• Natural Product Sciences
• /
• 제8권2호
• /
• pp.35-43
• /
• 2002

Glycosides of herbal medicines, such as glycyrrhizin, ginsenosides, kalopanaxsaponins, rutin and ponicirin, were studied regarding their metabolic fates and pharmacological actions in relation to intestinal bacteria using germ-free, gnotobiotic and conventional animals. When glycyrrhizin (GL) was orally administered, $18{\beta}-glycyrrhetinic\;acid\;(GA)$, not GL, was detected in plasma and intestinal contents of gnotobiotic and conventional rats. However, GA could not be detected in germ-free rats. When GL was incubated with human intestinal bacteria, it was directly metabolized to GA (>95%) or via $18{\beta}-glycyrrhetinic\;acid-3-{\beta}-D-glucuronide$(>5%). Orally administered GL was effective in gnotobiotic and conventional rats for liver injury induced by carbon tetrachloride, but was not effective in germ-free rats. When ginseng saponins were orally administered to human beings, compound K in the plasma was detected, but the other protopanxadiol saponins were not detected. The compound K was active for tumor metastasis and allergy. When kalopanaxsaponins were incubated with human intestinal microflora, they were metabolized to kalopanaxsaponin A, kalopanaxsaponin I and hederagenin. These metabolites were active for rheumatoid arthritis and diabetic mellitus while the other kalopanxsaponins were not. When flavonoid glycosides were orally administered to animals, aglycones and/or phenolic acids were detected in the urine. The metabolic pathways proceeded by intestinal bacteria rather than by liver or blood enzymes. These metabolites, aglycones and phenolic acids, showed antitumor, antiinflammatory and antiplatelet aggregation activities. These findings suggest that glycosides of herbal medicines are prodrugs.

• 공업화학
• /
• 제17권3호
• /
• pp.286-290
• /
• 2006

새로운 4급 염화 암모늄염, {alkyldimethyl-[5-(2-phenylthiazol-4-yl]-1,3,4-oxadiazol-2-ylmethyl]quaternary ammonium chlorides (ADOQACs): 6}을 화합물 5와 몇 가지 N,N-dimethylalkyl amine을 반응시켜 합성하였다. 합성한 화합물들의 구조와 물리적 특성을 조사하였고 계면활성을 측정하였다. 화합물 6의 표면장력($\gamma_{cmc}$)과 최소저해농도(MIC)는 알킬기의 영향을 받은 것으로 나타났으며, 특히 화합물 6c와 6d가 좋은 항균력과 계면활성을 보였다.

• Food Science and Biotechnology
• /
• 제16권2호
• /
• pp.218-222
• /
• 2007

The anticoagulant properties of Cinnamomum cassia bark-derived materials were evaluated against platelet aggregation induced by arachidonic acid (AA), collagen, platelet activating factor (PAF), or thrombin, and these effects were then compared to those of three commercially available compounds (cinnamic acid, cinnamyl alcohol, and aspirin). The active constituent obtained from C. cassia barks was isolated by silica gel column chromatography and high pressure liquid chromatography (HPLC), and was characterized as trans-cinnamaldehyde by MS, $^1H-NMR$, $^{13}C-NMR$, and IR spectroscopy. With regard to 50% inhibitory concentration ($IC_{50}$) values, cinnamaldehyde was found to effectively inhibit platelet aggregation induced by AA ($IC_{50},\;43.2\;{\mu}M$) and collagen ($IC_{50},\;3.1\;{\mu}M$). By way of comparison, cinnamaldehyde proved to be a significantly more potent platelet inhibitor against platelet aggregation induced by collagen than aspirin. The effect exerted by cinnamaldehyde against platelet aggregation induced by AA was 1.2 times less than that of aspirin. These results indicate that cinnamaldehyde may prove useful as a lead compound for the inhibition of platelet aggregation induced by AA and collagen.

• Archives of Pharmacal Research
• /
• 제27권5호
• /
• pp.495-501
• /
• 2004

A series of N-substituted-1,3-isoindolinedione derivatives (2-16) were synthesized for the purpose of defining the effect of N-substitution on the anticonvulsant activity of these derivatives. The target compounds (2-16) were obtained by condensation of phthalic anhydride with the corresponding amine derivative. The structures of the synthesized derivatives (2-16) were confirmed by means of IR, $^1$H-NMR, $^{13}$ C-NMR, MS and elemental analyses. The anticonvulsant activity of all compounds (2-16) were evaluated by subcutaneous pentylenetetrazole seizure threshold test at doses of 0.2, 0.4 and 0.8 mmol/kg compared with sodium valproate as a positive control. Their neurotoxicity were determined by the rotorod test. Many of the present series of compounds showed good anticonvulsant activity at the tested doses, as compared to sodium valproate. Three of them (4, 6 and 11) exhibited 100 % protection against convulsions, neurotoxicity and death at all tested doses. Out of the series, two compounds (12 and 13) were completely inactive with 100% mortality. 3-(p-chlorophenyl)-4-(1 ,3-dioxo-2,3-dihydro-1 H-2-isoindolyl) butanoic acid derivative (11) has emerged as the most active compound which is 20 times more active than valproate with ED$_{50}$ 8.7, 169 mg/kg; TD$_{50}$ 413, 406 mg/kg and PI 47.5, 2.4. The results revealed the importance of the combination of baclofenic and phthalimide moieties (compound 11) as a promising anticonvulsant candidate.

• Korean Journal of Acupuncture
• /
• 제20권4호
• /
• pp.53-63
• /
• 2003

Objective : Experimental studies were done to research the clinical effects of Herba Patriniae(HP) aqua-acupuncture ($BL_{13},\;BL_{17},\;BL_{13}{\cdot}BL_{17}$ and free points) on the anti-allergic inflammatory response. Methods : We measured active systemic anaphylatic shock induced by compound 48/80 and microvascular permeability increased by acetic acid. And we measured total IgE and plasma WBC level, serum total protein, albumin, immunoglobulin and NO levels induced by egg albumin. Results : HP aqua-acupuncture pretreatments at all acupoints inhibited active systemic anaphylatic shock induced by compound 48/80 and microvascular permeability increased by acetic acid. Total IgE and plasma WBC level inhibited by HP aqua-acupuncture pretreatment at $BL_{13}\;BL_{17}$ and free points. However, HP aqua-acupuncture didn't effect serum total protein, albumin, immunoglobulin and NO levels. Conclusion : These results suggest that HP aqua-acupuncture may be beneficial in the regulation of type Ⅰ allergic reaction, but is further required immunological studies on the allergic reaction.

• Journal of Microbiology and Biotechnology
• /
• 제27권2호
• /
• pp.242-250
• /
• 2017

Anti-photoaging effects of standardized Siegesbeckia glabrescens extract (SGE) and its major active compound kirenol were investigated using Hs68 human dermal fibroblasts and hairless mice, respectively. UVB-irradiated hairless mice that received oral SGE (600 mg/kg/day) showed reduced wrinkle formation and skinfold thickness compared with the UVB-irradiated control. Furthermore, SGE treatment increased the mRNA levels of collagen synthesis genes (COL1A1, COL3A1, COL4A1, and COL7A1) and activated antioxidant enzyme (catalase), while suppressing matrix metalloproteinase (MMP-2, -3, -9, and -13) expression. In Hs68 fibroblasts, kirenol also significantly suppressed MMP expression while increasing the expression of COL1A1, COL3A1, and COL7A1. Collectively, our data demonstrate that both SGE and kirenol attenuated UVB-induced photoaging in hairless mice and fibroblasts through inhibition of the mitogen-activated protein kinases and nuclear factor kappa B pathways, suggesting that SGE has potential to serve as a natural anti-photoaging nutraceutical.

• 한국식품영양과학회지
• /
• 제30권4호
• /
• pp.726-731
• /
• 2001

밤 가공공장에서 폐기되고 있는 밤의 귀피를 항산화 기능성 자원으로 활용하고자 밤 귀치의 methanol 추출물 및 용매획분을 benzoic acid 수산화법으로 hydroxyl radical 소거능과 ferric thiocyanate법으로 과산화물생성 억제능을 시험하였다. 대부분의 획분에서 항산화성을 보였으며 특히 ethyl acetate 획분에서 BHA나 $\alpha$-tocopherol과 거의 유사한 rkdgkshydroxyl radical 소거능과 지질과산화물생성 억제능을 보였다. Ethyl acetate 획분으로부터 항산화성 물질을 분리하기 위하여 Sephadex LH-20 column chromatography 및 prep HPLC를 행하여 단일 물질로 정제하였다. 분리 정제된 물질을 $^{1}$H-NMR과 $^{13}$C-NMR로 구조 분석한 결과 gallic acid로 동정하였다. 페놀산을 GC로 분석한 결과 밤 귀피의 주요 페놀산으로 ellagic acid(172.22 mg%) 와 gallic acid(107.39 mg%)가 확인되었다.

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

• 한국균학회지
• /
• 제26권1호통권84호
• /
• pp.78-85
• /
• 1998

전국 각지에서 채집한 사멸곤충에서 분리한 곤충 기생성 진균이 생산하는 살충성 생리활성물질을 탐색한 결과 곰팡이 분리주 CNAB-63 균주가 목화진딧물과 점박이응애 모두에 대해 다른 분리균주들보다 비교적 높은 살충효과를 보인 바, 본 균주가 생산하는 살충성분을 각종 chromatography로 분리 정제하였다. 정제된 활성물질 CNAB는 점박이응애에서 66.59%, 목화진딧물에서 52.96%의 살충효과를 보였으며, 그 외에도 온실가루이에 살충효과를 보였으나 배추좀나방에는 미미한 살충효과를 보였다. 한편 활성물질 CNAB는 $100\;{\mu}g/disk$ 농도에서 곰팡이, 효모, 세균류에 전혀 항균활성을 보이지 않았다.

• Biomolecules & Therapeutics
• /
• 제27권3호
• /
• pp.276-282
• /
• 2019

${\beta}$-amyloid precursor protein (APP) can be cleaved by ${\alpha}$-, and ${\gamma}$-secretase at plasma membrane producing soluble ectodomain fragment ($sAPP{\alpha}$). Alternatively, following endocytosis, APP is cleaved by ${\beta}$-, and ${\gamma}$-secretase at early endosomes generating ${\beta}$-amyloid ($A{\beta}$), the main culprit in Alzheimer's disease (AD). Thus, APP endocytosis is critical for $A{\beta}$ production. Recently, we reported that Monsonia angustifolia, the indigenous vegetables consumed in Tanzania, improved cognitive function and decreased $A{\beta}$ production. In this study, we examined the underlying mechanism of justicidin A, the active compound of M. angustifolia, on $A{\beta}$ production. We found that justicidin A reduced endocytosis of APP, increasing $sAPP{\alpha}$ level, while decreasing $A{\beta}$ level in HeLa cells overexpressing human APP with the Swedish mutation. The effect of justicidin A on $A{\beta}$ production was blocked by endocytosis inhibitors, indicating that the decreased APP endocytosis by justicidin A is the underlying mechanism. Thus, justicidin A, the active compound of M. angustifolia, may be a novel agent for AD treatment.