• Food Science and Preservation
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• v.15 no.3
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• pp.456-460
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• 2008

Santalum album has been used as a folk medicine for treatment of skin diseases, inflammation, gonorrhea, gleet, and cystitis in India and other Asian countries. In a search for possible bioactive agents from natural sources, we found that the various solvent extracts of S. album showed significant antioxidative effect in 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity test and moderate other biological functions submitted to the several bioassay systems for whitening and cytotoxicity evaluations. Among the tested extracts displayed DPPH radical scavenging activity, and the 70% acetone extract showed the most potent activity with an $IC_{50}$ value of $18.6\;{\mu}g/ml$, more potent than a positive control, L-ascorbic acid ($IC_{50}$, $28.7\;{\mu}g/mL$). Also, anti-lipid peroxidation, tyrosinase inhibitory, and cytotoxic effects were determined in each experiment. Total phenolic content of 70% acetone extract was found to be 117.1 mg equivalent of gallic acid per g of extract. Previous phytochemical investigation reveals the presence of phenolic compounds. The results indicate that S. album possess potential antioxidant activity and phenolic constituents are responsible for this capacity.

• Food Science and Biotechnology
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• v.16 no.1
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• pp.29-36
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• 2007

Five phenolic compounds 1-5 were isolated for the first time from the exudate of geminating peanut (Arachis hypogaea). The structures were fully characterized by analysis of physical and spectral data. All isolated compounds were tested for antioxidant activities using 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2-azino-bis-(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), and hydroxyl radical. Compounds 2, 3, and 5 exhibited a strong scavenging effect on DPPH (2: $IC_{50}\;=\;10.4\;{\um}M$, 3: $IC_{50}\;=\;45.2\;{\mu}M$, 5: $IC_{50}\;=\;5.0\;{\mu}M$), and ABTS (2: $IC_{50}\;=\;9.6\;{\mu}M$, 3: $IC_{50}\;=\;5.5\;{\mu}M$, 5: $IC_{50}\;=\;3.3\;{\mu}M$) radical activity, whereas these compounds had weak hydroxyl radical scavenging activity ($IC_{50}\;>\;200\;{\mu}M$). The total phenolic contents of the extracts using n-hexane, EtOAc, and n-BuOH were found to be 96.4-964.3 mg gallic acid equivalent per g dry material (GAE/g) and n-BuOH fraction showed the highest total phenolic content (964.3 mg GAE/g). These studies suggest that the exudate of geminating peanut may possess possible health related benefits to humans.

• Archives of Pharmacal Research
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• v.27 no.4
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• pp.381-385
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• 2004

Nine phenolic ($1\~9$) and two furan type (10, 11) compounds, were isolated from the methanolic extract of the tuber of Gastrodia elata Blume (Orchidaceae) in the course of continuing search for platelet anit-aggregating plant components. Compound 1 was identified as 4,4'-dihy-droxybenzyl sulfone, a novel compound for the best of our knowledge. Compound 10, 5-hydroxymethyl-2-furancarboxaldehyde, was isolated for the first time from this plant. Compound 1 ($IC_{50};\;83{\mu}M$) was about four times more inhibitory to U46619 induced aggregation than ASA ($IC_{50};\340{\mu}M$). Compound 9, 4,4'-dihydroxy-dibenzylether, ($IC_{50};\;5{\mu}M$, $3{\mu}M\;and\;33{\mu}M$, respectively) was $10\~}80$ fold more potent than ASA ($IC_{50};\;420\;{\mu}M,\;53\;{\mu}M\;and\;340\;{\mu}M$ respectively) to collagen, epinephrine and U46619 induced aggregation, although it is less active than ASA to AA induced aggregation.

• Journal of the Korean Chemical Society
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• v.55 no.5
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• pp.765-775
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• 2011

Novel analogs of bortezomib were designed, synthesized and in vitro biological evaluation was carried out using human tumor cell lines A549 and PC3. Docking studies of these analogs of bortezomib was discussed. According to biological investigations, the inhibitors 4, 6, and 8 were found to be more potent than reference drug candidate bortezomib. A549 cell line showed significant sensitivity towards 4, 6, and 8 with $IC_{50}$ values 14.03, 18.5, and 12.4 nM, respectively, and PC3 cell line showed IC50 values 26.1, 37.0, and 21.2 nM, respectively. The $IC_{50}$ values of bortezomib in these cell lines are 27.3 nM and 42.0 nM.

• Microbiology and Biotechnology Letters
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• v.28 no.2
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• pp.87-91
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• 2000

In the course of screening for the substances inhibiting apoptosis ofU937 human leukemia cell induced by etoposide, a fungal strain F80834 producing a high level of inhibitor was selected. The inhibitory substance was purified and identified as terrein by spectroscopic methods of UV, EI-MS, IH-NMR, 13C-NMR and DEPT. Terrein showed inhibitory activity of caspase 3, a major protease of apoptosis cascade, with an $IC_{50}$ value of $20\mu\textrm{g}/ml$ after 7 hrs of treatment. It also showed protective effect against cell death with an $IC_{50}$ value of $10\mu\textrm{g}/ml$ on U937 cells induced by etoposide after 24 hrs of treatment, but did not show any cytotoxicity at the same condition without etoposide.

• Journal of Applied Biological Chemistry
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• v.51 no.6
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• pp.302-306
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• 2008

To evaluated active principles for diabetic compolications from the Taraxacum mongolicum (T. mongolicum), Cirsium japonicum (C japonicum), and Cirsium setidens (C. setidens) and its constituents, as well as silymarin tested for their effect on rat lens aldose reductase. As a result, the MeOH extract of T. mongolicum ($IC_{50}\;8.71\;{\mu}g/mL$) have strong lens aldose reductase inhibition abilities. Also, Aldose reductase inhibitory showed an isolated luteolin ($IC_{50}\;20\;{\mu}M$) from the T. mongolicum and sliymarin ($IC_{50}\;13\;{\mu}M$).

• Journal of Microbiology and Biotechnology
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• v.28 no.11
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• pp.1806-1813
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• 2018

A new sesquiterpene lactone dimer [1], together with five known compounds (2-6), was isolated from the flowers of Inula britannica. The structures of these compounds were established by extensive spectroscopic studies and chemical evidence. The inhibitory activities of these isolated compounds (1-6) against human neutrophil elastase (HNE) were also evaluated in vitro; compounds 1 and 6 exhibited significant inhibitory effects against HNE activity, with $IC_{50}$ values of 8.2 and $10.4{\mu}m$, respectively, comparable to that of epigallocatechin gallate (EGCG; $IC_{50}=10.9{\mu}M$). In addition, compounds 3 and 5 exhibited moderate HNE inhibitory effects, with $IC_{50}$ values of 21.9 and $42.5{\mu}M$, respectively. In contrast, compounds 2 and 4 exhibited no such activity ($IC_{50}$ > $100{\mu}M$). The mechanism by which 1 and 3 inhibited HNE was noncompetitive inhibition, with inhibition constant ($K_i$) values of 8.0 and $22.8{\mu}M$, respectively.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.383.3-384
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• 2002

Rosmarinic acid (1) and methyl rosmarinic acid (2), isolated from the ethyl acetate soluble fraction of the methanolic extract of Salvia miltiorrhiza Bunge (Lamiaceae) were found to be the tyrosinase inhibitors and scavengers of 1, 1-diphenyl-2-picrylhydrzyl (DPPH) radical. Compounds 1 and 2 inhibited the oxidation of L-tyrosine catalyzed by mushroom tyrosinase with $IC_{50}$/ of 16.8 $\mu\textrm{M}$ and 21.5 $\mu\textrm{M}$. respectively. It compared well with kojic acid. a well-known tyrosinase inhibitor. with an $IC_{50}$ of 22.4 $\mu\textrm{M}$. The inhibitory kinetics, analyzed by a Lineweaver-Burk plot, found rosmarinic acid and its methyl ester to be competitive inhibitors with $K_{i}$ of $2.35{\times}10^{-5}M$ and $1.52{\times}10^{-5}M$ respectively. In addition, compounds 1 and 2 showed the scavenging activities on DPPH radical, with $IC_{50}$ of 4.27 $\mu\textrm{M}$ and 3.05 $\mu\textrm{M}$. respectively. These scavenging effects were more potent than that of L-ascorbic acid ($IC_{50}$ = 11.75$\mu\textrm{M}$).

• Bulletin of the Korean Chemical Society
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• v.32 no.9
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• pp.3459-3464
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• 2011

In order to extend the scaffold of non-peptidic calpain inhibitor, we have designed and synthesized 14 chalcone derivatives categorized into two groups based on their structures. Compounds 7 ($IC_{50}=16.67{\pm}0.42{\mu}M$) and 8 ($IC_{50}=16.92{\pm}0.14{\mu}M$) in group A were most selective ${\mu}$-calpain inhibitor over cathepsins B and L. On the other hand, compound 14 possessing furan ring exhibited inhibitory activities for ${\mu}$-calpain ($IC_{50}=15.39{\pm}1.34{\mu}M$) as well as cathepsin B ($IC_{50}=20.59{\pm}1.35{\mu}M$). The results discovered implicated that chalcone analogues possessing proper size and functional groups can be a potential lead core for selective non-peptidic ${\mu}$-calpain inhibitor. Furthermore, dual inhibitors for ${\mu}$-calpain and cathepsin B can also be developed from chalcones by elaborate structure manipulation.

• Natural Product Sciences
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• v.24 no.2
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• pp.93-98
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• 2018

Medicinal plants are potential sources of anticancer agents screening. A large number of phytochemicals, including triterpenoids, have been reported to have significant cytotoxic effects on cancer cells. From the fruits of Ligustrum japonicum Thunb., thirteen triterpenoids (1 - 13) were isolated and evaluated for their cytotoxic activity against Hela and HL-60 cells. As results, 8 (oleanolic acid) showed significant effects on Hela with $IC_{50}$ values of $5.5{\mu}M$, and moderate effects on HL-60 cells with $IC_{50}$ values of $55.9{\mu}M$. Meanwhile, 10 (oleanderic acid) and 11 ($3{\beta}$-acetoxy-urs-12-en-28-oic acid) exhibited moderate inhibitory effects on Hela with $IC_{50}$ value of 55.0 and $68.8{\mu}M$, respectively. Moreover, 10 showed cytotoxic effect on HL-60 cell line with $IC_{50}$ value of $63.9{\mu}M$. To our knowledge, this is the first report that oleanderic acid was isolated from L. japonicum and investigated in cytotoxic effects on Hela and HL-60 cells.