뽕나무에서 분리한 Steppogenin과 Oxyresveratrol의 효모 α-Glucosidase의 억제효과

진휘승(Hwi Seung Chin),남궁우(Kung-Woo Nam) 대한약학회 2010 약학회지 Vol.54 No.5

α-Glucosidase inhibitor is a target in the treatment of type II diabetes through the mainly inhibition of glucose levels after meals. In this study, we purified steppogenin and oxyresveratrol from the stem of Morus alba L. and examined their inhibitory activity against yeast α-glucosidase. Steppogenin and oxyresveratrol were inhibited yeast α-glucosidase in a dose dependent manner. The IC50 activities (50% inhibition) were 34.4 and 9.3 μM, respectively. The kinetic inhibition of steppogenin showed noncompetitive inhibition (Km: 1.1×10-3 M; Ki: 1×10-5 M), meanwhile oxyresveratrol showed competitive inhibition (Km: 4.3×10-3 M; Ki: 3.4×10-6 M) against yeast α-glucosidase. These results indicate that steppogenin and oxyresveratrol are noncompetitive and competitive inhibitors, respectively, against yeast α-glucosidase.

식품 및 환경, 기타 소목 추출물의 항균활성과 Brazilin의 구조분석

권현정 ( Hyun Jung Kwon ),김용현 ( Yong Hyun Kim ),남궁우 ( Kung Woo Nam ),김선기 ( Sun Ki Kim ),방인석 ( In Soek Bang ),한만덕 ( Man Deuk Han ) 한국미생물생명공학회 2010 한국미생물·생명공학회지 Vol.38 No.1

천연 약용식물 추출물의 여드름 원인균에 대한 항균 및 항염증 효과

이응지 ( Eung-ji Lee ),배성윤 ( Seong-yun Bae ),남궁우 ( Kung-woo Nam ),이용화 ( Yong-hwa Lee ) 대한화장품학회 2010 대한화장품학회지 Vol.36 No.1

여드름 완화 효과를 갖는 천연 약용식물 추출물을 개발하기 위하여 여드름 원인균에 대한 항균 활성 및 항염증 효과를 다양한 추출물을 대상으로 분석하였다. 검색 결과 얻어진 후보 소재들 중, 비교적 높은 항균 활성을 갖는 보골지, 당후박과 항염증 효과를 갖는 목향, 구절초 추출물을 대상으로 선정하였고 이후의 실험을 진행하였다. 보골지(Psoralea corylifolia L., AC-1), 당후박(Magnoliae officinalis, AC-2), 목향(Inula helenium L., ACF-1), 구절초(Chrysanthemum zawadskii var. latilobum, ACF-2) 추출물 및 복합소재(AC)는 50 μg/mL 이하에서 세포 독성이 없는 것으로 확인되었다. 보골지, 당후박 추출물 및 복합소재의 경우 여드름 유발 원인균인 Propionibacterium acnes (P. acnes)에 대해 양성 대조군으로 사용한 10 % salicylic acid 대비 각각 약 2.8배, 2.5배, 3.2배의 높은 항균 효과를 보였다. 또한 Staphylococcus aureus (S. aureus)에 대해서도 당후박 추출물과 복합소재의 경우 양성 대조군으로 사용한 10 % Methylparaben 대비 각각 약 1.4배, 1.5배 높은 항균 효과를 보였다. 목향, 구절초 추출물 및 복합소재의 경우 열에 의해 사멸시킨 P. acnes에 의해 활성화된 THP-1 세포의 IL-8 발현을 50 μg/mL 농도에서 각각 27 %, 38 %, 44 % 저해하였고 TNF-α 발현을 50 μg/mL 농도에서 각각 90 %, 88 %, 90 %로 크게 저해하였다. 이러한 항균, 항염증 활성을 보이는 보골지, 당후박, 목향, 구절초 추출물의 복합 소재를 이용하여 여드름 완화 효과를 갖는 화장품으로의 개발이 가능할 것으로 보인다. To develop natural therapeutic agents for acne vulgaris, we investigated antibacterial and anti-inflammatory effects of various medicinal plant extracts. Among candidate extracts, we selected Psoralea corylifolia L. extract (AC-1) and Magnoliae officinalis extract (AC-2) which showed the relatively high antibacterial effects, and Inula helenium L. extract (ACF-1) and Chrysanthemum zawadskii var. latilobum extract (ACF-2) which showed the relatively high anti-inflammatory effects for further investigations. All of them did not show cytotoxic effects below the concentration of 50 μg/mL. The antibacterial effects of AC-1, AC-2 and extract complex (AC) against P. acnes were 2.8, 2.5 and 3.2 times higher than that of 10 % salicylic acid respectively. And the antibacterial effect of AC-2 and extract complex against S. aureus were 1.4 and 1.5 times higher than that of 10 % methylparaben respectively. Also, it was shown that ACF-1, ACF-2 and extract complex had anti-inflammatory effects. All of them exhibited inhibitory effects for the secretion of IL-8 and TNF-α from THP-1 cells activated by heat-killed P. acnes. They reduced about 27 %, 38 %, 44 % of IL-8 secretion and 90 %, 88 %, 90 % of TNF-α secretion at concentration of 50 μg/mL respectively. These results showed that the complex of medicinal plant extracts, AC-1, AC-2, ACF-1, and ACF-2, had therapeutic effects to acne vulgaris through antibacterial and anti-inflammatory effects. Therefore, we suggest that extract complex of AC-1, AC-2, ACF-1 and ACF-2 may be used as a useful agent for development of natural cosmetics which have therapeutic effects to acne vulgaris.

머루 줄기와 자소자로부터 분리한 Resveratrol 올리고머와 Flavonoid의 항균효과

손락호(Rak Ho Son),진휘승(Hwi Seung Chin),함아름(Ahrom Ham),마응천(Woongchon Mar),남궁우(Kung-Woo Nam) 대한약학회 2010 약학회지 Vol.54 No.1

We studied the antimicrobial activities of five compounds isolated from the stems of Vitis coignetiae Pulliat and the seeds of Perilla frutescens (L.) Britton. Based on spectroscopic evidence, compounds 1 to 5 were characterized as resveratrol, ε-viniferin, ampelopsin E, apigenin, and luteolin, respectively. The antimicrobial activities against Gram-positive (Staphylococcus aureus) and -negative (Pseudomonas aeruginosa) bacteria and a fungus (Candida albicans) were investigated using the disc diffusion and broth dilution methods. C. albicans was not inhibited by the five compounds. Compounds 2 and 5 had significant anti-microbial activity against S. aureus, and the 50% inhibitory concentration (IC50) of compound 2 against S. aureus was 7.2 μM. Compounds 4 and 5 significantly inhibited P. aeruginosa and the minimum inhibitory concentration (MIC) of compounds 2 and 5 was 0.07 and 2.0 μM, respectively. Compounds 2, 4, and 5 had strong anti-microbial activity against S. aureus and P. aeruginosa.

원지와 영여자로부터 분리한 8종 화합물의 항균효과

진휘승(Hwi Seung Chin),손락호(Rak Ho Son),이용화(Yong-Hwa Lee),함아름(Ahrom Ham),마응천(Woongchon Mar),김원기(Won-Ki Kim),남궁우(Kung-Woo Nam) 대한약학회 2010 약학회지 Vol.54 No.2

The chemical structures of eight compounds purified from two plants (Polygala tenuifolia Willdenow and Dioscorea batatas Decene) were determined and their anti-microbial activity against three microbial strains (Staphylococcus aureus, Pseudomonas aeruginosa, and Candida albicans) was tested. The three micro organisms were cultured in 96-well plates or Petri dishes without (control) or with the eight compounds added at concentrations of 100 to 0.01 μM (wt/vol). The growth of the microorganisms in the medium was examined after a 24-h incubation. The inhibitory effect of each compound on the growth of the microorganisms was calculated from the optical density measured at 595 nm, turbidity, and size of the inhibition zone around the treated paper disc. The minimum inhiitory concentration (MIC) of compounds 4 to 7 against S. aureus was 0.08, 0.05, 1.3 and 0.02 μM, respectively, and 0.09, 0.1, 0.2 and 100 μM against C. albicans. The IC50 (50% inhibition) values of compounds 5 and 6 were 3.1 and 6.4 μM against S. aureus, respectively, and 10 and 2.4 μM against C. albicans. Therefore, compounds 4 to 6 were the most potent anti-microbial agents among the eight compounds tested.

광귤나무(Citrus aurantium) 열매에서 분리된 쿠마린의 iNOS 억제효과

김범선(Beom sun Kim),정의길(Eui Gil Jung),윤형선(Hyung Sun Youn),황경아(Kyung A Hwang),한만덕(Man Deuk Han),유연호(Yon ho Yu),남궁우(Kung Woo Nam) 대한약학회 2017 약학회지 Vol.61 No.5

Citrus fruits have been used as an edible fruit, and also as a traditional medicine, since ancient times. A crude methanol extract of Citrus aurantium was shown to suppress inducible proinflammatory cytokines, but its constituents were not known. In this study, we isolated four furanocoumarins, bergapten (1), imperatorin (2), isoimperatorin(3), and phellopterin (4), and one 7-geranyloxycoumarin, auraptene (5), from a methanol extract of dried Citrus aurantium fruit. The structures of these compounds were elucidated by extensive application of spectroscopic techniques, including 2D NMR spectroscopy and mass spectrometry. All of the isolated compounds were evaluated for their ability to inhibit the production of proinflammatory cytokine inducible nitric oxide synthase (iNOS) in lipopolysaccharide-activated RAW264.7 cells. Compounds 2−5 significantly suppressed iNOS production but compound 1 had no iNOS inhibitory effects. These results indicate that at least three furanocoumarins and one 7-geranyloxycoumarin are involved in the suppressive effects of citrus fruits against the production of inducible inflammatory cytokines.

천연물로부터 히알루로니다아제 저해제 검색

황선구(Seon Gu Hwang),양안나(Anna Yang),김수정(Soo Jung Kim),김민기(Min Kee Kim),김성수(Sung Soo Kim),오현정(Hyun Jung Oh),이정대(Jung Dae Lee),이은주(Eun Ju Lee),남궁우(Kung-Woo Nam),한만덕(Man-Deuk Han) 한국생명과학회 2014 생명과학회지 Vol.24 No.5

HAase는 신체의 연골, 피부, 눈의 초자체 등에 포함된 고분자 다당류의 HA를 분해하는 효소로서 상처나 염증질환 시 활성화되어 염증, 알레르기 유발과 관련된 효소이다. 본 연구는 500종 식물에서 각 종당 한 식물체로부터 한 천연물의 메탄올 추출물(500추출물)을 이용하여 생물학적으로 기능이 다양하고 산업적으로 활용 가능성이 많은 HAase 저해제를 검색하였다. 그 결과 HAase 저해효과가 가장 우수한 천연물 추출물은 때죽나무 줄기 추출물 57.28%, 매화말발도리 줄기 추출물 53.50%의 저해효과를 나타내었다. 이 같은 추출물들의 농도 별 저해효과를 확인한 결과 농도 의존적으로 저해율이 증가하였다. 이 같은 결과로 볼 때 때죽나무, 매화말발도리 추출물은 HAase 효소의 저해효과가 우수하여 향후 HA 분해와 관련된 항염증 및 항 알레르기 연구에 이용될 수 있다. Mammalian hyaluronidases (HAase, EC 3.2.1.35) are a family of enzymes that hydrolyse N-acetyl-Dglucosamine (1-4) glycosidic bonds in hyaluronic acid, which is found in skin, cartilage, and the vitreous body. Although HAase is generally present in an inactive form within subcellular lysosomes, it is released in an active form in some types of inflammation and tissue injuries, thereby contributing to the inflammatory response. The HAase inhibitory activity of 500 methanolic extracts of 500 species from medicinal plants was screened using a Morgan microplate assay. The viscosity of the hyaluronic acid was measured with an Ubbelohde viscometer. Three MeOH extracts inhibited more than 50% of HAase activity at a concentration of 2 mg/ml. HAase inhibitory rates (%) of three species of medicinal plant extracts, Styrax japonica, Deutzia coreana, and Osmanthus insularis were 57.28%, 53.50%, and 53.19%, respectively. The rate of HAase inhibition of the extracts was dose dependent. In the HAase inhibitory assay using the Ubbelohde viscometer, the results were in good agreement with the results from the Morgan assay. The results suggest that HAase inhibitory compounds extracted from the stem of S. japonica, D. coreana, and O. insularis might be multifunctional and prevent the degradation of hyaluronic acid and the induction of allergic reactions and inflammation.