Cerbera odollam fruit extracts enhance anti-cancer activity of sorafenib in HCT116 and HepG2 cells DOI Open Access
Supawadee Parhira, Orakot Simanurak,

Khemmachat Pansooksan

et al.

Chinese Herbal Medicines, Journal Year: 2024, Volume and Issue: 17(1), P. 108 - 126

Published: Nov. 20, 2024

While higher therapeutic doses of toxic cardiac glycosides derived from Cerbera odollam are frequently employed in cases suicide or homicide, ongoing research is investigating the potential anticancer properties low-concentration extracts obtained fruits C. odollam. The present study aimed to determine enhanced effects and minimize side combining Thailand with sorafenib against HCT116 HepG2 cells. dried powder fresh green was fractionated, its phytochemical contents, including total glycosides, phenolics, flavonoids, triterpenoids, were quantified. cytotoxic these fractions evaluated cells using MTT assay. showing most significant response subsequently combined examine their synergistic effects. Apoptosis induction, cell cycle progression, mitochondrial membrane (MMP) then assessed. underlying mechanism apoptotic effect further investigated by analyzing reactive oxygen species (ROS) generation expression levels antioxidant proteins. Phytochemical analysis showed that odollam-ethyl acetate fraction (COEtOAc) rich while dichloromethane (CODCM) contained high triterpenoids saponins. Following 24 h treatment, COEtOAc, responded well CODCM IC50 values (42.04 ± 16.94) μg/mL (123.75 14.21) μg/mL, respectively. Consequently, COEtOAc (20 μg/mL) (30 μg/mL), both administered at sub-IC50 concentrations, 6 μmol/L for 2 cells, incubated h. This combination resulted a suppression viability approximately 50%. treatments markedly apoptosis, diminished MMP, triggered G0/G1 phase arrest compared each treatment individually. Concurrently, increased formation ROS decreased enzymes superoxide dismutase catalase supported proposed apoptosis induction treatment. Importantly, demonstrated specific targeted action favorable safety profile, as evidenced HFF-1 displaying 2-3 times than those cancer Utilizing concentrations can enhance beyond achieved single-agent treatments, mitigating opposing Future will focus on extracting characterizing active constituents, especially compounds plants.

Language: Английский

Anticancer evaluations of iodoquinazoline substituted with allyl and/or benzyl as dual inhibitors of EGFRWT and EGFRT790M: design, synthesis, ADMET and molecular docking DOI Creative Commons
Ahmed K. B. Aljohani, Khaled El‐Adl, Basmah Almohaywi

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(12), P. 7964 - 7980

Published: Jan. 1, 2024

Fifteen new iodoquinazoline derivatives, 5a,b to 18, are reported in this study and their anticancer evaluation as dual inhibitors of EGFR WT T790M .

Language: Английский

Citations

5
Exploration of the VEGFR-2 inhibition activity of phthalazine derivatives: design, synthesis, cytotoxicity, ADMET, molecular docking and dynamic simulation DOI Creative Commons

Hatem Hussein Bayoumi,

Mohamed‐Kamal Ibrahim,

Mohammed A. Dahab

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(30), P. 21668 - 21681

Published: Jan. 1, 2024

Novel phthalazine derivatives were designed, synthesized and evaluated against Hep G2 MCF-7 as VEGFR-2 inhibitors.

Language: Английский

Citations

4
Rational design, docking, syntheses, ADMET and cytotoxicity assessments of iodoquinazoline derivatives as inhibitors of EGFRT790M and VEGFR-2 DOI
Ahmed K. B. Aljohani, Marwa Alsulaimany,

Omar M. Alatawi

et al.

Journal of Molecular Structure, Journal Year: 2025, Volume and Issue: unknown, P. 141634 - 141634

Published: Jan. 1, 2025

Language: Английский

Citations

0
Enhancement of apoptosis in HCT116 and HepG2 cells by Coix lacryma-jobi var. lacryma-jobi seed extract in combination with sorafenib DOI Open Access
Supawadee Parhira, Guo‐Yuan Zhu, Apirath Wangteeraprasert

et al.

Chinese Herbal Medicines, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 1, 2025

Language: Английский

Citations

0
Rationale, in silico docking, ADMET profile, design, synthesis and cytotoxicity evaluations of phthalazine derivatives as VEGFR-2 inhibitors and apoptosis inducers DOI Creative Commons

Hatem Hussein Bayoumi,

Mohamed‐Kamal Ibrahim,

Mohammed A. Dahab

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(37), P. 27110 - 27121

Published: Jan. 1, 2024

New phthalazine derivatives as vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors were synthesized joined to different spacers including pyrazole, α,β-unsaturated ketonic fragment, pyrimidinone and/or pyrimidinthione.

Language: Английский

Citations

2
Exploration of cytotoxicity of iodoquinazoline derivatives as inhibitors of both VEGFR‐2 and EGFRT790M: Molecular docking, ADMET, design, and syntheses DOI Open Access
Marwa Alsulaimany,

Sanadelaslam S. A. El‐Hddad,

Zuhir S. M. Akrim

et al.

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 357(11)

Published: Aug. 1, 2024

Novel inhibitors of epidermal growth factor receptor (EGFR)

Language: Английский

Citations

1
Cerbera odollam fruit extracts enhance anti-cancer activity of sorafenib in HCT116 and HepG2 cells DOI Open Access
Supawadee Parhira, Orakot Simanurak,

Khemmachat Pansooksan

et al.

Chinese Herbal Medicines, Journal Year: 2024, Volume and Issue: 17(1), P. 108 - 126

Published: Nov. 20, 2024

While higher therapeutic doses of toxic cardiac glycosides derived from Cerbera odollam are frequently employed in cases suicide or homicide, ongoing research is investigating the potential anticancer properties low-concentration extracts obtained fruits C. odollam. The present study aimed to determine enhanced effects and minimize side combining Thailand with sorafenib against HCT116 HepG2 cells. dried powder fresh green was fractionated, its phytochemical contents, including total glycosides, phenolics, flavonoids, triterpenoids, were quantified. cytotoxic these fractions evaluated cells using MTT assay. showing most significant response subsequently combined examine their synergistic effects. Apoptosis induction, cell cycle progression, mitochondrial membrane (MMP) then assessed. underlying mechanism apoptotic effect further investigated by analyzing reactive oxygen species (ROS) generation expression levels antioxidant proteins. Phytochemical analysis showed that odollam-ethyl acetate fraction (COEtOAc) rich while dichloromethane (CODCM) contained high triterpenoids saponins. Following 24 h treatment, COEtOAc, responded well CODCM IC50 values (42.04 ± 16.94) μg/mL (123.75 14.21) μg/mL, respectively. Consequently, COEtOAc (20 μg/mL) (30 μg/mL), both administered at sub-IC50 concentrations, 6 μmol/L for 2 cells, incubated h. This combination resulted a suppression viability approximately 50%. treatments markedly apoptosis, diminished MMP, triggered G0/G1 phase arrest compared each treatment individually. Concurrently, increased formation ROS decreased enzymes superoxide dismutase catalase supported proposed apoptosis induction treatment. Importantly, demonstrated specific targeted action favorable safety profile, as evidenced HFF-1 displaying 2-3 times than those cancer Utilizing concentrations can enhance beyond achieved single-agent treatments, mitigating opposing Future will focus on extracting characterizing active constituents, especially compounds plants.

Language: Английский

Citations

1