Apoptotic Potential of Artemsia sieberia Besser (Asteraceae) Fraction against Human Cancer Cell Lines

Purpose: To investigate the anti-proliferative and apoptotic activity of crude and dichloromethane fraction of A. sieberi against seven cancer cell lines (Colo20, HCT116, DLD, MCF7, Jurkat, HepG2 and L929).Methods: A. sieberi was extracted with methanol and further purification was carried out using liquidliquid extraction with hexane, dichloromethane and ethyl acetate. Each extract was assayed for cytotoxic potential against cancer cell lines using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium Bromide (MTT) assay. The morphology of the HepG2 cell nucleus was investigated by Hoechst 33342, DNA-binding dye. A Tali™ image-based cytometer was used to assess cell viability, death and apoptosis using annexin-v /pi (propidium iodide). A chromatographic fingerprint was constructed using high performance liquid chromatography (HPLC).Results: The most effective anticancer activity of the unrefined methanol extract was against HepG2 cell lines (LC50 = 161.5 μg/mL). The hexane and ethyl acetate fractions showed no antiproliferative activity. The dichloromethane fraction displayed higher cytotoxic activity (LC50 = 61.75 μg/mL) and also repressed the migration of the cells. About 50 % of HepG2 cells were apoptotic when treated for 24 h with the dichloromethane fraction at the concentration of 120 μg/mLConclusion: A. sieberi possesses apoptotic activity and inhibited the migration of the HepG2 cell lines.Keywords: Artemsia Sieberia, Apoptosiss, Cytotoxicity, Hoescht staining, HepG2 cell line

ANTICANCER POTENTIAL OF PLANT EXTRACTS FROM RIYADH (SAUDI ARABIA) ON MDA-MB-231 BREAST CANCER CELLS

Background: Medicinal plants have been used in traditional medicine for the treatment of numerous diseases worldwide. There is a dire need for new anticancer agents and plants used in traditional medicine are a particularly useful source. Materials and methods: In this study, extracts of five different plants that grow in the desert of Saudi Arabia were evaluated to assess their cytotoxicity against the MDA-MB-231 breast cancer cell line. Soxhlet extraction was carried out on the leaves and stems using different solvents. The cytotoxicity of these extracts against MDA-MB-231 breast cancer cells was assessed using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays. The apoptotic cellular morphological changes were observed using inverted and fluorescence microscopes. Results: Our results showed that two of the five different medicinal plants (Rumex vesicarius and Malva parviflora) exhibited strong anticancer activity against the breast cancer cells. Specifically, 2 of the 40 extracts (from the five studied plants) showed promising activity. The chloroform extract of the stem of R. vesicarius (RSV CHCL3) exhibited moderate anticancer activity with a half-maximal inhibitory concentration (IC50) of 230 µg/mL while that of the hexane extract of M. parviflora stems (MPS Hex) was 248 µg/mL. Loss of cell integrity, shrinkage of the cytoplasm, and cell detachment were observed in the extract-treated MDA-MB-231 cells. Conclusion: R. vesicarius and M. parviflora chloroform and n-hexane stem extracts showed significant cytotoxicity against MDA-MB-231 human breast carcinoma cells

Psiadia punctulata (DC.) Vatke induces cell apoptosis in highly metastatic MDA-MB-231 cells

Purpose: This study assessed the in vitro cell migration inhibitory and cell apoptotic effects of P. punctulata stem (PPS (and leaf hexane) PPL (extracts on breast cancer cell lines (MDA-MB-231 andMCF-7 cells).Methods: Cytotoxicity was quantified using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LD) release test after 48 h exposure of MDA-MB-231 cells to 0 – 200 μg/mL of PPS and PPL hexane extract. Cell apoptosis was determined using Muse™ cell cytometry, while the phytoconstituents of PPS and PPL hexane extracts were identified by gas chromatography–mass spectrometry.Results: The half-maximal inhibitory concentration (IC50) for PPS and PPL hexane extracts against MDA-MB-231 cells was 44.33 and 52.16 μg/mL, respectively. T, whereas the IC50 of PPS and PPL hexane extracts was 102.22 and 59.53 μg/mL against MCF-7 cells, sequentially. Treatment with 100 and 200 μg/mL of PPS and PPL hexane extract increased late apoptosis in MDA-MB-231 cells to 16.005 ± 1.155 and 52.58 ± 3.02 %, respectively, for PPS hexane extract and 77.34 ± 0 % and 95.21 ± 1.61 %, respectively, for PPL hexane extract, when compared to control cells (3.81% ± 0.79%). PPL hexane extract decreased cell migration and filled ~15.5 % of the wound gap on MDA-MB-231 cells after 24 h, while PPS hexane extract decreased cell migration by ~35 and ~42.5 % at 24 and 48 h, respectively. PPS and PPL hexane extracts contained several phytocompounds. Stem and leaf extracts of P. punctulata showed significant (p < 0.05) cell apoptotic and migration inhibition activities.Conclusion: The extracts P. punctulata exhibit potent cytotoxic activity against the tested breast cancer cells. Further research is required to assess the acute and subacute toxicity of the extracts

Phytochemical screening and GC-MS chemical profiling of an innovative anti-cancer herbal formula (PHF6)

The present investigation assessed the anticancer potential and chemical profile of the polyherbal formulation (PHF6) against human breast cancer cells. The plants (Alchemilla vulgaris, Cichorium pumilum, Crataegus azarolus, Eruca sativa, Ferula hermonis, and Hypericum triquetrifolium) were combined in equal quantities and extracted using soxhlet apparatus. The total polyphenolic (TPC) of the hexane and chloroform extract of PHF6 were 3.11 ± 0.004 and 7.88 ± 0.004 µg/mL (as gallic acid equivalent), respectively. The radical scavenging activity (RSA) values for the hexane and chloroform extract were 35.1 % ±0.01 and 36.9 % ±0.06, respectively. For hexane extract, the IC50 values were found to be 82.8 and 48.7 µg/mL against MCF-7ER(+)/PR(+) and MDA MB-231ER(−)/PR(−), respectively. Similarly, the IC50 value of chloroform extract was 44.4 µg/mL against both cell lines. The MDA MB-231ER(−)/PR(−) cells stained with DAPI post-treatment with hexane and chloroform extract showed cell shrinkage, nuclear fragmentation, and chromatin condensation. Moreover, GC–MS screening of the PHF6 revealed several compounds with different reported biological activities, such as phytol and octadecanoic acid. PHF6 showed promising anticancer activity against cancer cells tested, thus deserving more clinical studies in the future

Exploring the therapeutic potential of GC–MS separated compounds from Dracaena cinnabari against dengue virus and Aedes aegypti using in silico tools

The paper's main aim was to investigate bioactive molecules in Dracaena cinnabari extract using gas chromatography-mass spectroscopy (GC–MS) and to assess their therapeutic potential using molecular docking algorithm, ProTox II and ADME studies on dengue virus and Aedes aegypti. Molecular docking was carried out using AutoDock Vina, followed by drug-likeness potential and toxicity using in silico tools (ProTox II and ADME). A total of 25 different compounds were detected in the methanol extract, and the major compounds were cis-13-Octadecenoic acid (19.04 %), n-Hexadecanoic acid (16.5 %), beta-Sitosterol (10.5 %), and n-Heptadecanol-1 (9.74 %). Molecular docking revealed that beta-Sitosterol and stigmasterol are the lead compounds and scored the highest docking value among the compounds. The best-docked ligand score for dengue virus was recorded for 4V0Q (stigmasterol, −9.0 kcal/mol), whereas the best-docked ligand score for Ae. agypti was recorded for 1PZ4 (beta-Sitosterol, −9.9 kcal/mol). The toxicity prediction for the beta-Sitosterol and 4,4′-Dihydroxy-2 methoxydihydrochalcone did not violate the Lipinski rules. The values of LD50 predicted using ProTox II revealed that stigmasterol, 4,4′-dihydroxy-2-methoxydihydrochalcone, beta-Sitosterol, and vitamin E ranged from 890 to 5000 mg kg − 1 in a rat model. This study depicts the potential of promising molecules of D. cinnabari. However, in vivo and in vitro investigation is needed to support the results of this study

Cytotoxic potential of Commicarpus plumbagineus extracts against liver cancer cell lines through In-Vitro and In-Silico methods

Hepatocellular carcinoma holds the fifth position in terms of worldwide cancer prevalence. The challenges posed by drug adverse effects and resistance associated with existing anticancer therapies underscore the importance of exploring natural sources for potential solutions. This study assessed the in-vitro cytotoxicity of a range of solvent extracts (n-hexane, ethyl acetate, and methanol) against liver cancer cell lines using (3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) (MTT) assay. The bioactive extract was also examined for its impact on cell migration and subjected to in-silico predictions targeting 14 different protein targets. The results indicated that only the ethyl acetate (F2) extract was cytotoxic. The IC50 values for the F2 were 300, 320 and 318 μg/mL against HepG2, HuH7, and normal HUVECs cell lines, respectively. A significant reduction in the % relative migration of cells following treatment with 87.5 μg/mL of F2 extract was observed. The apoptotic potential of F2 was seen on HepG2 cells using the DAPI and AO/EtBr staining. The F2 extract underwent GC–MS analysis, uncovering the existence of 23 phytocompounds, which were subsequently employed in molecular docking studies. Loperamide, á-Sitosterol, and stigmasterol exhibited the highest binding affinity (−10.90 kcal/mol) for 4WEV and 4NOS. These phytochemicals from the F2 extract hold potential as promising drug candidates for liver cancer, subject to further validation

Phytochemical analysis and antibacterial activity of Washingtonia filifera (Lindl.) H. Wendl. fruit extract from Saudi Arabia

This work aimed to assess the antimicrobial potential of Washingtonia filifera extracts on some human pathogens. Agar well diffusion and minimum inhibitory concentrations (MIC) methods have been used to assess the antimicrobial activities of W. filifera extract against Staphylococcus aureus, Klebsiella pneumonia, Acinetobacter baumannii, Escherichia coli, and Candida albicans. Only the ethyl acetate (ETAC) and methanol extracts revealed antimicrobial activity against tested microorganisms. S. aureus appears to be the most sensitive microbes to the ETAC extract with equal inhibition zone (30 mm) and MIC (65 µg/mL) values. This is followed by K. pneumoniae, E. coli, and A. baumanni, respectively. The plant extract had different phytochemical constituents such as alkaloids, sterols, and polyphenols. Column chromatography of the ETAC extract resulted in the loss of inhibitory effect at the highest concentration tested (50 mg/mL) against tested microorganisms. The haemolytic activity of the different extracts was found in the following order: Hexane (83.57%) > ETAC (35.71%) > chloroform (23.57143) > methanol (0.71%) based on the highest concentration tested (8.3 mg/mL). In conclusion, ETAC extract was the most promsing extract among extracts tested. Secondary plant metabolites are of great value as natural antimicrobial agents

In vitro antiproliferative efficacy of Annona muricata seed and fruit extracts on several cancer cell lines

In Saudi Arabia, breast cancer is the second-most frequently identified common malignant cause of death for women. The present investigation was carried out to assess the impact of different Soxhlet solvent extracts of Annona muricata on apoptosis induction in breast cancer cells. Cell survival was estimated by post-incubation of cells with the extract for 24 h using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium (MTT) assay. Acridine orange (AO)/propidium iodide (PI) and 4′,6-diamidino-2-phenylindole (DAPI) staining were employed to study cell apoptosis. qRT-PCR was also employed to assess apoptotic genes’ expression, such as BAX and P53 genes. The results of the MTT assay showed that the chloroform extract inhibited the proliferation of MDA-MB-231 and MCF-7 cells dose-dependently. AO/PI and DAPI staining showed chromatin condensation and fragmentation. In treated cells, P53 expression significantly increased, correlated with the increase in BAX activity. The findings suggest that apoptosis may have been triggered post-chloroform extract treatment. Combining chloroform extract of A. muricata and doxorubicin at a 1:1 ratio increased the IC50 value (292.3 µg/mL). The chloroform extract of A. muricata contained a variety of substances, including diethyl carbonate (7.38%), 4-acetoxy-2,11-dodecadiene (58.13%), and hexadecanoic acid (34.48%), according to the results of the gas chromatography-mass spectrometry analysis. As a result, future research on the A. muricata chloroform extract as a potential anticancer drug could be suggested

Rational design of Ag-ZnO-Fe3O4 nanocomposite with promising antimicrobial activity under LED light illumination

Surface plasmon resonance effect, Fenton's reaction, plant extract, and nanoparticles have all proven to be efficient in killing or reducing the activity of numerous microorganisms. To study the synergetic effects among these key parameters, Ag-ZnO-Fe3O4 nanocomposites have been synthesized via solution combustion approach in the presence of aqueous extract of Thymus vulgaris leaves. The successful construction of Ag-ZnO-Fe3O4 nanocomposite and its purity were confirmed by X-ray diffraction, X-ray photoelectron spectra, and energy dispersive X-Ray spectroscopy analyses. Dynamic light scattering and transmission electron microscopy measurements showed that the size of the obtained particles is in the nanoscale. The synthesized nanocomposite showed broad inhibition against the selected bacteria and yeast under LED light. UV-vis absorption measurement showed that the heterostructure exhibits broad plasmonic peak centered around 434 nm. Hot charge carriers are generated in Ag under LED light illumination and separated through Ag-ZnO heterojunction resulting in the production of a considerable amount of (OH)-O-center dot radicals as confirmed by ESR analysis. Moreover, Ag acts as H2O2 donator and photogenerated electrons provider for the Fenton's reaction, resulting in the generation of much more (OH)-O-center dot radicals. Therefore, Ag-ZnO-Fe3O4 nanocomposite shows improved microbial activity under LED light illumination

Synthesis, Structure and <i>In Vitro</i> Anticancer Activity of Pd(II) Complex of Pyrazolyl-<i>s</i>-Triazine Ligand; A New Example of Metal-Mediated Hydrolysis of <i>s</i>-Triazine Pincer Ligand

The square planar complex [Pd(PT)Cl(H2O)]*H2O (HPT: 6-(3,5-dimethyl-1H-pyrazol-1-yl)-1,3,5-triazine-2,4(1H,3H)-dione) was obtained by the reaction of 2-methoxy-4,6-bis(3,5-dimethyl-1H-pyrazol-1-yl)-1,3,5-triazine (MBPT) pincer ligand with PdCl2 in a molar ratio (1:1) under thermal conditions and using acetone as a solvent. The reaction proceeded via C-N cleavage of one C-N moiety that connects the pyrazole and s-triazine combined with the hydrolysis of the O-CH3 group. The reaction of the chloride salt of its higher congener (PtCl2) gave [Pt(3,5-dimethyl-1H-pyrazole)2Cl2]. The crystal structure of [Pd(PT)Cl(H2O)]*H2O complex is stabilized by inter- and intra-molecular hydrogen bonding interactions. Hirshfeld analysis revealed that the H...H (34.6%), O...H (23.6%), and Cl...H (7.8%) interactions are the major contacts in the crystal. The charges at Pd, H2O, Cl and PT are changed to 0.4995, 0.2216, −0.4294 and −0.2917 instead of +2, 0, −1 and −1, respectively, using the MPW1PW91 method. [Pd(PT)Cl(H2O)]*H2O complex has almost equal activities against MDA-MB-231 and MCF-7 cell lines with IC50 of 38.3 µg/mL