybenzoic acid (9), protocatechuic acid (10), isovanillin (11), and ${\beta}$-hydroxypropiovanillon (12). Compounds 1 - 3, 5, 6, 8, 10, and 12 showed more potent activities, with $IC_{50}$ values ranging from 2.13 to $133.51{\mu}M$, than a positive control acabose ($IC_{50}$, $241.85{\mu}M$). The kinetic study indicated that oroxyloside (2) displayed mixed-type inhibition with inhibition constant (Ki) was $3.56{\mu}M$.

• Natural Product Sciences
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• 제16권4호
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• pp.239-244
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• 2010

Protein tyrosine phosphatase 1B (PTP1B), a negative regulator of insulin signaling, has served as a potential drug target for the treatment of type 2 diabetes. The MeOH extracts of twenty-nine medicinal plants, traditionally used in Vietnam as anti-diabetes agents, were investigated for PTP1B inhibitory activity in vitro. The results indicated that, most materials showed moderate to strong inhibitory activity with $IC_{50}$ values ranging from $3.4\;{\mu}g/mL$ to $35.1\;{\mu}g/mL$; meanwhile, eleven extracts (37.9%) could demonstrate PTP1B activity with $IC_{50}$ values less than $15.5\;{\mu}g/mL$; sixteen extracts (55.2%) could demonstrate PTP1B activity with $IC_{50}$ values ranging from $15.5\;{\mu}g/mL$ to $35.1\;{\mu}g/mL$. The study may provide a proof, at least in a part, for the ethno-medical use in diabetes disease of these plants.

• 약학회지
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• 제45권3호
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• pp.310-319
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• 2001

To compare skin irritation and cytotoxicity of anti-wrinkle agents, we examined skin irritation of six anti-wrinkle agents (ascorbic acid, glycolic acid, all trans-retinoic acid, ginseng extract, retinol, EB) in New Zealand white rabbit. Cytotoxicity of these agents was determined by MTT [tetrazolium salt 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide] at multi-time points in cultured HaCaT cell, a human immortalized keratinocyte cell. We then analyzed correlation between skin irritation and cytotoxicity by spearman's rank correlation analysis. All trans-retinoic acid showed the highest primary irritation index (0.92) in skin irritation test. Being all the six agents not irritant, retinal showed the most cytotoxic agents. The correlation between skin irritation and cytotoxicity ($IC_{50}$/ at different time point was 0.814, 0.757, 0.814 and 0.7 at 3, 24, 48 and 72 h, respectively. We also fecund that IC$_{20}$ and IC$_{80}$ of these agents showed similar correlation with skin irritation. These results therefore demonstrated that there is close correlation between skin irritation and cytotoxicity $IC_{50}$/ value by MTT in HaCaT cell at early time points by anti-wrinkle agents or IC$_{20}$ value. $IC_{50}$/ at earily time point or IC$_{20}$ values may be reliable alternative determinant of skin irritation.n.