Synthesis of New Simplified and Racemic Hemiasterlin Derivatives with Extremely High Cytotoxicity

Hemiasterlin is a potent antimitotic agent acting through inhibition of microtubule depolymerization. For this reason, the synthesis of new hemiasterlin derivatives has attracted a lot of interest in the organic chemistry community recently. In this paper, the synthesis and evaluation of the cytotoxicity of new simplified and racemic hemiasterlin derivatives were reported. All of the synthesized analogues were evaluated in vitro for cytotoxic activity against four human cell lines (KB, Hep-G2, LU and MCF7). Most of these analogues possess a strong cytotoxic activity on two human cancer cell lines (KB and Hep-G2) and very weak activity on LU and MCF7 cell lines.

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In Vitro cytotoxic activity of some Korean medicinal plants on human cancer cell lines: enhancement in cytotoxicity by heat processing

Phytotherapy Research ◽

10.1002/ptr.2213 ◽

2007 ◽

Vol 21 (9) ◽

pp. 900-903 ◽

Cited By ~ 15

Author(s):

Hye Hyun Yoo ◽

Jeong Hill Park ◽

Sung Won Kwon

Keyword(s):

Medicinal Plants ◽

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Heat Processing ◽

Human Cancer Cell ◽

Human Cancer Cell Lines

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CYTOTOXIC ACTIVITY OF LUVUNGA SCANDENS AGAINST HUMAN CANCER CELL LINES

Jurnal Teknologi ◽

10.11113/jt.v78.7328 ◽

2016 ◽

Vol 78 (10) ◽

Author(s):

Putri Nur Hidayah Al-Zikri ◽

Muhammad Taher ◽

Deny Susanti ◽

Solachuddin Jauhari Arief Ichwan

Keyword(s):

Cytotoxic Activity ◽

Cell Line ◽

Cell Lines ◽

A549 Cell ◽

Human Cancer ◽

In Vitro Cytotoxicity ◽

Breast Adenocarcinoma ◽

Human Cancer Cell Lines ◽

Mcf 7

Luvunga scandens belongs to the family of Rutaceae which usually inhabit tropical and moist environment. This plant is known as ‘Mengkurat Jakun’ among locals and used traditionally to treat fever and fatigue via decoction. The aim of this study was to investigate the cytotoxic activity of the leaves and stems extracts of L. scandens extract. Extracts of the leaves and stems were obtained from sequential extraction procedures by various organic solvents. All extracts were subjected to cytotoxic study by 3-(4, 5-dimethylthaizol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. In in vitro cytotoxicity assay, all L. scandens extracts exhibited cytotoxicity against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. The IC50 values of dichloromethane and methanol extracts from the leaves of L. scandens against MCF-7 cell line were 62.5 µg/mL and 88.0 µg/mL, respectively, whereas IC50 of methanol extract from stem was 81.0 µg/mL. All extracts were less active against A549 cell line where IC50 value were not be determined. The present findings revealed the potential of L. scandens as a cytotoxic agent against MCF-7 cell line. However, further studies should be planned to evaluate role of the plant in cytotoxic activity.

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Screening of in vitro cytotoxic activity potential of Odontobuthus doriae and bothutus Saulcyi scorpion venoms against a panel of human cancer cell lines

Toxicon ◽

10.1016/j.toxicon.2018.10.171 ◽

2019 ◽

Vol 158 ◽

pp. S49

Author(s):

Toktam M. Kashani ◽

Amir Salarian ◽

Hossein Vatanpour ◽

Farshad Shirazi ◽

Abbas Zare ◽

...

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Human Cancer Cell ◽

Human Cancer Cell Lines ◽

Scorpion Venoms

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Design, Synthesis, and Cytotoxic Activity of New Tubulysin Analogues

Synlett ◽

10.1055/s-0041-1737139 ◽

2021 ◽

Author(s):

Anh Tuan Tran ◽

Chien Van Tran ◽

Hai Van Le ◽

Loc Van Tran ◽

Thao Thi Phuong Tran ◽

...

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Cytotoxic Activities ◽

Design Synthesis ◽

Human Cancer Cell Lines ◽

Ht 29

AbstractSynthesis of tubulysin analogues, containing an N-methyl substituent on tubuvaline-amide together with the replacement of either the hydrophobic N-terminal N-methyl pipecolic acid (Mep) or at both N- and C- terminal peptides with available heteroaromatic acids and an unsaturated tubuphenylalanine moiety, respectively, were described. The in vitro cytotoxic activity by SRB assay on five cancer cell lines for sixteen tubulysins was evaluated. Among them, five analogues exhibited strong cytotoxic activities against five human cancer cell lines, including human breast carcinoma (MCF7), human colorectal adenocarcinoma (HT-29), HL-60, SW-480, human lung adenocarcinoma (A459). Interestingly, one analogue showed the strongest cytotoxicity on all five tested cell lines even much higher toxicity than the reference compound ellipticine.

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In vitro Cytotoxic Activity of Extracts and Isolated Constituents of Salvia leriifoliaBenth. against a Panel of Human Cancer Cell Lines

Chemistry & Biodiversity ◽

10.1002/cbdv.201000311 ◽

2011 ◽

Vol 8 (6) ◽

pp. 1152-1162 ◽

Cited By ~ 17

Author(s):

Rosa Tundis ◽

Monica R. Loizzo ◽

Federica Menichini ◽

Marco Bonesi ◽

Carmela Colica ◽

...

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Human Cancer Cell ◽

Human Cancer Cell Lines

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The in vitro cytotoxic activity of ethno-pharmacological important plants of Darjeeling district of West Bengal against different human cancer cell lines

BMC Complementary and Alternative Medicine ◽

10.1186/s12906-015-0543-5 ◽

2015 ◽

Vol 15 (1) ◽

Cited By ~ 16

Author(s):

Bipransh K Tiwary ◽

Sony Bihani ◽

Anoop Kumar ◽

Ranadhir Chakraborty ◽

Runu Ghosh

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

West Bengal ◽

Human Cancer ◽

Cancer Cell Lines ◽

Human Cancer Cell ◽

Human Cancer Cell Lines

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IN VITRO CYTOTOXIC ANTICANCER POTENTIAL OF BIOACTIVE FRACTION ISOLATED FROM INDONESIAN TIDAL SPONGE CALTHROPELLA SP.

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v12i1.23655 ◽

2019 ◽

Vol 12 (1) ◽

pp. 380

Author(s):

Fitria Susilowati ◽

Respati Tri Swasono ◽

Tatsufumi Okino ◽

Winarto Haryadi

Keyword(s):

High Resolution ◽

Cytotoxic Activity ◽

Cell Lines ◽

Bioactive Compounds ◽

Human Cancer ◽

Human Cancer Cell Lines ◽

Anticancer Properties ◽

Bioactive Fraction ◽

Mcf 7

Objective: This study was taken to examine the cytotoxicity of the bioactive fraction isolated from marine sponge Calthropella sp. as a preliminary anticancer assay and identify its bioactive compounds.Methods: The cytotoxic activity was assessed by 3-(4,5-dimethylthiazol-2-y1)-2,5-diphenyltetrazolium bromide assay against three human cancer cell lines, namely human breast (MCF-7), human lung (H-460), and human liver (HepG-2). The bioactive compounds were identified using a high-resolution liquid chromatography–mass spectroscopy (LC–MS).Results: The active fraction 7 showed moderate to strong cytotoxic activity on all cell lines tested and promising a strong potent cytotoxicity against MCF-7 cell lines with IC50 value as low as 1.925 μg/mL comparable to control, cisplatin (IC50 0.977 μg/mL). In regard to the promising bioactive compounds, the high-resolution LC–MS predicted the existing of several known compounds such as bengamide Q, clavepictine A, 4’-N-methyl-5’- hydroxystaurosporine, carteriofenone A, and one strong possibility of a new compound.Conclusion: This study has revealed that the isolated bioactive fraction of Indonesian tidal sponge, Calthropella sp., possesses potential anticancer properties with a promising significant cytotoxicity on MCF-7 cell lines (IC50 1.925 μg/mL).

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