Meroterpenoids from the Fungus Ganoderma sinensis and First Absolute Configuration Clarification of Zizhine H

Five new meroterpenoids, zizhines P-S and U (1−4,7), together with two known meroterpenoids (5 and 6) were isolated from Ganoderma sinensis. Their structures including absolute configurations were assigned by using spectroscopic, computational, and chemical methods. Racemics zizhines P and Q were purified by HPLC on chiral phase. Biological evaluation found that 4, 5 and 6 are cytotoxic toward human cancer cells (A549, BGC-823, Kyse30) with IC50 values in the range of 63.43–80.83 μM towards A549, 59.2 ± 2.73 μM and 64.25 ± 0.37 μM towards BGC-823, 76.28 ± 1.93 μM and 85.42 ± 2.82 μM towards Kyse30.

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Cassaine Diterpenoid Amide from Stem Bark of Erythrophleum fordii Suppresses Cytotoxic and Induces Apoptosis of Human Leukemia Cells

Molecules ◽

10.3390/molecules25143304 ◽

2020 ◽

Vol 25 (14) ◽

pp. 3304 ◽

Cited By ~ 1

Author(s):

Tu Thanh Thi Nguyen ◽

Dao Cuong To ◽

Phuong Hien Thi Vo ◽

Thanh Hoa Tran ◽

Phi Hung Nguyen ◽

...

Keyword(s):

Cancer Cells ◽

Human Cancer ◽

Stem Bark ◽

Binding Energies ◽

Human Leukemia ◽

Allosteric Site ◽

Human Cancer Cells ◽

Ic50 Values ◽

Erythrophleum Fordii ◽

Parp 1

Cassaine diterpenoids amides from the stem bark of Vietnamese Erythrophleum fordii Oliver were screened for their cytotoxic activity against human cancer cells. The cell proliferation assay results showed that, among the active compounds, 3β-acetyl-nor-erythrophlamide (3AEP) exhibited the most potential cytotoxicity against human leukemia HL-60 and KG cells with IC50 values of 12.0 ± 1.2 and 18.1 ± 2.7 µM, respectively. Treatment of 3AEP resulted in the apoptosis of HL-60 cells via the activation of caspase 3, and poly (ADP-ribose) polymerase (PARP). Molecular docking in silico results showed that the 3AEP can bind to both the procaspase-3 allosteric site and the PARP-1 active site, with binding energies of −7.51 and −9.63 kcal/mol respectively. These results indicated that the stem bark of Vietnamese E. fordii and its cassaine diterpenoid amides may be useful in the apoptosis induction of human leukemia cancer cells.

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3-Amino-thieno[2,3-b]pyridines as microtubule-destabilising agents: Molecular modelling and biological evaluation in the sea urchin embryo and human cancer cells

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2016.11.041 ◽

2017 ◽

Vol 25 (2) ◽

pp. 658-664 ◽

Cited By ~ 14

Author(s):

Chatchakorn Eurtivong ◽

Victor Semenov ◽

Marina Semenova ◽

Leonid Konyushkin ◽

Olga Atamanenko ◽

...

Keyword(s):

Cancer Cells ◽

Sea Urchin ◽

Molecular Modelling ◽

Human Cancer ◽

Biological Evaluation ◽

Human Cancer Cells ◽

Sea Urchin Embryo

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Synthesis of novel flavone derivatives possessing substituted benzamides and their biological evaluation against human cancer cells

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2016.07.063 ◽

2016 ◽

Vol 26 (17) ◽

pp. 4170-4173 ◽

Cited By ~ 3

Author(s):

Bo Hee Yun ◽

Young Hun Lee ◽

Kyung Tae Park ◽

Su Jin Jung ◽

Yong Sup Lee

Keyword(s):

Cancer Cells ◽

Human Cancer ◽

Biological Evaluation ◽

Human Cancer Cells ◽

Substituted Benzamides ◽

Flavone Derivatives

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Synthesis and biological evaluation of novel artemisone–piperazine–tetronamide hybrids

RSC Advances ◽

10.1039/d1ra00750e ◽

2021 ◽

Vol 11 (30) ◽

pp. 18333-18341

Author(s):

Meng-Xue Wei ◽

Jia-Ying Yu ◽

Xin-Xin Liu ◽

Xue-Qiang Li ◽

Jin-Hui Yang ◽

...

Keyword(s):

Cancer Cells ◽

Human Cancer ◽

Biological Evaluation ◽

Human Cancer Cells ◽

Synthesis And Biological Evaluation

Six novel artemisone–piperazine–tetronamide hybrids were efficiently synthesised and investigated for their cytotoxicity against some human cancer cells.

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Sulforaphene Isolated from Radish (Raphanus Sativus L.) Seeds Inhibits Growth of Six Cancer Cell Lines and Induces Apoptosis of A549 Cells

10.20944/preprints201807.0060.v1 ◽

2018 ◽

Author(s):

Sooyeon Lim ◽

Jinchul Ahn ◽

Eun Jin Lee ◽

jongkee Kim

Keyword(s):

Cancer Cells ◽

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

A549 Cells ◽

Adenosine Diphosphate ◽

Cancer Cell Lines ◽

Human Cancer Cells ◽

Ic50 Values ◽

Induced Apoptosis

Sulforaphene (SFE), a major isothiocyanate in radish seeds, is a close chemical relative of sulforaphane (SFA) isolated from broccoli seeds and florets. The anti-proliferative mechanisms of SFA against cancer cells have been well investigated, but little is known about the potential anti-proliferative effects of SFE. In this study, we showed that SFE purified from radish seeds inhibited the growth of six cancer cell lines (A549, CHO, HeLa, Hepa1c1c7, HT-29, and LnCaP), with relative half maximal inhibitory concentration (IC50) values ranging from 1.37 to 3.31 g/mL. Among the six cancer cell lines evaluated, SFE showed the greatest growth inhibition against A549 lung cancer cells. In A549 cells, SFE induced apoptosis via changes in the levels of poly (adenosine diphosphate ribose) polymerase and caspase-3, -8, and -9. Our results indicate that SFE from radish seeds may have significant anti-proliferative potency against a broad range of human cancer cells via induction of apoptosis.

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Design, synthesis and biological evaluation of novel carbamodithioates as anti-proliferative agents against human cancer cells

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2018.07.038 ◽

2018 ◽

Vol 157 ◽

pp. 1526-1540 ◽

Cited By ~ 1

Author(s):

Xia Liu ◽

Zhijun Wang ◽

Rui Xie ◽

Pingwah Tang ◽

Qipeng Yuan

Keyword(s):

Cancer Cells ◽

Human Cancer ◽

Biological Evaluation ◽

Design Synthesis ◽

Human Cancer Cells ◽

Synthesis And Biological Evaluation

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Unsymmetric dihydropyridines bearing 2-pyridyl methyl carboxylate as modulators of P-glycoprotein; synthesis and biological evaluation in resistant and non-resistant cancer cells

Canadian Journal of Chemistry ◽

10.1139/cjc-2018-0351 ◽

2019 ◽

Vol 97 (8) ◽

pp. 603-614

Author(s):

Maryam Nejati ◽

Hossein Sadeghpour ◽

Sara Ranjbar ◽

Katayoun Javidnia ◽

Najmeh Edraki ◽

...

Keyword(s):

Cancer Cells ◽

Human Cancer ◽

Binding Mode ◽

Biological Evaluation ◽

Multi Drug Resistance ◽

Glycoprotein P ◽

Glycoprotein Synthesis ◽

Human Cancer Cells ◽

P Glycoprotein ◽

Mdr Reversal

Multi-drug resistance (MDR) in cancer cells is often associated with overexpression of P-glycoprotein (P-gp or ABCB1 or MDR1); therefore, modulators of this transporter might be helpful in overcoming MDR. In this study, 16 novel unsymmetrical dihydropyridine (DHP) derivatives bearing 2-pyridyl methyl carboxylate at C3 and a nitroimidazole or nitrophenyl ring at C4 positions of the DHP ring were synthesized. Their cytotoxicity was tested against four human cancer cells by MTT assay. The reversal capacity of MDR was examined in P-gp overexpressing cells (MES-SA/DX5) by measuring the alteration of doxorubicin’s IC50 and performing flow cytometric determination of intracellular rhodamine 123 accumulation. The calcium channel blocking (CCB) activity, as a side effect of DHPs, was tested on the ileum of a guinea pig. Molecular docking was performed to explain the binding mode of compounds. Two derivatives, 4a and 4c, containing 4-nitrophenyl at C4 and possessing methyl (4a) and iso-propyl (4c) carboxylates at the C5 position of DHP core demonstrated superior cytotoxic and MDR reversal activities and lower CCB effect. Docking analysis confirmed the importance of the 4-nitrophenyl ring for P-gp inhibitory activity. Some of the synthesized DHP derivatives with considerable MDR reversal capacity could be promising compounds for further discovery of useful agents for management of drug resistant cancer.

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