• Title/Summary/Keyword: Natural product new drug

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A Screen for Dual-protection Molecules from a Natural Product Library against Neuronal Cell Death and Microglial Cell Activation (신경세포 사멸과 미세아교세포활성화 억제 동시 가능 천연물질 탐색 연구)

  • Min, Ju-Sik;Lee, Dong-Seok
    • Journal of Life Science
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    • v.25 no.6
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    • pp.656-662
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    • 2015
  • Natural products and natural product structures play a general and highly significant role in drug discovery and development process because it has various merits and potentials for new drug source that have extensive clinical experience, development time contraction, excellent stability and safety. In several neurological disorders, neuronal death and excessive activation of microglia (neuro-inflammation) are observed. A number of drug discovery-related neuronal cell death and neuro-inflammation was studied from natural products, respectively. However, until now, it has not been possible to study dual-protection molecules recorded in the Natural Product library. In the present study, using the natural product-derived library of the Institute for Korea Traditional Medical Industry, we investigated dual-protective molecules against glutamate (a classical excitatory neurotransmitter)-induced oxidative stress mediated neuronal cell death and LPS-induced excessive activated microglial cells (immune cells of the brain). Chrysophanol, extracted from Rheum palmatum, had dual-protective effects against both glutamate-induced neuronal cell death and LPS-induced NO production, triggering proinflammatory cytokines and microglia activation and resulting in neuroinflammation. Flow-cytometry analysis revealed that chrysophanol had a scavenger effect, scavenging glutamate- and LPS-induced reactive oxygen species (ROS) produced by neuronal and microglial cells, respectively. Based on the present study, chrysophanol may have an important protective role against neuronal cell death and neuroinflammation in the brain. The results may be helpful for studying drug development candidates for treating central nervous system disorders.

Molecular Detection of $\alpha-Glucosidase$ Inhibitor-producing Actinomycetes

  • Hyun Chang-Gu;Kim Seung-Young;Hur Jin-Haeng;Seo Myung-Ji;Suh Joo-Won;Kim Soon-Ok
    • Journal of Microbiology
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    • v.43 no.3
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    • pp.313-318
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    • 2005
  • In this study, we demonstrate the use of a PCR-based method for the detection of the specific genes involved in natural-product biosynthesis. This method was applied, using specifically designed PCR primers, to the amplification of a gene segment encoding for sedo-heptulose 7-phosphate cyclase, which appears to be involved in the biosynthetic pathways of $C_7N$ aminoacyclitol or its keto analogue-containing metabolites, in a variety of actinomycetes species. The sequences of DNA fragments (about 540 bp) obtained from three out of 39 actinomycete strains exhibited a high degree of homology with the sedo-heptulose 7-phosphate cyclase gene, which has been implicated in acarbose biosynthesis. The selective cultivation conditions of this experiment induced the expression of these loci, indicating that the range of $C_7N$ aminoacyclitol or its keto analogue-group natural products might be far greater than was previously imagined. Considering that a total of approximately 20 $C_7N$ aminoacyclitol metabolites, or its keto analogue-containing metabolites, have been described to date, it appears likely that some of the unknown loci described herein might constitute new classes of $C_7N$ aminoacyclitol, or of its keto analogue-containing metabolites. As these metabolites, some of which contain valienamine, are among the most potent antidiabetic agents thus far discovered, the molecular detection of specific metabolite-producing actinomycetes may prove a crucial step in current attempts to expand the scope and diversity of natural-product discovery.

Development of Analytical Method and Validation using HPLC/PDA for Discrimination between Artemisiae Argyi Folium and Artemisiae Iwayomogii Herba

  • Le, Duc Dat;Nguyen, Duc Hung;Zhao, Bing Tian;Min, Byung Sun;Woo, Mi Hee
    • Natural Product Sciences
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    • v.25 no.3
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    • pp.275-283
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    • 2019
  • In this study, we described the new developed method to simultaneously discriminate two herbal drugs of Artemisiae Argyi Folium and Artemisiae Iwayomogii Herba using eight marker compounds (1 - 8) on an HPLC-PDA system. The developed method was applied to quantify the major components of two herbal drugs. The pattern analysis successfully discriminated and evaluated different components between Artemisiae Argyi Folium and Artemisiae Iwayomogii Herba. Results were used for classification of different species from collected samples.

Isolation and Structure Elucidation of a New Glycolipid from the Soft Coral Lobophytum microlobulatum Collected from Havellock Island of Andaman and Nicobar Group of Islands

  • Anjaneyulu, Ammanamanchi S.R.;Rao, Nidasanametla S. Kameswara;Garg, H.S.
    • Natural Product Sciences
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    • v.2 no.2
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    • pp.102-105
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    • 1996
  • A new glycolipid, 2-hydroxy-3 $(octadecyloxy)-propyl-{\alpha}-D-arabinopyranoside$ (1) has been isolated from Lobophytum microlobulatum and its structure has been elucidated by physical and spectral $(UV,\;IR,\;^1H,\;^{13}C\;NMR,\;FABMS)$ data.

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Anti-inflammatory and Antimicrobial activities of Petroleum ether and Ethanol extracts of Scutia myrtina (Rhamnaceae)

  • Kritheka, N;Kumar, R Sambath;Kumar, S Suresh;Murthy, N Venkateswara;Sundram, R Shanmuga;Perumal, P
    • Advances in Traditional Medicine
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    • v.8 no.4
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    • pp.400-407
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    • 2008
  • The aim of the present study is to investigate the anti-inflammatory and antimicrobial activity of petroleum ether and ethanol extracts of Scutia myrtina (Family: Rhamnaceae). In anti-inflammatory activity carrageenan and histamine induced paw oedema and cotton pellet induced granuloma for acute and chronic inflammatory models were studied in Wister albino rats. Based on the results of the present study it can be concluded that petroleum ether and ethanol extract of Scutia myrtina at 400 mg/kg has potential anti-inflammatory effect and they act in a dose dependent manner. Both extracts of Scutia myrtina showed antimicrobial activity against all bacterial and fungal strains tested at the concentration of $100\;{\mu}g$/ml. From the result, it can be concluded that the Scutia myrtina contain antibacterial and antifungal principle. Further more, besides the confirmation of the popular use; the obtained results demonstrate this herbal drug to represent a new source of antimicrobial and anti-inflammatory agent.

NEW SELECTIVE AND POTENT INHIBITORS OF HUMAN CYTOCHROM P450 1A FAMILY ENZYMES

  • F. Peter Guengerich;Chun, Young-Jin;Kim, Sanghee;Kim, Donghak;Lee, Sang-Kwang;Dong, Mi-Sook;Ueng, Yune-Fang
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.10a
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    • pp.37-38
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    • 2001
  • The cytochrome P450 (P450) 1 family (1A1, 1A2, 1B1) is involved in the activation of many pro-carcinogens. Previously we characterized a number of synthetic bi- and polycyclic hydrocarbon acetylenes as selective-mechanism-based inhibitors of recombinent P450s 1A1, 1A2, 1B1 (Shimada et al., Chem. Res. Toxicol., 11, 1048-1056, 1998). We reported that the drug oltipraz is a mechanism-based indicator of P450 1A2 (Lagouet et al. Chem. Res. Toxicol., 13, 245-252, 2000).(omitted)

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Lanostane Triterpenoids from Ganoderma tropicum Collected in Vietnam and Their Nitroblue Tetrazolium Reductive Activity In Vitro

  • Nguyen, Thi Duyen;Nguyen, Minh Khoi;Phan, Nguyen Truong Thang;Duong, Minh Tan;Tran, Viet Hung;Do, Thi Ha
    • Natural Product Sciences
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    • v.26 no.4
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    • pp.334-339
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    • 2020
  • A new compound, 3��-acetoxylanosta-7,9(11),24-triene-26-al (3), and seven known compounds (1 - 2 and 4 - 8) were isolated from Ganoderma tropicum (Jung.) Bres. collected in Tay Nguyen, Vietnam. The structures of these compounds were determined by one- and two-dimensional nuclear magnetic resonance spectroscopy, electrospray ionization mass spectrometry (ESI-MS), and high-resolution ESI-MS, and by comparison with literature data. All of the isolated compounds were tested for nitroblue tetrazolium (NBT) reduction activity in Saccharomyces cerevisiae-stimulated RAW 246.7 cells. Among them, compounds 2 - 4 and 6 - 8 enhanced the NBT reduction in a dose-dependent manner.

Down-Regulation of MicroRNA-210 Confers Sensitivity towards 1'S-1'-Acetoxychavicol Acetate (ACA) in Cervical Cancer Cells by Targeting SMAD4

  • Phuah, Neoh Hun;Azmi, Mohamad Nurul;Awang, Khalijah;Nagoor, Noor Hasima
    • Molecules and Cells
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    • v.40 no.4
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    • pp.291-298
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    • 2017
  • MicroRNAs (miRNAs) are short non-coding RNAs that regulate genes posttranscriptionally. Past studies have reported that miR-210 is up-regulated in many cancers including cervical cancer, and plays a pleiotropic role in carcinogenesis. However, its role in regulating response towards anti-cancer agents has not been fully elucidated. We have previously reported that the natural compound 1'S-1'-acetoxychavicol acetate (ACA) is able to induce cytotoxicity in various cancer cells including cervical cancer cells. Hence, this study aims to investigate the mechanistic role of miR-210 in regulating response towards ACA in cervical cancer cells. In the present study, we found that ACA down-regulated miR-210 expression in cervical cancer cells, and suppression of miR-210 expression enhanced sensitivity towards ACA by inhibiting cell proliferation and promoting apoptosis. Western blot analysis showed increased expression of mothers against decapentaplegic homolog 4 (SMAD4), which was predicted as a target of miR-210 by target prediction programs, following treatment with ACA. Luciferase reporter assay confirmed that miR-210 binds to sequences in 3'UTR of SMAD4. Furthermore, decreased in SMAD4 protein expression was observed when miR-210 was overexpressed. Conversely, SMAD4 protein expression increased when miR-210 expression was suppressed. Lastly, we demonstrated that overexpression of SMAD4 augmented the anti-proliferative and apoptosis-inducing effects of ACA. Taken together, our results demonstrated that down-regulation of miR-210 conferred sensitivity towards ACA in cervical cancer cells by targeting SMAD4. These findings suggest that combination of miRNAs and natural compounds could provide new strategies in treating cervical cancer.

Bioactive Marine Natural Products in Drug Development

  • Kim, Se-Kwon;Ravichandran, Y. Dominic;Kim, Moon-Moo;Jung, Won-Kyo
    • Journal of Marine Bioscience and Biotechnology
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    • v.2 no.4
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    • pp.209-223
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    • 2007
  • Nature is one of the most important sources of pharmacologically active compounds in the search for drugs against life threatening diseases. Even though plants and terrestrial microorganisms have played as an important source for the new drug candidates from nature, marine organisms such as tunicates, sponges, soft corals, sea horses, sea snakes, marine mollusks, seaweeds, nudibranches, sea slugs and marine microorganisms are increasingly attracting attention in recent years. Marine organisms also have the potential to develop into future drugs against important diseases, such as cancer, a range of bacterial and viral diseases, malaria, and inflammations. Even though the mechanism of action in the molecular level of most metabolites is still unclear, the mechanisms by which they interfere with the pathogenesis of a wide range of diseases have been reported. The knowledge of this is one of the key factors necessary to develop bioactive compounds into medicines. This is due to their structurally unique and pharmacologically active compounds. The potential pharmaceutical, medicinal and research applications of some of these compounds are discussed in hundreds of scientific papers, and are reviewed here.

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Semantic Change of Crude Drug Preparations in Korea and Policy Evaluation (생약제제의 의미 변천과 정책적 문제 검토)

  • Kim, Yun-Kyung;Cho, Sunyoung;Kim, Jiyeon;Kang, Yeonseok
    • Herbal Formula Science
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    • v.21 no.2
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    • pp.29-43
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    • 2013
  • Objectives : The aim of this study is reviewing the past legal definition and regulations, to provide basis for the future desirable direction of Korean herbal pharmaceutical industry and national herbal drug policies. Methods : We reviewed how concept of herbal medicinal preparation has been utilized and changed along with various national laws and regulations. And this study also reviewed problems related herbal medicinal preparation policies. Results : Since 1990s, especially inauguration of Korea Food & Drug Administration (KFDA) at 1998, the concept of crude drug preparation has constantly expanded and distorted the scope of herbal medicinal preparations. This resulted in decline of herbal medicinal preparation industry. Conclusions : It means policies related herbal medicinal preparation which was driven steadily during this decade have lost their consistency. Also, it restricted the various medical options which can guarantee people's health rights.