• Advances in Traditional Medicine
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• v.8 no.1
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• pp.97-102
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• 2008

A total of five compounds namely, 2-methylanthracene-9, 10-dione (1), 1-hydroxy-6-methylanthracene-9,10-dione (2), $\beta$-sitosterol (3), stigmasterol (4) and sitosterone (5) were isolated from the stem extracts of Polygonum lanatum for the first time. The structures of the isolated compounds (1-5) were established by extensive spectroscopic studies, including 2D NMR such as $^{1}H-^{1}H$ COSY, HSQC and HMBC studies. The crude extracts and purified compound (1) were screened for antimicrobial activity against a wide range of Gram-positive and Gram-negative bacteria and fungi by the disc diffusion method. The n-hexane and dichloromethane soluble partitionates of the methanolic extract revealed mild to moderate inhibition of growth of the test organisms. The cytotoxic potential of the extractives and compound 1 was also determined by using brine shrimp lethality bioassay, where the extractives demonstrated significant cytotoxic activities.

• Biomolecules & Therapeutics
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• v.31 no.3
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• pp.312-318
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• 2023

The natural flavonoid macakurzin C (1) exhibited adiponectin biosynthesis-inducing activity during adipogenesis in human bone marrow mesenchymal stem cells and its molecular mechanism was directly associated with a pan-peroxisome proliferator-activated receptor (PPAR) modulator affecting all three PPAR subtypes α, γ, and δ. In this study, increases in adiponectin biosynthesis-inducing activity by macakurzin C derivatives (2-7) were studied. The most potent adiponectin biosynthesis-inducing compound 6, macakurzin C 3,5-dimethylether, was elucidated as a dual PPARα/γ modulator. Compound 6 may exhibit the most potent activity because of the antagonistic relationship between PPARδ and PPARγ. Docking studies revealed that the O-methylation of macakurzin C to generate compound 6 significantly disrupted PPARδ binding. Compound 6 has therapeutic potential in hypoadiponectinemia-related metabolic diseases.

• YAKHAK HOEJI
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• v.43 no.5
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• pp.584-590
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• 1999

Bioactivity-directed fractionation from the seeds of Annona cherimolia resulted in the isolation of two known cytotoxic compounds : corrosolin (1) and compound-2 (2). The structures of these compounds were characterized on the basis of chemical and spectral data. Corrosolin has a relative stereochemical relationship of threo/trans/threo for the mono-tetrahydrofuran (THF) ring with two flanking hydroxyls, from C-15 to C-20, which is the annonacin type. Compound-2 has a relative stereochemical relationship of threo/trans/threo/trans/threo for the adjacent bis-THF ring with two flanking hydroxyls, such as in the asimicin type. The absolute configurations of carbinol carbons in corrosolin in corrosolin were determined as 10R, 15R, and 20R by analysis of its Mosher ester derivatives. Corrosolin and compound-2 are known, but are first isolated in this plant.

• Korean Journal of Pharmacognosy
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• v.41 no.1
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• pp.67-72
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• 2010

In the recent version of the Korea Pharmacopoeia(KP) and the Korean Herbal Pharmacopoeia(KHP), there are 563 items(181 in KP, 381 in KHP) of herbal medicines including finished drugs. Also, approximately 507 items including herbal extracts and herbal medicinal products was published in the 3th edition of Korea Pharmaceutical Codex (KPC). These items help the persons working in the pharmaceutical manufacturing field to register the drug and in research fields to develop the new drug considering as a standard specifications. This study was carried out to establish standard analytical methods for 'Compound Hawthorn Berry 60% Ethanol Extract, Ginkgo Biloba Leaf Extract and Garlic Oil Capsules' in the 3th edition of Korea Pharmaceutical Codex. Ginkgo flavonoid and terpene lactone were employed as reference compounds for analytical method. Analytical methods established in this study could be applied to a reasonable and unified quality control of G. biloba leaf extract and hawthorn berry extract.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.7
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• pp.3293-3298
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• 2012

The present study was conducted to evaluate in vivo anticancer activity of two novel mononuclear ruthenium(II) compounds, namely Ru(1,10-phenanthroline)$_2$(2-nitro phenyl thiosemicarbazone)$Cl_2$(Compound $R_1$) and Ru (1,10-phenanthroline)$_2$(2-hydroxy phenyl thiosemicarbazone)$Cl_2$(Compound $R_2$) against Ehrlich ascites carcinoma (EAC) mice and in vitro cytotoxic activity against IEC-6 (small intestine) cell lines and Artemia salina nauplii using MTT [(3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide)] and BLT [brine shrimp lethality] assays respectively. The tested ruthenium compounds at the doses 2 and 4 mg/kg body weight showed promising biological activity especially in decreasing the tumor volume, viable ascites cell counts and body weights. These compounds prolonged the life span (% ILS), mean survival time (MST) of mice bearing-EAC tumor. The results for in vitro cytotoxicity against IEC-6 cells showed the ruthenium compound $R_2$ to have significant cytotoxic activity with a $IC_{50}$ value of $20.0{\mu}g/mL$ than $R_1$ ($IC_{50}=78.8{\mu}g/mL$) in the MTT assay and the $LC_{50}$ values of $R_1$ and $R_2$ compounds were found to be 38.3 and $43.8{\mu}g/mL$ respectively in the BLT assay. The biochemical and histopathological results revealed that there was no significant hepatotoxicity and nephrotoxicity associated with the ruthenium administration to mice.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.362.4-363
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• 2002

Costunolide which is known as a chemopreventive drug is a sesquiterpene compound isolated from Magnolia Sieboldii. and has antitumor and antiinflamatory activities. it is very hard to collect enough amount of natural extracts of costunolide for the activity studies. therfore. synthesis of costunolide derivatives is honestly needed. the aim of this research is to develope new methods for costunolide synthesis and to test biological activities. (omitted)

• Natural Product Sciences
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• v.11 no.2
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• pp.63-66
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• 2005

A rare flavonol glycoside identified as $eupalitin-3-O-{\beta}-D-glucoside$ (I) was isolated from Tephrosia spinosa (Leguminosae) and its anti-inflammatory activity was evaluated against carrageenin induced paw edema. The compound exhibited significant activity when compared to the standard drug indomethacin.

• Archives of Pharmacal Research
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• v.22 no.1
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• pp.75-77
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• 1999

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 $87{\mu}M$, respectively.

• Natural Product Sciences
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• v.5 no.1
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• pp.20-24
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• 1999

Bioassay-guided fractionation of anti-emetic constituents of Alpinia katsumadai Hayata was performed. Nine compounds including one novel compound, (3R,5S)-trans-3,5-dihydroxy-1,7-diphenyl-1-heptene (9) were isolated from it. Among these compounds, four diarylheptanoids, one sesquiterpenoid and one flavonoid showed anti-emetic activity on copper sulfate induced-emesis in young chicks.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.253.1-253.1
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• 2002

DA-8159 is a new PDEV inhibitor, synthesized by Dong-A Pharm, as an oral agent to treat male erectile dysfunction. DA-8159 and sildenafil are mainly metabolized by cytochrome P450 enzyme CYP 3A4. In this study. we compared the metabolism of DA-8159 with sildenafil in vitro and in vivo. First, we quantified the remaining gatio of original compound, DA-8159 and sidenafil., after we incubated drugs for 30 minutes with human liver microsome cytochrome P 450 3A4. (omitted)