Cytotoxic, Apoptosis-Inducing Activities, and Molecular Docking of a New Sterol from Bamboo Shoot Skin Phyllostachys heterocycla var. pubescens

Abdelhameed, Reda F. A.; Nafie, Mohamed S.; Ibrahim, Ahmed K.; Yamada, Koji; Abdel‐Kader, Maged S.; Ibrahim, Amany K.; Ahmed, Safwat A.; Badr, Jihan M.; Habib, Eman S.

doi:10.3390/molecules25235650

Cited by 11 publications

(7 citation statements)

References 34 publications

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“…As shown in Figure 4 , compound 1 treatment showed an increase at G1-phase cell-cycle arrest with 1.3-fold (59.63%, compared to 45.75% for control), while it decreased the cell population distribution at S (18.46 compared to 26.20%), G2 (15.22 compared to 18.77%), and G2/M (1.88 compared to 1.89%) phases; this may have resulted in compound 1 treatment-induced cytotoxic activity in HepG2 cells by arresting cell cycle progression at the G1 phase. These results agreed with our previous studies [ 27 , 28 ], which investigated the apoptotic activity of some solvent extracts using the flow cytometric analyses.…”

Section: Resultssupporting

confidence: 93%

Chemical Constituent Profiling of Phyllostachys heterocycla var. Pubescens with Selective Cytotoxic Polar Fraction through EGFR Inhibition in HepG2 Cells

et al. 2021

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Different extracts of the Bamboo shoot skin Phyllostachys heterocycla var. pubescens were screened against panel of cancer cell lines and normal one. The cell viability results exhibited that the ethyl acetate extract showed the least vitality percentage of 2.14% of HepG2 cells. Accordingly, it was subjected to chromatographic separation, which resulted in the isolation of a new natural product; 7-hydroxy, 5-methoxy, methyl cinnamate (1), together with four known compounds. The structures of the pure isolated compounds were deduced based on different spectroscopic data. The new compound (1) was screened against the HepG2 and MCF-7 cells and showed IC50 values of 7.43 and 10.65 µM, respectively. It induced apoptotic cell death in HepG2 with total apoptotic cell death of 58.6% (12.44-fold) compared to 4.71% in control by arresting cell cycle progression at the G1 phase. Finally, compound 1 was validated as EGFR tyrosine kinase inhibitor in both enzymatic levels (IC50 = 98.65 nM compared to Erlotinib (IC50 = 78.65 nM). Finally, in silico studies of compound 1 through the molecular docking indicated its high binding affinity towards EGFR protein and the ADME pharmacokinetics indicated it as a drug-like.

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Section: Resultssupporting

confidence: 93%

Chemical Constituent Profiling of Phyllostachys heterocycla var. Pubescens with Selective Cytotoxic Polar Fraction through EGFR Inhibition in HepG2 Cells

et al. 2021

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“…The appearance of an anomeric proton doublet resonance at δ H 4.21 (1H, d, J =7.7, H‐1′), four oxymethine signals between δ H 3.01 and δ H 3.12, and resonances for an oxymethylene at δ H 3.64 and 3.40 and the associated 13 C resonances indicated the presence of a sugar unit. A comparison with literature data confirmed that the compound is β‐sitosterol 3‐ O ‐β‐D‐glucoside [35,36] ( Figure 1).…”

Section: Resultssupporting

confidence: 54%

Antiplasmodial and Cytotoxic Activities of Extract and Compounds from Ozoroa obovata (Oliv.) R. & A. Fern. var. obovata

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et al. 2021

Chemistry & Biodiversity

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Ozoroa obovata (Oliv.) R. & A. Fern. var. obovata found in KwaZulu‐Natal in South Africa was investigated for phytochemical constituents, and for antiplasmodial and cytotoxic effects. The plant leaves were collected from the University of KwaZulu‐Natal (UKZN) arboretum on the Pietermaritzburg Campus, in March 2019. The inhibitory activity against 3D7 Plasmodium falciparum was determined using the parasite lactate dehydrogenase (pLDH) assay and cytotoxicity against HeLa cells was evaluated using the resazurin assay. The bioactive compounds were isolated by chromatographic purification and their structures were established with spectroscopic and spectrometric techniques. The plant leaf extract displayed significant antiplasmodial activity at 50 μg/mL and was also cytotoxic against HeLa cells. Chromatographic purification of the extract led to the isolation of two biflavonoids, four flavonoid glycosides, a steroid glycoside, and a megastigmene derivative. The compounds displayed antiplasmodial and antiproliferative activities at 50 μg/mL but the activity was substantially reduced at 10 μg/mL. The activities and compounds are being reported in O. obovata for the first time.

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Section: Resultssupporting

confidence: 94%

“…It increased the induction of early apoptosis by 2.44% compared to 0.61% for the control, and late apoptosis by 22.52% compared to 0.23% for the control. Our results are in accordance with our previous studies [37,38] of apoptosis induction with various isolates from medicinal plants. As shown in Figure 3, compounds 1, 2 and 5 exhibited remarkable cytotoxic activities against HepG2 cells with IC 50 values of 8.6, 12.3 and 9.4 µM, respectively.…”

Section: Annexin V/pi Stainingsupporting

confidence: 93%

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New Antiproliferative Triflavanone from Thymelaea hirsuta—Isolation, Structure Elucidation and Molecular Docking Studies

et al. 2021

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In this study isolates from Thymelaea hirsuta, a wild plant from the Sinai Peninsula of Egypt, were identified and their selective cytotoxicity levels were evaluated. Phytochemical examination of the ethyl acetate (EtOAc) fraction of the methanolic (MeOH) extract of the plant led to the isolation of a new triflavanone compound (1), in addition to the isolation of nine previously reported compounds. These included five dicoumarinyl ethers found in Thymelaea: daphnoretin methyl ether (2), rutamontine (3), neodaphnoretin (4), acetyldaphnoretin (5), and edgeworthin (6); two flavonoids: genkwanin (7) and trans-tiliroside (8); p-hydroxy benzoic acid (9) and β sitosterol glucoside (10). Eight of the isolated compounds were tested for in vitro cytotoxicity against Vero and HepG2 cell lines using a sulforhodamine-B (SRB) assay. Compounds 1, 2 and 5 exhibited remarkable cytotoxic activities against HepG2 cells, with IC50 values of 8.6, 12.3 and 9.4 μM, respectively, yet these compounds exhibited non-toxic activities against the Vero cells. Additionally, compound 1 further exhibited promising cytotoxic activity against both MCF-7 and HCT-116 cells, with IC50 values of 4.26 and 9.6 μM, respectively. Compound 1 significantly stimulated apoptotic breast cancer cell death, resulting in a 14.97-fold increase and arresting 40.57% of the cell population at the Pre-G1 stage of the cell cycle. Finally, its apoptosis-inducing activity was further validated through activation of BAX and caspase-9, and inhibition of BCL2 levels. In silico molecular docking experiments revealed a good binding mode profile of the isolates towards Ras activation/pathway mitogen-activated protein kinase (Ras/MAPK); a common molecular pathway in the development and progression of liver tumors.

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Cytotoxic, Apoptosis-Inducing Activities, and Molecular Docking of a New Sterol from Bamboo Shoot Skin Phyllostachys heterocycla var. pubescens

Cited by 11 publications

References 34 publications

Chemical Constituent Profiling of Phyllostachys heterocycla var. Pubescens with Selective Cytotoxic Polar Fraction through EGFR Inhibition in HepG2 Cells

Chemical Constituent Profiling of Phyllostachys heterocycla var. Pubescens with Selective Cytotoxic Polar Fraction through EGFR Inhibition in HepG2 Cells

Antiplasmodial and Cytotoxic Activities of Extract and Compounds from Ozoroa obovata (Oliv.) R. & A. Fern. var. obovata

New Antiproliferative Triflavanone from Thymelaea hirsuta—Isolation, Structure Elucidation and Molecular Docking Studies

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