• Archives of Pharmacal Research
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• v.29 no.6
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• pp.497-502
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• 2006

A new natural C-benzylated chalcone, $2',4'-dihydroxy-3'-(2-hydroxybenzyl)-6{\c}-methoxychalcone$ (2), along with two other flavonoids, tiliroside and kaempferol 3-O-rutinoside, and an oxoaporphine alkaloid, lanuginosine were isolated from the aerial parts of Ellipeiopsis cherrevensis (Annonaceae). Two known polyoxygenated cyclohexene derivatives, ferrudiol and zeylenol, and a new analog, ellipeiopsol D, were also isolated. The chalcone 2 exhibited cytotoxic activity against human small-cell lung-cancer (NCl-H187), epidermoid carcinoma (KB) and breast cancer (BC) cell lines with $IC_{50}$ values of 1.40, 5.31 and $13.92\;{\mu}g/mL$, respectively. This compound also showed antimalarial activity against Plasmodium falciparum with an $IC_{50}$ value of $7.1\;{\mu}g/mL$ as well as antimicrobacterial activity against Mycobacterium tuberculosis with a MIC of 25 mg/mL.

• Advances in Traditional Medicine
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• v.8 no.4
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• pp.329-338
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• 2008

The aim of the study is to investigate the antioxidant activity through, reducing power, 2, 2-diphenyl-1-picryl hydrazyl radical (DPPH), nitric oxide radical (NO), superoxide radical, hydrogen peroxide radical ($H_2O_2$) scavenging activity and the amount of total phenolic compounds of chloroform, ethyl acetate, methanol and aqueous extracts of the leaves of Talinum portulacifolium. Chloroform extract of leaves of T. portulacifolium showed highest antioxidant activity, with a direct relationship between activity and concentration of extracts ($15-240\;{\mu}g/mL$). Among all the extracts, the highest amount of the total polyphenolic compounds was found in the chloroform extract. Chloroform extract of T. portulacifolium showed an important free radical scavenging activity towards the DPPH, NO, Superoxide and $H_2O_2$ radicals, with $IC_{50}$ values of 133.26, 165.75, 156.34 and $135.29\;{\mu}g/mL$, respectively. In the lipid peroxidation assay, extracts of chloroform and ethyl acetate showed a remarkable inhibitory activity. The extracts showed significant activity in all the experiments but lower than the standard antioxidant, ascorbic acid.

• Archives of Pharmacal Research
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• v.13 no.1
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• pp.19-23
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• 1990

A series of hexahydro-s-triazine derivative were prepard. Cytotoxic activity testing using mouse leukemia cells (p 388) and antimicrobial testing indicated that the compounds which contain isoxazolyl moiety higher activity than those containing other hetercyclic moieties.

• Archives of Pharmacal Research
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• v.29 no.10
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• pp.826-833
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• 2006

Previously, we synthesized and evaluated several benzofuran derivatives containing heterocyclic ring substituents linked to the benzofuran nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV-1, anticancer and antimicrobial agents. Among these derivatives, NSC 725612 and NSC 725716 exhibited interesting anti-HIV-1 activity. To further investigate the structure-activity relationship, we synthesized several new benzofuran derivatives derived from 2-acetylbenzofuran (2, 3a-c) and 2-bromoacetylbenzofuran (6; 7a,b; 8a,b). The compounds were designed to comprise the heterocyclic substituents directly linked to the benzofuran nucleus at C-2. Moreover, various related benzimidazoles derived from 2-acetylbenzimidazole and from 2-cyanomethylbenzimidazole (12a,b; 13a,b; 15; 16a,b) were also prepared as isosteres. The synthesized compounds were preliminarily evaluated for their in vitro anti-HIV-1, anticancer and antimicrobial activity. Compounds 2, 3a, 3b, and 12b showed weak anti-HIV-1 activity. Compound 6 exhibited mild activity against S. aureus, while compound 15 had mild activity towards S. aureus and C. albicans. However, no significant anticancer activity was observed with any of the tested compounds. From these results, we conclude that the presence of the spacer between the heterocyclic substituent and the benzofuran nucleus may be essential for the biological activity.

• Proceedings of the PSK Conference
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• 2001.10a
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• pp.236.1-236.1
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• 2001

• The Journal of Asian Finance, Economics and Business
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• v.8 no.2
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• pp.737-745
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• 2021

This study aims to determine whether there are differences in the average abnormal return, trading volume activity, and trading frequency activity in pharmaceutical stocks before and after the announcement of the first case of the coronavirus (COVID-19) in Indonesia. The sample was selected using a purposive sampling method and collected as many as nine pharmaceutical companies listed on the Indonesia Stock Exchange during 2019-2020. The data used in this study were secondary data in the form of daily data on stock closing prices, Composite Stock Price Index (IHSG), stock volume trading, number of shares outstanding, and stock trading frequency. This study was an event study with an observation period of 14 days, namely seven days before and seven days after the announcement of the coronavirus's first positive case in Indonesia. Hypothesis testing employed the paired sample t-test method. Based on the results, it was found that there was no difference in the average abnormal return of pharmaceutical stocks before and after the announcement of the first case of COVID-19. However, there was a difference in the average trading volume activity and the average trading frequency activity in pharmaceutical stocks before and after the announcement of the first case of COVID-19.

• BMB Reports
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• v.43 no.12
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• pp.801-806
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• 2010

The existence of glycine residues in long-chain scorpion toxins has been well documented. However, their role as analgesics has not been evaluated. To address this issue, we investigated the functional role of glycines in the C-terminal end of Chinese-scorpion toxin from Buthus martensii Karsch (BmK AGP-SYPU2) using site-directed mutagenesis and analgesic activity assays. Recombinant BmK AGP-SYPU2 and its mutants were efficiently expressed in E. coli and purified to homogeneity using immobilized metal ion affinity chromatography (IMAC) and cation exchange chromatography. The mouse-twisting test was used to detect the analgesic activity of BmK AGP-SYPU2 and its mutants. As a result, we identified glycines at the C-terminal end that, when altered, significantly affected analgesic activity. Also, Mut6566 was significantly decreased compared to BmK AGP-SYPU2. These data indicate that the glycines at the C-terminal end are important for the analgesic activity of BmK AGP-SYPU2.

• Korean Journal of Pharmacognosy
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• v.39 no.3
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• pp.223-227
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• 2008

Advanced glycation end products (AGEs) contribute to the progression of micro and macrovsacular complication of diabetes and therefore present a promising target for therapeutic agents. In this study, 40 Korean herbal medicines have been investigated with an in vitro evaluation system using AGEs inhibitory activity. Of these, 21 herbal medicines $(IC_{50}<50{\mu}g/ml)$ exhibited an inhibitory activity against AGEs formation compared with anminoguanidine $(IC_{50}=72.12{\mu}g/ml)$. Particularly, 7 herbal medicines, Actinidia arguta (root and stem), Crataegus pinnatifida (twig), Camellia japonica (whole), Kalopanax pictus (bark), Lagerstroemia indica (leaf-stem), Reynoutria sachalinensis (root) showed more potent inhibitory activity (approximately 3-10 fold) than the positive control aminoguanidine.

• Natural Product Sciences
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• v.12 no.4
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• pp.210-213
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• 2006

A 4,5-dioxoaporphine type alkaloid, cepharadione B (1), a phenolic acid, protocatechuic acid (2), and flavonols, quercetin (3), afzelin (4), and quercitrin (5), were isolated from the EtOAc-soluble extract of the whole plants of Houttuynia cordata. All the isolates (1-5) were subjected to in vitro bioassays to evaluate advanced glycation end products (AGEs) formation and rat lens aldose reductase (RLAR) inhibitory activity. The three flavonols 3-5 exhibited a significant inhibitory activity on AGEs formation with $IC_{50}$ values of 66.9, 58.9, and $32.3{\mu}M$, respectively. While the two flavonol rhamnosides 4 and 5 showed a remarkable inhibitory activity against RLAR with $IC_{50}$ values of 0.81 and $0.16{\mu}M$, respectively.

• Journal of Microbiology and Biotechnology
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• v.28 no.12
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• pp.2141-2144
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• 2018

Based on previous studies reporting the anti-prion activity of poly-${\text\tiny{L}}$-lysine and poly-${\text\tiny{L}}$-arginine, we investigated cationic poly-${\text\tiny{L}}$-ornithine (PLO), poly-${\text\tiny{L}}$-histidine (PLH), anionic poly-${\text\tiny{L}}$-glutamic acid (PLE) and uncharged poly-${\text\tiny{L}}$-threonine (PLT) in cultured cells chronically infected by prions to determine their anti-prion efficacy. While PLE and PLT did not alter the level of $PrP^{Sc}$, PLO and PLH exhibited potent $PrP^{Sc}$ inhibition in ScN2a cells. These results suggest that the anti-prion activity of poly-basic amino acids is correlated with the cationicity of their functional groups. Comparison of anti-prion activity of PLO and PLH proposes that the anti-prion activity of poly-basic amino acids is associated with their acidic cellular compartments.