• Preventive Nutrition and Food Science
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• 제20권1호
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• pp.15-21
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• 2015

The skin plays a key role in protecting the body from the environment and from water loss. Cornified envelope (CE) and natural moisturizing factor (NMF) are considered as the primary regulators of skin hydration and barrier function. The CE prevents loss of water from the body and is formed by cross-linking of several proteins. Among these proteins, filaggrin is an important protein because NMF is produced by the degradation of filaggrin. Proteases, including matriptase and prostasin, stimulate the generation of filaggrin from profilaggrin and caspase-14 plays a role in the degradation of filaggrin. This study elucidated the effects of an ethanol extract of Boesenbergia pandurata (Roxb.) Schltr., known as fingerroot, and its active compound panduratin A on CE formation and filaggrin processing in HaCaT, human epidermal keratinocytes. B. pandurata extract (BPE) and panduratin A significantly stimulated not only CE formation but also the expression of CE proteins, such as loricrin, involucrin, and transglutaminase, which were associated with $PPAR{\alpha}$ expression. The mRNA and protein levels of filaggrin and filaggrin-related enzymes, such as matriptase, prostasin, and caspase-14 were also up-regulated by BPE and panduratin A treatment. These results suggest that BPE and panduratin A are potential nutraceuticals which can enhance skin hydration and barrier function based on their CE formation and filaggrin processing.

• 동의생리병리학회지
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• 제20권2호
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• pp.455-459
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• 2006

The inhibitors of prostaglandin $E_2\;(PGE_2)$ production and cyclooxygenase-2 (COX-2) activity have been considered as potential anti-inflammatory agents. In this study, we evaluated 9 compounds isolated from 5 Korean phytomedicinal plants (Spirea prunifolia, Paeonia suffruticosa, Salvia miltiorrhiza, Scutellaria baicalensis, and Artemisia capillaris) for the inhibition of $PGE_2$production and COX-2 expession in lipopolysaccharide (LPS)-stimulated human macrophages U937 cells. As a result, several compound such as prunioside A, penta-O-galloyl-beta-D-glucose, tanshinone IIA, baicalin, baicalein, wogonin, scopolatin, scoparone and decursinol showed potent inhibition of $PGE_2$production (50-70% inhibition at the test concentration of $10\;{\mu}M$). In addition, these compounds were also considered as potential inhibitors of COX-2 activity (45-73% inhibition at the test concentration of $10\;{\mu}M$). These active compound mediating COX-2 inhibitory activities are warranted for further elucidation of active principles for development of anti-inflammatory agents and these properties may contribute to the anti-atopic dermatitis activity.

• Natural Product Sciences
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• 제16권3호
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• pp.169-174
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• 2010

The seed of Phaseolus calcaratus Roxburgh (PHCR) is traditionally used for anti-pyretic and antiinflammatory effects. Although these effects are believed to be related to its antioxidant potential, little information is available for the mechanisms by which PHCR seed might scavenge free radicals or otherwise act as an antioxidant. In the present study, we purified some fractions from the ethanol extract of PHCR seed and evaluated each fraction's ability to scavenge free radicals generated by cell-free systems. We also identified active compound that is putatively responsible for free radical scavenging by analyzing NMR spectra. PHCR samples exhibited a concentration-dependent radical scavenging activity against hydroxyl radicals, superoxide anions, and DPPH radicals. Of the samples tested, a methanol-eluted sub-fraction from the PHCR extract, named $FF_4$, scavenged these radicals more effectively than the other fractions. We identified catechin-7-O-$\beta$-Dglucopyranoside as the active compound responsible for free radical scavenging potential of $FF_4$.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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• pp.178-178
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• 1998

We reported that the hexane fraction of Torilis Fructus have an anti-inflammatory and analgesic effect. Therefore, in order to isolate the active compound, the hexan fraction of Torilis Fructus was chromatographed on silica gel column. The subfraction of hexane fraction was crystallized as colorless stout needles. The chemical structure of this compound was verified to be torilin through m.p., UV, IR, GC-MS, and NMR spectral data. In pharmacological tests, torilin exhibited strong anticarrageenan activity at the dose of 90 and 270 mg/kg, p.o. in rats, and it had inhibitory effect on the vascular permeability at the dose of 30 and 90 mg/kg, p.o. in mice. Torilin showed potent inhibition of leucocyte emigration in CMC-pouch at the dose of 3 and 9 mg/rat, s.c. Torilin have the analgesic effect at the dose of 30, 90 and 270 mg/kg, p.o. in both of the acetic acid- and phenyl-p-benzoquinone-induced writhing syndrome. It also increased the pain threshold at the dose of 30, 90 and 270 mg/kg, p.o. in the tail pressure method and the Randall-Selitto method. Torilin did not show a hypothermic action at the dose of 30 and 90 mg/kg, p.o. in mice. The acute toxicity of torilin was very weak: the LD$\_$50/ value was more than 5000 mg/kg, p.o. and 2000 mg/kg, Lp. in mice. From the above mentioned results, it was suggested that torilin had potent anti-inflammatory and analgesic activities in animals.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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• pp.185-185
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• 1998

As part of our continuing attempts to evaluate biologically active compounds from fruiting bodies of cultivated fungus of Paecilomyces japonicus Yasuda, we conducted series of experiments on various fractions and compounds isolated by systematic fractionations. Our main efforts were concentrated on searching for compounds showing antitumor activities, which were tested on mice carrying Sarcoma-180 ascitic tumor. The antitumor activity was assessed by the life spans after these mice were administered Lp. with test compounds for consecutive 20 days. One of two pure compounds, which we have isolated to date, demonstrated significant prolongation of life span. ( Mean Survival Time: 30.3 days compared to that of control: 23.6 days). Structural analysis showed that this compound corresponds to D-mannitol. On the other hand, Ergosterol, another isolated pure compound didn't show efficient antitumor activity. We also obtained water-soluble fractions containing protein-bound polysaccharides and n-butantol fractions, which showed strong antitumor activities, 35.4(150%) and 32.1(136.0%) days of MST, respectively. In SRB assay, however, the test materials didn't show any toxic effects, but the level of acid phosphatase increased significantly when they were applied in cultured macrophage in vitro. Therefore, we concluded that antitumour activities might be attributed to immunostimulating rather than cytotoxic effects. Further experiments are underway to purify and structurally characterize new antitumour compounds from the active fractions.

• 대한한의학회지
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• 제18권1호
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• pp.169-186
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• 1997

Scutellariae Radix has been widely used as oriental herbal medicine for the treatment of bacterial infections in the respiratory or the gastrointestinal tract. In partition experiment for better understanding of herbal medicine with various solvents, baicalein or wogonin have more hydrophobic characteristics than baicalin or wogonoside. Unexpectedly, methylene chloride could extract more for baicalin or wogonoside over other active ingredients. New compound from baicalin is discovered casting frointier area on herbal medicine in the future. Application study with new molecule hydrolyzed from baicalin is on the way for better treatment of the patient against specific disease. The baicalin modified with reaction has been shown weak antibacterial activity against Streptococcus pyogenes 308A and Pseudomonas aeruginosa 1771. The minimum inhibitory concentration (MIC) of the baicalin modified compound against those strains were about $600\;{\mu}g/mL$, respectively. In vitro antitumor experiment, $EC_{50}$ of baicalin modified with reaction was more than $300\;{\mu}g/mL$ and $EC_{50}$ of baicalein was $100\;{\mu}g/mL$. Among these compounds, baicalin exhibited high level of antitumor activity. $EC_{50}$ of baicalin was less than $33.3\;{\mu}g/mL$.

• Archives of Pharmacal Research
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• 제26권1호
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• pp.34-39
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• 2003

The traditional Asian medicinal herb, roots of Astragalus (A.) membranaceus (Leguminosae), is used for many purposes, some of which are purported to stimulate the release of growth hormone in vivo. Extracts of A. membranaceus were tested to determine whether they stimulate the release of growth hormone in rat pituitary cell culture. A. membranaceus was extracted sequentially with 80% ethanol (fraction A), n-hexane (fraction B); the test compound from the herbal extraction was isolated using silica gel column chromatography and was identified with spectral data. Test compound was also extracted by traditional boiling water methods. Induction of growth hormone in pituitary cell culture was conducted with isolated compounds and extracted fractions of A. Radix (dried roots of A. membranaceus). The fraction A was not active in the rat pituitary cell culture, but the fraction B derived from the ethanol fraction stimulated the release of growth hormone in culture. Six compounds from fraction B (1-6) were isolated and identified previously. The compounds 1,2-benzendicarboxylic acid diisononylester (1), $\beta$-sitosterol (2), and 3-Ο-$\beta$-D-galactopyranosyl-$\beta$-sitosterol (5) did not induce growth hormone release in the culture. Formononetin (3), 9Z, 12Z-octadecadienoic acid (4), stigmast-4-en-6$\beta$-o1-3-one (6) and 98-E, a mixture of 1'-9, 12-octadecadienoic acid (Z,Z)-2',3'-dihydroxy-propylester (7) and 1'-hexadecanoic acid-2',3'-dihydroxy-propylester (8) stimulated the release of growth hormone in the rat pituitary cell culture significantly compared to the control. In conclusions, four compounds isolated from extracts of A. Radix induced growth hormone release in the rat pituitary cell culture. The 98-E isolate was the most active inducer of growth hormone release.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1978년도 학술대회지
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• pp.43-49
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• 1978

This study was devised to observe the cytotoxic activity of extracts of Panax ginseng root against some cancer cells and to purify the crude extract. Three kinds of cancer cells(leukemic cells L5178Y, HeLa cells and Sarcoma 180 cells) and mouse embryo cells (as normal cells) were used for this study. The ginseng roots were extracted with petroleum ether in soxhlet apparatus, and the crude extracts were purified by the silicic acid column chromatography and thin-layer chromatography methods. The results obtained are summarized as follows; 1. Eight to ten mg of the petroleum ether extract (crude extract) were obtained from 1 g of Panax ginseng root, and its activities per mg were about 1,000 units. 2. Doubling time of the L5178Y cells was increased to two fold by 24 hours incubation in culture medium containing about one ${\mu}g$ of extract per ml, and eight and ten folds higher concentration of ginseng extract were required for the Sarcoma 180 cells and HeLa cells, respectively, than for the leukemic cells(L5178Y) to inhibit the cellular growth to the same degree. 3. When the L5178Y cells were exposed to medium containing various concentration of the extract for 24 hours before initiation of the soft agar cloning procedure, about $99\%$ of the L5178Y cells were killed at concentration of 8 units per ml. 4. The growth rate of mouse embryo cell (as normal cell) was not affected by the culture with media containing various amounts (1.45 to 30.0 ${\mu}g/ml$) of the extract. 5. The crude extract could be purified about four times by silicic acid column chromatography using several solvent systems, and one spot of active compound could be obtained on the thin-layer chromatogram. 6. In the Swiss mice inoculated with Sarcoma 180 cells, a survival time of the experimental group (injection group of active compound) was extended more. 1.5 to 2.0 times than the control group's(no injection group).

• 한국자원식물학회지
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• 제18권1호
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• pp.57-63
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• 2005

인삼 callus의 기내배양에 의해서 항암물질을 대량생산하기 위한 연구의 일환으로 인삼 callus의 polyacetylene생산에 미치는 전구물질 및 elicitor의 효과를 조사하였다. 5mg/l의 L-phenylalanine첨가배지에서 인삼 callus의 생장과 polyacethylene합성이 가장 양호하였으며 panaxynol뿐만 아니라 panaxydol도 형성되었다. 반면에 $\alpha-methyl-D.L.methionine$과 D.L.-norleucine 첨가구에서는 polyacetylene이 전혀 생성되지 않았다. Elicitor로 사용되는 nigeran은 농도가 높아질수록 인삼 callus의 생장을 억제시키지만 polyacetylene생성에는 전혀 영향을 미치지 못했다. 그러나 chitosan은 0.5mg/l의 농도에서 는 인삼 callus의 생장과 polyacetylene의 생성에 영향을 주지 못하였으나, 1mg/l 이상 처리구에서는 panaxynol은 검출되지 않았지만 panaxydol은 검출되었다.

• 한국약용작물학회지
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• 제26권4호
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• pp.317-327
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• 2018

Background: The root of Angelica gigas Nakai is used as a traditional herbal medicine in Korea for the treatment of many diseases. However, the poor water solubility of the active components in A. gigas Nakai is a major obstacle to its bioavailability. Methods and Results: This work aimed at enhancing the solubility of the active compounds of A. gigas Nakai by a chemical (using a surfactant) and physical (hot melt extrusion, HME) crosslinking method. Fourier transform infrared spectroscopy revealed multiple peaks in the case of the extrudate solids, attributable to new functional groups including carboxylic acid, alkynes, and benzene derivatives. Differential scanning calorimetry analysis showed that the extrudate soilid had a lower glass transition temperature ($T_g$) and enthalpy (${\Delta}H$) ($T_g:43^{\circ}C$, ${\Delta}H$ : < 6 J/g) as compared to the non-extrudate ($T_g:68.5^{\circ}C$, ${\Delta}H:123.2$) formulations. X-ray powder diffraction analysis revealed the amorphization of crystalline materials in the extrudate solid. In addition, enhanced solubility (53%), nanonization (403 nm), and a higher amount of extracted phenolic compounds were achieved in the extrudate solid than in the non-extrudate (solubility : 36%, nanonization : 1,499 nm) formulation. Among the different extrudates, acetic acid and span 80 mediated formulations showed superior extractions efficiency. Conclusions: HME successfully enhanced the production of amorphous nano dispersions of phenolic compound including decursin from extrudate solid formulations.