The polyherbal extract may be a complementary candidate in oral carcinoma management via antioxidant, anti-inflammatory, and antiproliferative effects via antioxidant, anti-inflammatory, and antiproliferative effects.
Abstract
Oral carcinoma is a major global health concern and a leading cause of carcinoma-related mortality. This study evaluated a methanolic polyherbal extract for its phytochemical composition and biological efficacy, along with mechanistic insights via in silico network pharmacology. GC-MS and UPLC profiling confirmed diverse bioactive compounds, particularly polyphenols, with UV peaks at 272 nm. The extract showed strong antioxidant activity (IC₅₀ = 108 ± 0.17 µg/mL) and significant antimicrobial effects (inhibition zones: 6.00–21.33 mm). Cytotoxicity assays revealed anticancer activity against OECM-1 oral carcinoma cells (IC₅₀ = 18.86 µg/mL). The polyphenolic fraction suppressed pro-inflammatory cytokines (IL-6, IL-10, TNF-α, IL-1β, TGF-β) with IC₅₀ values of 3.02–6.15 µg/mL. Network pharmacology and molecular docking indicated multi-target interactions of key phytochemicals in pathways relevant to oral carcinoma progression. These findings suggest the polyherbal extract may be a complementary candidate in oral carcinoma management via antioxidant, anti-inflammatory, and antiproliferative effects.
Background/Objectives: Propolis is a resinous natural product rich in phenolic acids and flavonoids, recognized in ethnopharmacology for its antioxidant and anti-inflammatory properties. This study aimed to identify the most bioactive Saudi propolis extract using a bioassay-guided strategy and investigate its chemical profile and mechanistic anti-inflammatory potential. Methods: Four propolis extracts (P1–P4) collected from different regions of Saudi Arabia were evaluated for their antioxidant (DPPH and ABTS) and anti-inflammatory (COX-1 and COX-2) activities. The most active extract was profiled using liquid chromatography–mass spectrometry (LC–MS), followed by molecular docking and molecular dynamics simulations. Results: Among all samples, P3 demonstrated the strongest antioxidant activity, with IC50 values of 25.84 ± 0.96 µg/mL (DPPH) and 32.30 ± 1.20 µg/mL (ABTS), comparable to ascorbic acid (27.45 ± 1.42 and 21.22 ± 0.79, respectively). P3 also exhibited potent and selective COX-2 inhibition with an IC50 of 6.19 ± 0.21 µg/mL (relative to celecoxib, IC50 0.681 ± 0.02 as positive control). LC–MS analysis identified 26 secondary metabolites. Computational studies ranked kaempferol as forming the most conformationally stable COX-2 complex among the ligands examined, including the reference inhibitor, on the basis of molecular dynamics descriptors of pose persistence and conformational confinement. Conclusions: Saudi propolis P3 is a potent source of bioactive compounds with strong antioxidant and selective COX-2 inhibitory activity. These findings highlight its anti-inflammatory potential and suggest its value as a natural lead for developing safer therapeutics targeting inflammation-related chronic diseases.
H. Aati, Jawaher H. Alqahtani, A. Al-Taweel et al.· Pharmaceutics· 0 citations
BACKGROUND
Oral squamous cell carcinoma (OSCC) accounts for over 90% of oral and pharyngeal malignancies and remains a leading cause of cancer-related mortality worldwide. The search for safer, plant-derived anticancer agents has highlighted the therapeutic potential of Cuminum cyminum (cumin), a medicinal spice rich in bioactive phytochemicals.
AIM
This study evaluated the phytochemical composition, antioxidant, , cytotoxic and apoptosis-inducing activities of the methanolic extract of Cuminum cyminum (MECC) against human oral carcinoma cell lines (KB, KB-31 and KB-CHR.8.5) and normal Vero cells. Additionally, the antibacterial potential of MECC was also evaluated.
MATERIALS AND METHODS
Phytochemical profiling was performed using HPLC. Cytotoxicity was assessed using MTT and Trypan Blue assays following treatment with MECC (500-1000 μg/mL). Antioxidant activity was evaluated using the DPPH assay, while antibacterial activity was determined by the disc diffusion method against Staphylococcus aureus and Escherichia coli. Apoptosis was assessed using acridine orange/ethidium bromide (AO/EtBr) and Hoechst 33342 staining.
RESULTS
HPLC analysis revealed multiple phytochemical constituents, with a major peak at 9.90 min. MECC exhibited dose-dependent cytotoxicity, with predicted IC₅₀ values of approximately 600 μg/mL (KB), 720 μg/mL (KB-31), 1318 μg/mL (KB-CHR.8.5) and 3250 μg/mL (Vero), yielding tumor selectivity indices of 5.42, 4.51 and 2.47, respectively. MECC also demonstrated significant antioxidant activity (DPPH IC₅₀ ≈ 354 μg/mL) and induced concentration-dependent apoptosis, characterized by chromatin condensation and nuclear fragmentation. No significant antibacterial activity was observed against either of the evaluated bacterial strain.
CONCLUSION
MECC exhibited selective cytotoxicity and apoptosis induction in oral cancer cells with minimal toxicity toward normal Vero cells, supporting its potential as a promising natural chemopreventive and an adjunct chemotherapeutic candidate for oral cancer. Further mechanistic and in vivo studies are warranted.
M. Khan, Anamika Gupta, A. Srivastava et al.· Tissue & Cell· 0 citations
Background: Inflammation is the immune system’s first reaction to an injury or infection. Corticosteroids, immunosuppressants, and Non-Steroidal Anti-Inflammatory Drugs (NSAID) often used to treat inflammatory illnesses have serious adverse effects, such as cardiovascular, renal, and gastrointestinal damage. To lessen the negative effects of currently available medications, there is an urgent need to create innovative anti-inflammatory regimens derived from natural sources. Aim: The current study evaluated Ziziphus mauritiana for its anti-inflammatory potential, as it contains numerous bioactive constituents like phenolics, flavonoids, and saponins, which can contribute to the development of safer and cost-effective plant-based therapeutics for the treatment of inflammation. Methods: Methanol, hexane and ethyl acetate leaf extracts were evaluated for anti-inflammatory potential using LPS-stimulated RAW 264.7 macrophages at concentrations of 3-100 µg/mL for 24 hours. Nitric oxide production was evaluated by the Griess assay. Liquid Chromatography- Mass Spectrometry (LC-MS) analysis for characterisation of various phytoconstituents was determined on a Waters Alliance e2695 High Performance Liquid Chromatography (HPLC) system using a gradient of water, acetonitrile, methanol, and acetic acid. Results: Qualitative estimation shows the presence of phenols, triterpenoids, flavonoids and cardiac glycosides in methanol and ethyl acetate extract. In-vitro cytotoxicity evaluation demonstrated that the methanol and ethyl acetate extracts maintained more than 50% cell viability at 3 to 20 µg/mL, whereas the hexane extract showed reduced viability, indicating toxicity. Nitric oxide production in RAW 264.7 macrophages was inhibited significantly by methanol and ethyl acetate extract, with maximum inhibition at a concentration of 20µg/mL. LC-MS profiling of ethyl acetate fraction has shown the presence of various bioactive compounds such as L-carnitine, Delphinidin, caffeine, ononin, saccharopine, sinapine, Kaempferol-7-O-neohesperidoside, fortunellin, diosmin, marein etc. Conclusion: Results indicate that leaves of Z. mauritiana are rich in bioactive compounds and exhibit significant anti-inflammatory potential, mediated by quenching nitric oxide production, highlighting their potential for the development of plant-derived anti-inflammatory medications that are safe to use and have minimal side effects.
Major Findings: Ziziphus mauritiana leaf extract has shown significant anti-inflammatory potential by the inhibition of nitric oxide production in the RAW 264.7 cell line. The anti-inflammatory potential of this plant may be attributed to the presence of various bioactive compounds such as L-carnitine, Delphinidin, caffeine, sinapine, Kaempferol-7-O-neohesperidoside, fortunellin, diosmin, marein, etc., analysed by LC-MS.
Insha Qadir, M. Masoodi· Journal of Natural Remedies· 0 citations
Background: Lung cancer is a major cause of cancer-related morbidity and mortality worldwide. Plant-derived therapeutics have attracted attention as safer, multitarget candidates for cancer management. Aim: This study evaluated the phytochemical profile, antioxidant activity, selective cytotoxicity, and docking-based anti-cancer potential of the aqueous leaf extract of Combretum indicum in A549 cells. Methods: Qualitative and quantitative phytochemical analyses were performed, followed by antioxidant assays [2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide, nitric oxide, lipid peroxidation, and Ferric Reducing Antioxidant Power (FRAP)], Gas Chromatography-Mass Spectrometry (GC-MS), 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assays in A549 and Vero cells, and molecular docking against Epidermal Growth Factor Receptor (EGFR), Anaplastic Lymphoma Kinase (ALK), C-Ros Oncogene 1 Receptor Tyrosine Kinase (ROS1), Phosphatidylinositol 3-Kinase (PI3K), and Mesenchymal-Epithelial Transition Receptor (MET). Results: The extract contained alkaloids, flavonoids, tannins, carbohydrates, proteins, and sterols. Flavonoids and tannins were present at high levels. C. indicum-Aqueous Leaf Extract (CI-ALE) showed concentration-dependent antioxidant activity and selective cytotoxicity against A549 cells, with an IC50 of 163.11 µg/mL. More than 80% of Vero cells remained viable at the highest tested concentration. GC-MS detected 38 compounds; phytol, n-hexadecanoic acid, octahydro-2(1H)-quinoline, and stigmasterol were prominent. Docking analysis showed that stigmasterol had the strongest binding affinity across major non-small cell lung cancer targets. Conclusion: The aqueous leaf extract of C. indicum demonstrated promising antioxidant and anti-cancer potential. Further mechanistic and in vivo evaluation is warranted.
Major Findings: CI-ALE showed selective cytotoxicity toward A549 cells, strong antioxidant activity, and multi-target docking interactions. Stigmasterol emerged as the most promising lead phytoconstituent against EGFR, ALK, ROS1, PI3K, and MET.
Ambika Sundararajan, C. Loganathan, J. Angayarkanni· Journal of Natural Remedies· 0 citations
The anti-inflammatory potential of Oroxylum indicum (OI), a traditional medicinal plant, was evaluated through in vitro, ex vivo, and molecular docking studies. The stem bark extract exhibited a significant, dose-dependent inhibition of protein denaturation in both egg albumin and bovine serum albumin assays at concentrations of 10, 30, and 100µg/mL. Molecular docking revealed strong binding affinities of key bioactive compounds, especially Oroxylin B (docking score -8.79), to the cyclooxygenase-2 (COX-2) enzyme, suggesting a mechanistic basis for anti-inflammatory effects. The extract exhibited no cytotoxicity on human lymphocytes across tested concentrations (20-200µg/mL) in the MTT assay, indicating safety. Ex vivo, OI extract significantly reduced COX-2 enzyme levels from 124.66 ± 0.16ng/mL in radiation controls to 107.33 ± 0.10ng/mL, comparable to diclofenac (106.36 ± 0.08ng/mL). Furthermore, IL-6 and TNF-alpha pro-inflammatory cytokine levels were substantially elevated by radiation but significantly decreased upon treatment with OI extract; IL-6 levels were reduced to 21.74 ± 0.95pg/mL compared to 27.45 ± 0.82pg/mL in radiation controls and TNF-alpha levels were similarly lowered, comparable to the diclofenac-treated group. These findings support the notion that the extract derived from the stem bark of Oroxylum indicum holds considerable strong possibility as a natural anti-inflammatory agent with modulatory effects on key inflammatory enzymes and cytokines, meriting further pharmacological and clinical evaluation.
Sushma Swaroopa, T. Gnanasekaran, Nanditha Bhat et al.· Prostaglandins & other lipid...· 0 citations
Background: Breast cancer ranks as a major cause of cancer-related mortality among women worldwide, with CCND1 (Cyclin D1) gene overexpression contributing significantly to disease progression. Bauhinia purpurea, a medicinal plant rich in bioactive compounds, has shown antioxidant, hepatoprotective, hypoglycemic, and antiproliferative properties, highlighting its potential as an anticancer agent. Methods: This study assessed the cytotoxic potential and modulation of CCND1 gene expression by B. purpurea leaf extracts obtained using 96% ethanol, ethyl acetate, and n-hexane, tested in vitro on MCF-7 breast cancer cells. Cytotoxicity was measured through the MTT assay following 48 h of treatment, while CCND1 expression levels were analyzed via qRT-PCR with GAPDH as the internal control. Results: Phytochemical analysis identified flavonoids, tannins, polyphenols, steroids/triterpenoids, and alkaloids within the extracts. After 48 h, the MTT assay indicated that the ethyl acetate fraction exhibited moderate cytotoxicity (IC50 = 88.5 μg/mL), the n-hexane fraction showed weak cytotoxicity (IC50 = 271.8 μg/mL), and the ethanol fraction displayed no cytotoxic effect (IC50 = 979.99 μg/mL). Gene expression analysis showed that all extracts significantly reduced CCND1 levels at IC25, IC50, and IC75, with effects comparable to doxorubicin (p < 0.05). Conclusion: Bauhinia purpurea leaf extracts showed solvent-dependent cytotoxicity and downregulated CCND1 gene expression comparable to doxorubicin, highlighting its potential as a phytopharmaceutical for breast cancer therapy via cell cycle inhibition.
Teja Koswara, Rina Masadah, B. Nelwan et al.· Natural Resources for Human...· 0 citations
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