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Colorectal cancer is known for its substantial impact on global morbidity and mortality, with higher prevalence in developed regions. This study delves into the potential treatment advantages of resveratrol (RSV) in addressing colorectal cancer. Apoptosis and gene expression associated with apoptotic factors were explored using Caco-2 cells, a pertinent model for colorectal adenocarcinoma. The effect of RSV on Caco-2 cell viability was investigated using MTT assay and neutral red uptake assay. The level of generated ROS was high in cells exposed to RSV. Likewise, the enzyme superoxide dismutase, responsible for converting ROS into hydrogen peroxide, was concurrently elevated. The effect of RSV on DNA damage was examined through the TUNEL assay. The gene expression analyses for pro-apoptotic elements were studied using qRT-PCR. Furthermore, the impact of RSV on the migration of Caco-2 cells was conducted through a wound-healing assay. Our results reveal RSV’s cytotoxicity on Caco-2 cells, showing dose-dependent inhibition of viability, indicating its promise as a treatment agent. The induction of cell death by apoptosis is substantiated by DNA damage. Notably, the upregulated expression of caspase-3, Bax, and p53 genes suggests RSV’s potential to modulate key apoptosis-related elements. In addition, RSV displayed an inhibitory effect on cellular migration, a significant (p < 0.05 and p < 0.01) in cancer metastasis. These findings underscore RSV’s potential to be a multifaceted therapeutic agent targeting apoptosis and metastatic processes in colorectal cancer.

Dengue virus (DENV) infection is one of the diseases for which no drug is available for the treatment. The DENV NS2B-NS3 protease is considered to be the prime target for anti-dengue drug development because of its importance in the development of new virus subunits via DENV poly-protein breakdown. Pentacyclic triterpenoids (Lantadenes) from the weed Lantana camara L. and its semi-synthetic congeners have shown a wide array of biological activities in the last two decades. The virtual screening strategy was used on the library of 78 natural and semi-synthetic lantadenes to predict the potent antagonists for the NS2B-NS3 protease enzyme of DENV and their experimental validation by in vitro assay of lead molecules. In the in silico analysis of 78 triterpenoids, two lead molecules (−10.60 and −9.93 kcal/mol) were predicted to be inhibitors of protease (viral) when compared to its reference ligand 1,8-dihydroxy-4,5-dinitroanthraquinone (−5.377 kcal/mol). At the same time, binding affinity, pharmacokinetic, and toxicity profiling, along with molecular dynamics simulations, were studied. The in vitro viral infection inhibition assay inferred that lead molecule 62 exhibited a 60% and 45% reduction in DENV titers at 10 and 5 µM concentrations, respectively. The lead molecule 62 can further be optimized for its pharmacophore and has the potential to be developed as a drug-like molecule.

Multiple beneficial effects have been reported to numerous species of Capparis genus. Among these, Capparis spinosa has exhibited several biological benefits, including anti-inflammatory hepatoprotective, antioxidant, and antidiabetic effects. Herein, C. spinosa was extracted with different solvents and the ability of these fractions to suppress nitric oxide (NO) production in RAW 264.7 cells were assessed via Griess reagent. The effects of C. spinosa fractions on different inflammatory markers were also determined in THP-1 and Human umbilical vein endothelial cells (HUVEC) using reverse transcription polymerase chain reaction. Additionally, high-performance liquid chromatography (HPLC) ultra-violet was employed to estimate the presence of three flavonoid compounds, namely, apigenin, kaempferol, and rutin. Our results indicate that chloroform (CHCl3) and ethyl acetate (EtOAc) fractions of C. spinosa exhibited a promising anti-inflammatory activity via in vitro inhibition of NO in lipopolysaccharide stimulated RAW 264.7 cells. Pretreated stimulated THP-1 cells with either CHCl3 or EtOAc fractions showed decreased expression of interleukin 1 beta (IL-1β) and tumor necrosis factor Alpha in a dose-dependent manner. In HUVEC cells, both fractions downregulate the expression of IL-1β, upregulate the peroxisome proliferator-activated receptor alpha PPAR-α while no significant impact was observed on PPAR-ϒ gene expression. The presence of apigenin, kaempferol, and rutin in the crude extract has been confirmed through HPLC method. Collectively, these results support the ethnopharmacological usage of C. spinosa as a potential therapy for inflammation related conditions including atherosclerosis.

Colorectal cancer remains a challenging medical issue worldwide, and utilizing natural products and plants to produce novel, effective and safe therapies against this disease is continuously a sought-after strategy. Fruit and leaf extracts of Pithecellobium dulce (P. dulce) showed potential anticancer properties as they induced apoptosis of breast cancer and Dalton’s lymphoma ascites cells. Thus, the main objective of the current study is to determine whether the seed extract of P. dulce will affect apoptosis, cell cycle, migration, and inflammation of LoVo colorectal cancer cells. The high-resolution liquid chromatography–mass spectrometry was used to determine the chemical composition of the P. dulce seed extract, which revealed the presence of 35 phytochemicals. The findings of this study indicated a significant cytotoxic effect of seeds of this plant in colorectal cancer characterized by induction of apoptosis, cell cycle arrest, and reduction of migration. In addition, the seed extract suppressed several genes that are essential for cancer progression such as MMP2, MMP9, and IL-8, and, on the other hand, upregulated pro-apoptotic genes such as BAX and P53. This study has established P. dulce as a potential and valuable source for providing future therapies against colorectal cancer and other cancers.

Cancer is the second largest cause of mortality worldwide. Many natural bioactive chemicals generated from plants have favorable impacts on health, including cancer chemoprevention, compared to their manufactured counterparts. Persicaline, a novel sulfur-containing imidazoline alkaloid derived from Salvadora persica, has been shown to display promising antioxidant activity. In this study, the antiproliferative activity of persicaline was tested against different cancer cells using (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay. The cell death mode and cell-cycle arrest were examined using flow cytometry analysis. In addition, the proapoptotic and molecular mechanism effects of persicaline against mammary MCF-7 cell line were explored. Furthermore, the impact of persicaline on apoptotic genes markers, generation of reactive oxygen species (ROS), and mitochondrial membrane potential were monitored. It was found that persicaline inhibits cell proliferation in a dose-dependent manner. Persicaline-treated MCF-7 cells also showed initiation of apoptotic events and G1 cell-cycle arrest. In addition, persicaline treatment led to an increase in ROS generation, Bax and caspase upregulation while the Bcl-2 was downregulated. Hence, for the first time, this study showed that persicaline causes G1 phase arrest and apoptosis induction in MCF-7 cells. Increased proapoptotic genes and ROS levels were required for the antiproliferative and apoptotic effects of persicaline.

Dodonaea viscosa (Sapindaceae) was collected from Riyadh, Saudi Arabia. For the simultaneous measurement of quercetin and kaempferol, a validated high-performance thin-layer chromatography (HPTLC) approach was devised in D. viscosa leaf extract. The antioxidant activity was evaluated using diphenyl 1-picrylhydrazyl (DPPH) and 2,2′-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays. Moreover, the cytotoxic effect was tested against three cancer cell lines A549, HepG2, and MDA-MB-231. The potential anti-inflammatory properties of different fractions of D. viscosa were also evaluated using lipopolysaccharide (LPS)-induced THP-1 macrophages cells. The test samples include a crude extract of leaves and its solvent-soluble fractions of D. viscosa. The results showed that the crude extract and its fractions exhibited various significant biological activities, the fraction of chloroform demonstrated the highest free radical scavenging activity with IC50 values: 172.2 and 257.7 µg/mL for both DPPH and ABTS tests. Additionally, the chloroform fraction had the greatest cytotoxic activity against MDA-MB-231 (IC50 values: 24.6 ± 0.4 µg/mL). Moreover, the chloroform fraction exhibited the highest downregulation of the LPS-induced expression of TNF-α and IL-6. Quercetin and kaempferol were estimated concurrently in leaves crude extract using a validated technique on an HPTLC plate (10 cm2 × 10 cm2) with a combination of toluene–ethyl acetate–formic acid (5:4:0.2; v/v/v) as the mobile phase and a λ max of 254 nm. The amount of quercetin and kaempferol was found to be 31.8 and 15.01 mg/g of dried leaf extract, respectively. The presence of high levels of quercetin and kaempferol in D. viscosa leaves extract could explain its remarkable antioxidant, cytotoxic, and anti-inflammatory effects. The devolved HPTLC method can be used for routine analysis and standardization of D. viscosa crude plant material, extracts, and/or finished products using quercetin and kaempferol as appropriate markers.

Guaianolide is a type of naturally occurring sesquiterpene lactone compounds that have attracted attention due to their diverse biological properties. In this work, a guaiane-type sesquiterpene lactone identified as deoxycynaropicrin (compound 1) was isolated and reported for the first time from the leaves of Centaurothamnus maximus with two known flavonoid derivatives namely luteolin 6-O-methyl ether (compound 2) and quercetin 3-methyl ether 5-O-glucopyranoside (compound 3). The cytotoxic activity of all the three compounds was evaluated against the THP-1 human leukemia cell lines. Moreover, flow cytometry was employed to explore the cell cycle arrest and apoptosis induction for the active compound. We found that compound 1 (deoxycynaropicrin) exerted the highest cytotoxicity while compounds 2 and 3 showed no activity. Cell cycle analysis showed that compound 1 arrested the cells’ population at the G2/M phase. Furthermore, THP-1 cells treated with compound 1 exhibited a marked increase in the apoptotic cells compared to the control. Overall, this study showed that deoxycynaropicrin induces cytotoxicity against human leukemia cell lines and provided an important insight into its potential therapeutic effects against leukemia cells.

The nutrient contents of Raphanus sativus L. (white radish) leaves (RSLs) and roots are known to have promising vital effects. We comparatively investigated the leaves and roots of R. sativus grown in Saudi Arabia to estimate the total phenol and flavonoid contents using the standard colorimetric methods. The antioxidant activity of RSLs and R. sativus roots (RSRs) were measured by 2,2′-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assays. Both extracts’ cytotoxic activity was assessed by MTT assay against several human cancer cell lines (A549, HepG2, MDA-MB-231, and MCF-7). High-performance thin-layer chromatography was used to identify and quantify the biomarker compound rutin in both extracts. The total phenolic content in RSLs (125.3 mg of gallic acid equivalent [GAE]/g) was higher than that in roots (95.8 of GAE/g), whereas the flavonoid content (44.5 mg of quercetin equivalent [QE]/g) was almost double compared in RSR extract (24.4 of QE/g). Similarly, RSLs exhibited a higher antioxidative activity than RSRs in both DPPH (IC50 216.8 vs 359.7 µg/mL) and ABTS (IC50 326.7 vs 549 µg/mL) models. RSLs also demonstrated the highest antiproliferative efficiency against all cell lines, with IC50 values of 217–453 µg/mL. The reversed-phase-high-performance thin-layer chromatography results showed the presence of rutin (5.2 µg/mg) only in RSLs. Our study indicates RSLs as a promising source of bioactive compounds compared with roots.

Different phytochemicals from various plant species exhibit promising medicinal properties against cancer. Juniperus phoenicea is a plant species that has been found to present medicinal properties. Herein, crude extract and fractions of J. phoenicea were examined to determine its anticancer properties against several cancer cells. The active fraction was chosen to assess its activity on cell cycle progression and apoptosis induction by annexin and propidium iodide (PI) biomarkers. Further, phytochemical screening for possible contents of active fraction using gas chromatography–mass spectrometry (GC-MS) analysis was conducted. It was demonstrated that cell proliferation was suppressed, and the MCF-7 cell line was the most sensitive to J. phoenicea chloroform fraction (JPCF), with the IC50 values of 24.5 μg/mL. The anti-proliferation activity of JPCF in MCF-7 cells was linked to the aggregation of cells in the G1 phase, increases in early and late apoptosis as well as necrotic cell death. Contents analysis of JPCF using GC-MS analysis identified 3-methyl-5-(2′,6′,6′-trimethylcyclohex-1′-enyl)-1-penten-3-ol (16.5%), methyl 8-oxooctanoate (15.61%), cubenol (13.48%), and 7-oxabicyclo [2.2.1] heptane (12.14%) as major constituents. Our present study provides clear evidence that J. phoenicea can inhibit cell proliferation, trigger cell cycle arrest, and induce apoptosis in tested cancer cells.

The essential oil of Ducrosia ismaelis Asch. (Apiaceae) that grows wild in Saudi Arabia was investigated utilizing gas chromatography (GC), and gas chromatography-mass spectrometry. Fifty constituents were characterized, representing 96.1% of the total oil. The D. ismaelis essential oil (DIEO) was distinguished by a high composition of oxygenated monoterpenes (51.6%). Decanal (40.6%), α-pinene (15.1%) and dodecanal (13.7%) were the fundamental components. Additionally, DIEO was evaluated for its cytotoxic, antibacterial, antifungal and antioxidant activities. DIEO revealed a great cytotoxic effectiveness against the tested cancer cell lines with IC50 values between 66.2 and 137.3 μg/mL particularly against MCF-7 cancer cells. Furthermore, the induction of apoptosis against MCF-7 cells has been asserted using staining assay (annexin VFITC and/or propidium iodide (PI) dyes) and flow cytometry technique. The DIEO possessed a strong antimicrobial activity against Gram-positive bacterial and fungal strains with MIC-values between 0.07 and 0.31 mg/ml. The values of MBC or MFC were almost once higher than those of MIC’s. Moreover, the β-carotene-bleaching and DPPH free radical-scavenging tests showed that DIEO had a moderate activity (68%) as an antioxidant agent in decolouring of the β-carotene at 1.0 mg/mL and a moderate radical scavenging for DPPH (66 and 72%) at 0.50 and 1.0 mg/mL.

The coronavirus disease 2019 (COVID-19), caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus, is a highly contagious respiratory disease with widespread societal impact. The symptoms range from cough, fever, and pneumonia to complications affecting various organs, including the heart, kidneys, and nervous system. Despite various ongoing efforts, no effective drug has been developed to stop the spread of the virus. Although various types of medications used to treat bacterial and viral diseases have previously been employed to treat COVID-19 patients, their side effects have also been observed. The way SARS-CoV-2 infects the human body is very specific, as its spike protein plays an important role. The S subunit of virus spike protein cleaved by human proteases, such as furin protein, is an initial and important step for its internalization into a human host. Keeping this context, we attempted to inhibit the furin using phytochemicals that could produce minimal side effects. For this, we screened 408 natural phytochemicals from various plants having antiviral properties, against furin protein, and molecular docking and dynamics simulations were performed. Based on the binding score, the top three compounds (robustaflavone, withanolide, and amentoflavone) were selected for further validation. MM/GBSA energy calculations revealed that withanolide has the lowest binding energy of -57.2 kcal/mol followed by robustaflavone and amentoflavone with a binding energy of -45.2 kcal/mol and -39.68 kcal/mol, respectively. Additionally, ADME analysis showed druglike properties for these three lead compounds. Hence, these natural compounds robustaflavone, withanolide, and amentoflavone, may have therapeutic potential for the management of SARS-CoV-2 by targeting furin. [ABSTRACT FROM AUTHOR]