• 제목/요약/키워드: Natural product new drug

검색결과 53건 처리시간 0.024초

Synthesis and Evaluation of Biological activities of New Imine Derivatives of Apicidin

  • Jin, Cheng-Hua;Kim, Hyung-Kyo;Han, Jeong-Whan;Lee, Hyang-Woo;Lee, Yin-Won;Zee, Ok-Pyo;Jung, Young-Hoon
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.253.2-253.2
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    • 2002
  • Apicidin. a natural product HDAC inhibitor. is recently isolated from Fusarium sp. at Merk Research Laboratories, induces therapeutic applications as a broad spectrum antiprotozoal agent to muti-drug resistant malaria and a potential antitumor agent. The biological activity of apicidin appears to be apicocomplexan HDAC at low nanomolar concentrations. (omitted)

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Synthesis of new apicidin derivatives as Histone deacetylase(HDAC) inhibitors

  • H.O. Kang;C.H. Jin;J.W. Han;Lee, H.W.;Lee, Y.W.;Park, H.J.;O.P. Zee;Y.H. Jung
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 2001년도 추계학술대회 및 정기총회
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    • pp.110-110
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    • 2001
  • Histone deacetylase(HDAC), a neuclear enzyme that regulates gene trascription and the assembly of newly synthesized chromatin, has received much attention in recent literature. The explosion of activity in this field has yielded the cloning of a mammalian gene which encodes a complementary histone acetyl trasferases. Several cyclic tetrapeptide inhibitors of HDAC has been reported to affect the hyperacetylation of mammalian and plant histones. Apicidin, a natural product HDAC inhibitor recently isolated at Merck Research Laboratories, induces therapeutic applications as a broad spectrum antiprotozoal agent to multi-drug resistant malaria and a potential antitumor agnet. The biological activity of apicidin appears to be attributable to inhibition of apicocomplexan HDAC at low nanomolar concentrations.

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Effects of the Essential Oil Components from Ligusticum chuanxiong on Proinflammatory Mediators of RAW264.7 Macrophage Cells

  • Lim, Hye-Rim;Shin, Seung-Won
    • Natural Product Sciences
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    • 제16권4호
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    • pp.259-264
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    • 2010
  • The essential oil fraction was obtained from the underground parts o of Ligusticum chuanxiong (Umbelliferae) by steam distillation, and its main components, Z-ligustilide and butylidene phthalide, were isolated by column chromatography. Its essential oil fraction and the isolated main components were examined for effects on their anti-inflammatory properties in RAW 264.7 macrophage cells to develop a new natural anti-inflammatory drug. The results showed that the L. chuanxiong essential oil fraction and its main components, Z-ligustilide and butylidene phthalide, inhibited the production of nitric oxide significantly in lipopolysaccharide (LPS)-treated RAW 264.7 cells. LPS-induced interleukin-$1{\beta}$ (IL-$1{\beta}$), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-$\alpha$) production was also decreased in a dose-dependent manner. In addition, western blot analysis revealed that the L. chuanxiong essential oil fraction and also its main components, Z-ligustilide, and butylidene phthalide reduced the expression levels of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS).

Antimicrobial Studies of Stem of Different Berberis Species

  • Singh, Meenakshi;Srivastava, Sharad;Rawat, Aks
    • Natural Product Sciences
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    • 제15권2호
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    • pp.60-65
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    • 2009
  • Berberis is an important medicinal plant, of the family Berberidaceae. Different Berberis species and their parts are very common in herbal drug markets of India and world over as an adulterant/substitute to 'Daruharidra' i.e. B. aristata DC. Antimicrobial activity of 50% hydroalcoholic extracts of stem of four Berberis species viz. B. aristata DC., B. asiatica Roxb. ex DC., B. chitria Lindl. and B. lycium Royle and the isolated alkaloid berberine were tested against eleven bacterial and eight fungal strains. The extracts with the strongest antibacterial activity was obtained from B. lycium followed by B. aristata, B. asiatica and B. chitria. Based on these results it is possible to conclude that the hydroalcoholic extract and alkaloid (berberine) has stronger and broader spectrum against bacterial strains as compared to fungal strains. The result obtained in the present study authenticates and support the use of these plants in folklore medicine for treatment of various infectious diseases caused by the bacterial pathogens. However, an attempt has been made to explore the possibilities of utilizing stem part rather than roots of these species with the aim to conserve this species which is over exploited due to diverse use of its root. These findings will stimulate the search for novel, natural products as new antibacterial/antifungal agents which may be useful to pharmaceutical industries.

Inhibition of Experimental Gastric Ulcer by Potato Tubers and the Starch

  • Lee, Jun-Gi;Jin, Jeong-Ho;Lim, Hak-Tae;Choi, Hee-Don;Kim, Hyun-Pyo
    • Natural Product Sciences
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    • 제15권3호
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    • pp.134-138
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    • 2009
  • In an attempt to establish anti-ulcerogenic activity of potato tubers, inhibitory activity against ethanol- and indomethacin-induced gastric ulcer models in rats was evaluated for the first time. From several varieties of potato tubers including Solanum tuberosum L. cv. Superior (white skin and fresh potato) and two new varieties of (Bora valley and Gogu valley), raw potato juice was prepared and the starch was obtained from each juice by filtration and drying. Upon oral administration to rats, raw potato juice showed more or less inhibitory activity. The starch showed higher and dose-dependent inhibitory activity, suggesting that the active ingredient in raw potato juice may be the starch. Particularly, the starch obtained from the tubers of new potato variety, "Bora valley," with purple color, showed the highest inhibitory activity (62.4% and 37.1% inhibition of ulcer index at 500 mg/kg), while omeprazole (proton pump inhibitor) used as a reference drug showed 74.4% and 75.7% inhibition at 20 mg/kg against ethanol- and indomethacin-induced ulcer formation, respectively. The present study provides a first evidence of anti-ulcerogenicity of raw potato juice and the starch. Especially, the starch from "Bora valley" strongly inhibited ulcer formation in rats. Considering that these are food components, they may be safely used for anti-ulcerogenic nutraceuticals.

녹용 물추출물과 항암제의 병용투여에 관한 연구(제 1보) -녹용 물추출물과 cis-Platin 및 Mitomycin C 병용투여에 의한 항암제 부작용 경감효과- (Studies on Combined Usage of Velvet Antler Water Extract and Anti-neoplastic Drugs (I) -Reducing Effect of Velvet Antler Water Extract to the Adverse Actions of cis-Platin and Mitomycin C-)

  • 심상범;김재근;원도희;홍남두;김남재
    • 생약학회지
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    • 제29권2호
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    • pp.93-103
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    • 1998
  • In order to investigate the reducing effect of velvet antler water extract (VAWE) on the toxicity of anti-cancer drug, cis-platin (CDDP) and mitomycin C (MMC), we examined effects of co-administration with VAWE and anti-cancer drugs on their toxicities. We recognized that $LD_{50}$ of CDDP/MMC were increased by co-administration with VAWE and them in mice. It was found that co-administration of VAWE and MMC increased the survival rate in mice treated by lethal dose of MMC. Also, co-administration of VAWE and CDDP/MMC inhibited decrease of the body weight and organ weight in mice intoxificated by CDDP/MMC. The increase of serum blood urea and serum creatinine levels in rats intoxicated by CDDP were significantly inhibited by the co-administrationin with VAWE and CDDP. The decrease of RBC and WBC in rats intoxificated by MMC were significantly inhibited by the co-administration with VAWE and MMC. These results suggest that the combined usage of VAWE and CDDP/MMC drugs may be a new method for prevented or minimized the toxicity of them.

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이원화 체계 하에서의 현대적 한약제제 분류 방안 고찰 (Suggestion about Modernized Classification of Herbal Medicinal Preparations in Dual Medical Systems)

  • 김지훈;조선영;한상용;박선동;김윤경
    • 대한한의학회지
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    • 제36권1호
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    • pp.61-74
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    • 2015
  • Objectives: The main purpose of this study is to find a solution for modernized classification of herbal medicinal preparations in dual medical systems. Through this study, we expect to provide a reasonable foundation of herbal medicine for public health. Methods: We studied legal or technical terms of herbal medicinal preparations from the past regulations, and through this procedure, we could suggest clear definitions of terms for herbal medicinal preparations. We also investigated documents for approval of herbal medicinal preparation from US, EU(European union), The People's Republic of China, Japan, so that we can refer to them to revise regulation for appropriate use of herbal preparations. Results: In Korea pharmaceutical affairs act, any basis of 'Crude drugs' does not exist. But in some subordinary notifications, the way that they use the 'Natural product medicine' is used as a means of limiting basic rights of doctor or pharmacist of Korean medicine compared to doctor or pharmacist. At the same time, in subordinary notifications, provisions are vague and not enough for scientific evidence of Korean medicine. Thus, we re-categorized herbal medicinal preparations into new drugs, drugs made from herbal medicinal preparations and suggested requirements for drug approval. Conclusions: Instead of using the term 'Crude drug preparations', and we should use term 'Herbal medicinal preparations' in related act and notification. And also we suggest to amend subordinary regulations and documents for approval of herbal medicinal preparations. Through this, we can make herbal medicinal preparations be more industrialized.

Bleeding Time Prolongation Effect of Methanol Extract of Viscum album var. coloratum

  • Yang, Hyun-Ok;Park, Shin-Young;Hong, Kyung-Hee;Kang, Lin-Woo;Choe, Kwang-Hoon;Kim, Young-Kyoon
    • Natural Product Sciences
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    • 제8권4호
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    • pp.152-154
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    • 2002
  • The methanol extract of Viscum album var. coloratum, Korean mistletoe, showed potent prolongation effects on the bleeding time in rats in vivo, and whole blood clotting time and plasma recalcification time in rats ex vivo. The prolongation effect on the bleeding time of Korean mistletoe is comparable to that of Viscum album L., European mistletoe, 185.6% and 176.5%, respectively. However, the water extracts of the both plants did not show any prolongation effects. Platelet activating factor (PAF) receptor binding assay was carried out to elucidate the action mechanisms of the extracts, and both of the methanol extracts did not show any inhibitory activity. The $LD_{50}$ of the methanol extracts of both mistletoes are more than 2 g/kg. These results suggest that the mehtanol extract of Korean mistletoe might be a potential candidate to develop new drug to improve microcirculation.

An International Collaborative Program To Discover New Drugs from Tropical Biodiversity of Vietnam and Laos

  • Soejarto, Djaja D.;Pezzuto, John M.;Fong, Harry H.S.;Tan, Ghee Teng;Zhang, Hong Jie;Tamez, Pamela;Aydogmus, Zeynep;Chien, Nguyen Quyet;Franzblau, Scott G.;Gyllenhaal, Charlotte;Regalado, Jacinto C.;Hung, Nguyen Van;Hoang, Vu Dinh;Hiep, Nguyen Tien;Xuan, Le Thi;Hai, Nong Van;Cuong, Nguyen Manh;Bich, Truong Quang;Loc, Phan Ke;Vu, Bui Minh;Southavong, Boun Hoong
    • Natural Product Sciences
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    • 제8권1호
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    • pp.1-15
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    • 2002
  • An International Cooperative Biodiversity Group (ICBG) program based at the University of Illinois at Chicago initiated its activities in 1998, with the following specific objectives: (a) inventory and conservation of of plants of Cuc Phuong National Park in Vietnam and of medicinal plants of Laos; (b) drug discovery (and development) based on plants of Vietnam and Laos; and (c) economic development of communities participating in the ICBG project both in Vietnam and Laos. Member-institutions and an industrial partner of this ICBG are bound by a Memorandum of Agreement that recognizes property and intellectual property rights, prior informed consent for access to genetic resources and to indigenous knowledge, the sharing of benefits that may arise from the drug discovery effort, and the provision of short-term and long-term benefits to host country institutions and communities. The drug discovery effort is targeted to the search for agents for therapies against malaria (antimalarial assay of plant extracts, using Plasmodium falciparum clones), AIDS (anti-HIV-l activity using HOG.R5 reporter cell line (through transactivation of the green fluorescent protein/GFP gene), cancer (screening of plant extracts in 6 human tumor cell lines - KB, Col-2, LU-l, LNCaP, HUVEC, hTert-RPEl), tuberculosis (screening of extracts in the microplate Alamar Blue assay against Mycobacterium tuberculosis $H_{37}Ra\;and\;H_{37}Rv),$ all performed at UIC, and CNS-related diseases (with special focus on Alzheimer's disease, pain and rheumatoid arthritis, and asthma), peformed at Glaxo Smith Kline (UK). Source plants were selected based on two approaches: biodiversity-based (plants of Cuc Phuong National Park) and ethnobotany-based (medicinal plants of Cuc Phuong National Park in Vietnam and medicinal plants of Laos). At mc, as of July, 2001, active leads had been identified in the anti-HIV, anticancer, antimalarial, and anti- TB assay, after the screening of more than 800 extracts. At least 25 biologically active compounds have been isolated, 13 of which are new with anti-HIV activity, and 3 also new with antimalarial activity. At GSK of 21 plant samples with a history of use to treat CNS-related diseases tested to date, a number showed activity against one or more of the CNS assay targets used, but no new compounds have been isolated. The results of the drug discovery effort to date indicate that tropical plant diversity of Vietnam and Laos unquestionably harbors biologically active chemical entities, which, through further research, may eventually yield candidates for drug development. Although the substantial monetary benefit of the drug discovery process (royalties) is a long way off, the UIC ICBG program provides direct and real-term benefits to host country institutions and communities.

천연물에 의한 초파리수명연장 효과 (The Effect of Natural Compounds on the Longevity Extending in the Insect, Drosophila melanogaster)

  • 이정훈;권기상;이은령;유보경;고영화;최지영;권오유
    • 생명과학회지
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    • 제27권1호
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    • pp.95-99
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    • 2017
  • 우리는 이전실험에서 배양세포를 사용하여 4종류의 천연물(Corydaline, (${\pm}$)-Car-3-ene-2,5-dione, Cinobufagin, Corilagin)이 ERAP1와 FOXO1 (DFA16) 유전자발현을 2배 이상 상승시키는 것을 증명하였다. 본 실험은 1% agar, 5% sucrose, natural compound $20{\mu}l$를 넣은 먹이를 만들어 4시간 starvation후에 4시간 동안 먹였다. Cinobufagin와 Corilagin를 먹이면 대조군에 비하여 6-8일 정도 더 생존하였다. RT-PCR 실험결과 ERAP1와 FOXO1 유전자 발현을 조절하는 것이 증명되었다. 산업곤충질병 진단과 치료에 사용될 것이며, 초파리를 대신한 생쥐에서도 동일한 결과를 실험하여 수명연장을 위한 신약으로 발전시킬 것이다.