• Title/Summary/Keyword: $IC_{50}$ values

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Evaluation of in vitro antioxidant activities of the methanol extracts of Glinus oppositifolius and Trianthema decandra

  • Mazumder, Upal Kanti;Gupta, Malaya;Haldar, Pallab Kanti;Kandar, Chandi Charan
    • Advances in Traditional Medicine
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    • v.7 no.3
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    • pp.290-296
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    • 2007
  • Glinus oppositifolius and Trianthema decandra belonging to the Ficoidaceae family were commonly used by tribal peoples for the treatment of liver disorders and cancer. The preliminary phytochemical screening of those plants showed the presence of flavonoids, terpenoids, tannins and saponins. The aim of this study was to evaluate the in vitro antioxidant activities of the methanol extracts of Glinus oppositifolius (MEGO) and Trianthema decandra (METD). The antioxidative capacities of MEGO and METD were determined by the following four complementary assay; DPPH radical scavenging assay, superoxide anion generation by xanthine-xanthine Oxidase assay, hydroxyl radical scavenging assay and $Fe^{2+}$-ascorbate induced by lipid peroxidation assay. The $IC_{50}$ values of the both extracts were calculated from the inhibition curve. The $IC_{50}$ MEGO and METD in DPPH, superoxide anion, hydroxyl radical scavenging and lipid peroxidation assay are 1.85, 7.31, 13.95, 22.82 and 2.21, 9.78, 14.87, 19.76 ${\mu}g/ml$ respectively. Both the extracts exhibited a significant antioxidant effects.

Cytotoxic and Anti-oxidant Constituents from the Aerial Parts of Aruncus dioicus var. kamtschaticus

  • Zhao, Bing Tian;Jeong, Su Yang;Vu, Viet Dung;Min, Byung Sun;Kim, Young Ho;Woo, Mi Hee
    • Natural Product Sciences
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    • v.19 no.1
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    • pp.66-70
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    • 2013
  • Ten compounds (1 - 10), palmitic acid (1), 10-nonacosanol (2), pentacosan-1-ol (3), phytol (4), ${\beta}$-sitosterol (5), ${\beta}$-sitosterol-3-O-${\beta}$-D-glucopyranoside (6), 2,4-dihydroxycinnamic acid (7), hyperoside (8), uridine (9) and adenosine (10), were isolated from the n-hexane and EtOAc-soluble fractions of the aerial parts of A. dioicus var. kamtschaticus (Rosaceae). The structures of these compounds were elucidated on the basis of spectroscopic evidence. All compounds (1 - 10) were isolated for the first time from this plant. Cytotoxicity of 1 - 10 against Jurkat T (T-lymphocytic leukemia cells), HeLa (Human cervical epitheloid carcinoma cells), MCF-7 (Human breast cancer cells), and HL-60 (Human promyelocytic leukemia cells) cell lines was measured. Compound 6 showed good cytotoxicity against HL-60 cell line with $IC_{50}$ value of 8.13 ${\mu}g/mL$. In addition, compounds 7 and 8 exhibited antioxidant activity with $IC_{50}$ values of 16.30 and 12.42 ${\mu}g/mL$, respectively.

Inhibitory Effect of Ruta chalepensis Leaf-Derived Component against Alcohol Dehydrogenase

  • Jeon, Ju-Hyun;Cho, Jang-Hee;Kim, Hyo-Gyung;Lee, Hoi-Seon
    • Food Science and Biotechnology
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    • v.14 no.6
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    • pp.832-835
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    • 2005
  • Inhibitory activity of active compound isolated from Ruta chalepensis leaf was examined against alcohol dehydrogenase and, upon comparison to those of four commercially available compounds (quinoline, quinoline-3-carboxaldehyde, quinoline-3-carboxylic acid, and quinoline-4-carboxylic acid) and 1,10-phenanthroline as alcohol dehydrogenase inhibitor, was characterized as quinoline-4-caboxaldehyde by spectral analyses. Inhibitory effects ($IC_{50}$) of quinoline-4-caboxaldehyde and quinoline derivatives varied depending on chemicals and concentrations used. The $IC_{50}$ values of quinoline-4-carboxaldehyde, quinoline-3-carboxaldehyde, quinoline, quinoline-3-carboxylic acid, and quinoline-4-carboxylic acid were 0.04, 0.3, 0.8, >1, and >1 mg/mL, respectively. These results suggest inhibitory action of quinoline-4-carboxaldehyde against alcohol dehydrogenase as prospective therapeutics for treatment of alcoholic liver diseases such as alcohol hepatitis and cirrhosis resulting from chronic alcohol abuse.

Antiplatelet Aggregation Potencies of some Allium spp. Grown in Indonesia

  • Wijaya, C. Hanny;Muchtadi, Deddy;Lalel, Herianus J.;Zakaria, Fransiska;Koswara, Sutrisno
    • Natural Product Sciences
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    • v.2 no.1
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    • pp.37-42
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    • 1996
  • Several species and varieties of Allium spp. grown in Indonesia were screened for their in vitro antiplatelet aggregation activities. The extracts were also analyzed by GC for their volatile sulfur-containing compounds, and measured for their Volatile Reducing Substances (VRS) contents. Antiplatelet aggregation potencies of Allium spp. were varied among the species and varieties studied. Garlic extracts showed the greatest ability to inhibit platelet aggregation followed by extract of shallot, chive, yellow onion, and green onion. The 'Jawi' and 'local Padang' variety of garlic showed high activities with $IC_{50}$ values of 9.1 and $9.8\;{\mu}g/ml$, respectively. The local Kupang variety of shallot showed the highest antiplatelet activity among the shallot varieties evaluated, with an $IC_{50}$ value of $111\;{\mu}g/ml$. Antiplatelet aggregation activities of Allium extracts showed a positive correlation with the level of volatile compounds.

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Phenolic Compounds from the Leaves of Homonoia riparia and their Inhibitory Effects on Advanced Glycation End Product Formation

  • Lee, Ik-Soo;Jung, Seung-Hyun;Kim, Chan-Sik;Kim, Jin Sook
    • Natural Product Sciences
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    • v.23 no.4
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    • pp.274-280
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    • 2017
  • In a search for novel treatments for diabetic complications from natural resources, we found that the ethyl acetate-soluble fraction from the 80% ethanol extract of the leaves of Homonoia riparia has a considerable inhibitory effect on advanced glycation end product (AGE) formation. Bioassay-guided isolation of this fraction resulted in identification of 15 phenolic compounds (1 - 15). These compounds were evaluated in vitro for inhibitory activity against the formation of AGE. The majority of tested compounds, excluding ethyl gallate (15), markedly inhibited AGE formation, with $IC_{50}$ values of $2.2-89.9{\mu}M$, compared with that of the positive control, aminoguanidine ($IC_{50}=962.3{\mu}M$). In addition, the effects of active isolates on the dilation of hyaloid-retinal vessels induced by high glucose (HG) in larval zebrafish was investigated; (-)-epigallocatechin-3-O-gallate (6), corilagin (7), and desmanthine-2 (11) significantly decreased HG-induced dilation of hyaloid-retinal vessels compared with the HG-treated control group.

Pharmacological Effects of Bioactive Fractions from Brachyglottis monroi

  • Kwag Jung Sook;Na Young Soon;Perry Nigel B.;Kim Hyung Min;Baek Seung Hwa
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.1
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    • pp.260-264
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    • 2004
  • The effects of bioactive fractions from Brachyglottis monroi on biological activity were investigated. this bioactive subfraction 6-5 is the most cytotoxic to P388 murine leukaemia cell lines. A comparison of IC/sub 50/ values of these subfraction in cancer cell lines showed that their susceptibility to these subfractions decreased in the following order; Fr. 6-5 > Fr. 6-3 > Fr. 6-6 > Fr. 6-1 > Fr. 6-2 > Fr. 6-4 by the MTT method. Silica gel flash column chromatography concentrated the cytotoxic activity in subfraction 6-5 which eluted with 30% and 40% ethyl acetate : hexane gave a major bioactive (51 mg, P388 IC/sub 50/ 8,286 ng/mL at 7.5 ㎍/disc).

Cytotoxicity Against Human Cancer Cell Lines by Paecilomyces tenuipes DUGM 32001 (눈꽃동충하초(Paecilomyces tenuipes)의 인간 암세포주에 대한 세포독성)

  • 심중섭;민응기;장해룡;이창윤;김삼수;한영환
    • Korean Journal of Microbiology
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    • v.36 no.4
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    • pp.312-315
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    • 2000
  • Paecilomyces tenuipes DGUM 32001, an entomopathogenic fungus, was examined to evaluate in vitro cytotoxicity against several human cancer cells. The fruiting bodies of P. tenuipes were extracted with methanol and fractioned with some organic solvents i.e. chloroform, ethyl acetate, and butanol. The methanol extracts of P. tenuipes showed significant cytotoxicity against human cancer cell lines; HeLa, HeLa S3, and A-431. Among the fractions tested, the ethyl acetate fraction had the highest cytotoxicity against three cancer cell lines. The $IC_{50}$ values of ethyl acetate fraction against HeLa, HeLa S3, and A-431 were 13, 35, and 30 $\mu$g/ml, respectively. However, cytotoxicity might not be due to apoptosis. The methanol extract of cultured mycelia showed high cytotoxicity against HeLa cell lines.

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Anti-aging skin and antioxidant assays of protein hydrolysates obtained from salted shrimp fermented with Salinivibrio cibaria BAO-01

  • Anh, Pham Thi Ngoc;Le, Bao;Yang, Seung Hwan
    • Journal of Applied Biological Chemistry
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    • v.63 no.3
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    • pp.203-209
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    • 2020
  • This study focused on the preparation and characterization of anti-wrinkle peptides from the salted and fermented shrimp (Acetes japonicus) inoculated with Salinivibrio cibaria BAO-01 (SFSC). The results showed the proximate composition of SFSC to be 9.23% water, 75.32% protein, 0.23% fat, and 13.3 mg/g ash. Interestingly, the S. cibaria fermentation significantly increased the amount of methionine, leucine, and arginine. The in vitro antioxidant activity was assayed by the diphenylpicrylhydrazyl method and its IC50 value was found to be 43.02±2.84 ㎍/mL. It was observed to inhibit the activity of elastase, tyrosinase, collagenase, and hyaluronidase. The IC50 values of SFSC were 182.75±12.38 ㎍/mL for anti-elastase activity, 186.78±7.95 ㎍/mL for anti-tyrosinase activity, 444.4±34.81 ㎍/mL for anti-collagenase activity, and 1447.95±28.92 ㎍/mL for anti-hyaluronidase activity. These results suggest that salted and fermented shrimp has strong potential for the development of nutricosmetic products.

The Interaction of Barley Acetolactate Synthase with 4,6-Dimethoxypyrimidine Inhibitors

  • Shim, Hee-Ok;Kim, Dae-Whang;Chang, Soo-Ik;Choi, Jung-Do
    • BMB Reports
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    • v.28 no.6
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    • pp.471-476
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    • 1995
  • Acetolactate synthase (ALS) catalyzes the first common step in the biosynthesis of valine, leucine, and isoleucine. ALS is the target enzyme for several classes of structually diverse herbicides. We have synthesized 4,6-dimethoxypyrimidine derivatives as ALS inhibitors, and their inhibitory activities on barley ALS were determined. $IC_{50}$ values for the derivatives are 0.2~200 ${\mu}m$. K11570, the most potent ALS inhibitor with $IC_{50}$ of 0.2 ${\mu}m$, showed mixed-type inhibition with respect to substrate pyruvate, and the progress curves for ALS inhibition by K11570 indicated that the amount of inhibition increased with time. Inhibition-competition experiments were carried out and indicated that three different classes of inhibitors, K11570, a sulfonylurea Ally, and leucine, bind to ALS in a mutually exclusive manner. Chemical modification of tryptophanyl and tyrosyl residues of ALS decreased the sensitivity of ALS to K11570, while cysteine modification did not affect the sensitivity. These results suggest that tryptophanyl and tyrosynyl residues are probably located at or near the inhibitor binding site.

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Biological Activities and Stability of a Standardized Pentacyclic Triterpene Enriched Centella asiatica Extract

  • Puttarak, Panupong;Brantner, Adelheid;Panichayupakaranant, Pharkphoom
    • Natural Product Sciences
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    • v.22 no.1
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    • pp.20-24
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    • 2016
  • Pentacyclic triterpenes, mainly, asiatic acid, madecassic acid, asiaticoside, and madecassoside are the active constituents of Centella asiatica. A pentacyclic triterpene enriched C. asiatica extract (PRE) was prepared and standardized to contain a total pentacyclic triterpenes not less than 65% w/w. This work was focused on determination of antiinflammatory, antioxidant, and tyrosinase inhibitory activities of PRE and its stability. The PRE exhibited a satisfactory nitric oxide inhibitory effect, with an $IC_{50}$ value of $64.6{\mu}g/mL$. In addition, the PRE inhibited tyrosinase enzyme activity with an $IC_{50}$ value of $104.8{\mu}g/mL$. In contrast, the PRE possessed only weak antioxidant activity. The PRE was stable over a period of four months when stored as a dried powder but only in a well-closed container protected from light at $4^{\circ}C$. An aqueous alcoholic solution of the PRE was stable at pH values of 5.8 and 7.0, but was not stable at a pH of 8.2. Preparations of the PRE in an aqueous solution should be performed in acidic or neutral conditions.