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Development of Anti-viral Agents from Natural Sources
Hattori, Masao The Plant Resources Society of Korea 2001 Plant Resources Vol.4 No.3
Human immunodeficiency virus (HIV), the causative agent of AIDS, still continues to spread rapidly in the world population, especially in Africa and Southeast Asia. At present, two kinds of therapeutic approaches are used for treatment of AIDS. One is to target HIV reverse transcriptase, which is responsible for the viral genome transcription. The other is to inhibit HIV pretense PR, which is essential for the processing of viral proteins. Drug combinations based on these approaches can reduce the blood virus to an undetectable level. However, a small amount of virus may lurk inside the immune cells in a dormant state. Another major obstacle of long-term treatment of the disease is remarkable mutation in HIV. Most of the clinical chemotherapeutic agents have one or more of these problems. High cost and harmful side-effects further reduced the desirability of these drugs. In the course our studies on development of anti-HIV agents from natural products, we investigated various crude drugs for their inhibitory activity against HIV-induced cytopathic effects (CPE) in culture cells, HIV-pretense (PR), HIV-reverse transcriptase (RT) including ribonuclease H (RNase H), and HIV integrase (INT). In the present paper, some inhibitory substances relating to the development of anti-HIV agents are reported.
Inhibitory Constituents against HIV-1 Protease from Agastache rugosa
Min, Byung Sun,Hattori, Masao,Lee, Hyeong Kyu,Kim, Young Ho 충남대학교 약학대학 의약품개발연구소 1999 藥學論文集 Vol.15 No.-
Two diterpenoid compounds, agastanol (1) and agastaquinone (2), were isolated from the roots of Agastache rugosa (Labiatae). Compound 1 and 2 showed significant inhibitory effects against human immunodeficiency virus type 1 (HIV-1) protease activity with IC_50 values of 360 and 87μM, respectively.
Effects of Triterpenoids and Flavonoids Isolated from Alnus firma on HIV-1 Viral Enzymes
유영법,Hirotsugu Miyashiro,Norio Nakamura,Masao Hattori,박종철 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.7
Triterpenoids and flavonoids isolated from Alnus firma S. Z. were found to inhibit HIV-1 virus replication and controlled its essential enzymes. In this study, the inhibition of HIV-1 viral replication and its essential enzymes, such as reverse transcriptase, protease and α-glucosidase, were observed using 18 Korean plant extracts. Among the extracts, the methanol extract of Alnus firma leaves showed potent inhibition against the HIV-1 induced cytopathic effect (CPE) in MT-4 cells on microscopic observation (the minimum concentration for complete inhibition of HIV-1 induced CPE, IC=50 µg/mL). Thus, 14 compounds were isolated and identified from the methanol extract of Alnus firma leaves. Of these compounds, the alnustic acid methyl ester exhibited inhibition against HIV-1 protease, with an IC50 of 15.8 µM, and quercetin, quercitrin and myricetin 3-O-β-D-galactopyranoside displayed inhibition against HIV-1 reverse transcriptase, all with IC50 values of 60 µM. Based on these results, the viral replication inhibition of the methanol extract of Alnus firma leaves was adjudged to be acutely related to the protease inhibition activation of the alnustic acid methyl ester as well as the reverse transcriptase inhibition activation of flavonoids.
Effects of Triterpenoids and Flavonoids Isolated from Alnus firma on HIV-1 Viral Enzymes
Yu, Young-Beob,Miyashiro, Hirotsugu,Nakamura, Norio,Hattori, Masao,Park, Jong-Cheol 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.7
Triterpenoids and flavonoids isolated from Alnus firma S. Z. were found to inhibit HIV-1 virus replication and controlled its essential enzymes. In this study, the inhibition of HIV-1 viral replication and its essential enzymes, such as reverse transcriptase, protease and ${\alpha}-glucosidase$, were observed using 18 Korean plant extracts. Among the extracts, the methanol extract of Alnus firma leaves showed potent inhibition against the HIV-1 induced cytopathic effect (CPE) in MT-4 cells on microscopic observation (the minimum concentration for complete inhibition of HIV-1 induced CPE, IC=50 ${\mu}g/mL$). Thus, 14 compounds were isolated and identified from the methanol extract of Alnus firma leaves. Of these compounds, the alnustic acid methyl ester exhibited inhibition against HIV-1 pretense, with an $IC_{50}$ of 15.8 ${\mu}M$, and quercetin, quercitrin and myricetin $3-O-{\beta}-D-galactopyranoside$ displayed inhibition against H IV-1 reverse transcriptase, all with $IC_{50}$ values of 60 ${\mu}M$. Based on these results, the viral replication inhibition of the methanol extract of Alnus firma leaves was adjudged to be acutely related to the protease inhibition activation of the alnustic acid methyl ester as well as the reverse transcriptase inhibition activation of flavonoids.
사방오리 잎의 Triterpenoid 및 Flavonoid 화합물
유영법,Norio Nakamura,Hirotsugu Miyashiro,Masao Hattori,박종철 한국생약학회 2007 생약학회지 Vol.38 No.1
Abstract − In this study, three triterpenoids, two steroids and nine flavonoids were isolated from the leaves of Alnus firma Sieb. et Zucc. On the basis of spectroscopic evidences, the structures of these compounds were established as β-amyrin acetate, β- amyrin, β-sitosterol, alnustic acid methyl ester, β-sitosterol glucoside, pinocembrin, alnustinol, quercetin, quercetin-3-O-α-Larabinofuranoside, quercetin-3-O-α-L-rhamnopyranoside, quercetin-3-O-β-D-glucopyranoside, myricetin-3-O-β-D-galactopyranoside, (+)-catechin and (−)-epicatechin.
Inhibitory Effects of Methanol Extracts from Korean Medicinal Plants against HIV-1 Protease Activity
Jong-Cheol Park,Hirotsugu Miyashiro,Masao Hattori 한국약용작물학회 2003 한국약용작물학회지 Vol.11 No.4
Korean medicinal plants were screened for their inhibitory activity against HIV-1 protease. The inhibitory activity of protease was determined by incubating the extracts in reaction mixtures containing protease and substrate His-Lys-Ala-Arg-Val-Leu-(p-NO2-Phe)-Glu-Ala-Nle-Ser-NH2 to perform proteolytic cleavage reactions. In this study the twenty six extracts from medicinal plants were investigated. Of the extracts tested, the extracts from the stem of Morus alba. exhibited the strongest activity with inhibition of 81% at a concentration of 100μg/ml. The extracts of the flower of Saxjfraga stolonifera, and stems of Euonymus japonica and Castanea crenata showed appreciable inhibitory activity (〉50%) against HIV-1 protease at same concentration.
Cytotoxicity of Shikonin Metabolites with Biotransformation of Human Intestinal Bacteria
MIN, BYUNG SUN,MESELHY, MESELHY R.,HATTORI, MASAO,KIM, HWAN MOOK,KIM, YOUNG HO 한국미생물 · 생명공학회 2000 Journal of microbiology and biotechnology Vol.10 No.4
Six shikonin metabolites were obtained from human intestinal bacteria, Bacteriodes fragilis subsp. thetaotus, following biotransformation. The transformation of shikonin (1) was performed anaerobically for 3 day at 37℃ in the bacterial suspension of B. fragilis which was cultured overnight in GAM broth. The incubation mixture was extracted with EtOAc to give a dark-brown residue. The residue was applied to a silica gel column, which was eluted successively with hexane (Fr. A). CHCl_3, (Fr. B), and CHCl_3:MeOH (9:1) (Fr. C). Six metabolites, Fr.A (2 and 3), Fr. B ( 6 and 7). and Fr. C (4 and 5) were isolated by repeated silica gel column chromatography, preparative TLC, followed by Sephadex LH-20. In vitro cytotoxicities were tested against human tumor cell lines; PC-3 (prostate), ACHN (renal), A549 (lung). SW620 (colon), K562 (leukemia), and Du145 (prostate). The shikonin metabolites 2, 4, 5, and 6 showed weaker cytotoxicity than the parent shikonin (1), whereas shikonin monomeric metabolite 3 (ED_50 0.44-1.22㎍/㎖) and dimeric metabolite 7 (ED_50 0.48-2.35㎍/㎖) exhibited stronger activities compared with adriamycin, which was used as the positive control.
Inhibitory Effects of Methanol Extracts from Korean Medicinal Plants against HIV-1 Protease Activity
Park, Jong-Cheol,Miyashiro, Hirotsugu,Hattori, Masao The Korean Society of Medicinal Crop Science 2003 韓國藥用作物學會誌 Vol.11 No.4
Korean medicinal plants were screened for their inhibitory activity against HIV-1 protease. The inhibitory activity of protease was determined by incubating the extracts in reaction mixtures containing protease and substrate $His-Lys-Ala-Arg-Val-Leu-(p-NO_{2}-Phe)-Glu-Ala-Nle-Ser-NH_{2}$ to perform proteolytic cleavage reactions. In this study the twenty six extracts from medicinal plants were investigated. Of the extracts tested, the extracts from the stem of Morus alba. exhibited the strongest activity with inhibition of 81% at a concentration of $100{\mu}g/ml$. The extracts of the flower of Saxjfraga stolonifera, and stems of Euonymus japonica and Castanea crenata showed appreciable inhibitory activity (>50%) against HIV-1 protease at same concentration.