Background: Hepatocellular carcinoma is a common type of tumour worldwide with a high mortality rate and with low response to current cytotoxic and chemotherapeutic drugs. The prediction of activity spectra for the substances (PASS) software, which predicted that more than 300 pharmacological effects, biological and biochemical mechanisms based on the structural formula of the substance was efficiently used in this study to reveal new multitalented actions for Vitex negundo (VN) constituents.
Methods: Experimental studies based on antioxidant and antiproliferative assays verified the predictions obtained by the PASS-predicted design strategy. Antioxidant activity of VN extract was studied using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and Ferric reducing or antioxidant power (FRAP) assays. The antiproliferative activity of VN extract against WRL68 and HepG2 was investigated based on methylthiazol tetrazolium (MTT) spectrophotometric assay.
Results: VN extract showed 79.43% inhibition of DPPH stable radical with IC50 13.31 ± 0.18 μg/ml. This inhibition was too closed to butylated hydroxyl toluene (BHT) 82.53% (IC5013.8 ± 0.14) and gallic acid 89.51% (IC50 3.1 ± 0.08). VN extract exhibited the strongest free radical scavenging power compared with two commercial antioxidants, BHT and ascorbic acid. VN increased the activities of antioxidant enzymes in normal embryonic liver cells (WRL68) including, superoxide dismutase (SOD) and glutathione peroxidase (GPX) compared with to H2O2 group. The ethanolic extract of VN showed cytotoxicity to HepG2 cells in a dose and time-dependent manner with IC50 66.46 μg/ml, 57.36 μg/ml and 65.12 μg/ml at 24, 48, and 72-hours incubation respectively, with no sensitivity in WRL68 cells. This was associated with significant elevation in lactate dehydrogenase (LDH) release in HepG2 cells. In addition, the activation of caspase-3 enzyme suggesting that the observed cytotoxicity was mediated via an intrinsic apoptosis pathway.
Conclusions: PASS-predicted plant activity could efficiently help in selecting a promising pharmaceutical leads with high accuracy and required antioxidant and antiproliferative properties. This is the first report on PASS-predicted VN activity.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4235047 | PMC |
| http://dx.doi.org/10.1186/1472-6882-13-343 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Chemical Profiling, Antioxidant, and Antiproliferative Activities of Algerian Cistus creticus L. Leaf Extracts: Evidence from In vitro and In Silico Studies.
Curr Top Med Chem
January 2025
Medicinal Chemistry Department, Theodor Bilharz Research Institute Kornaish El Nile, Warrak El-Hadar, Imbaba (P.O. 30), Giza 12411, Egypt.
Background: Research into oxidative stress, cancer, and natural products revealed promising avenues for therapeutic intervention. Natural products are considered potent pharmaceuticals in combating oxidative stress and its relationship with cancer.
Methods: This study was carried out to evaluate the chemical profile and antioxidant activities using DPPH, ABTS, Phenanthroline, Cupric, Phosphomolybdenum, FRAP, Hydroxyl, Iron chelation in vitro assays, and anticancer properties by MTT method of Cistus creticus extracts.
Multi-target regulatory effects of rhaponticin in a rat model of hepatic fibrosis revealed by non-targeted metabolomics.
Front Pharmacol
January 2025
School of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang, China.
Introduction: Hepatic fibrosis (HF), a progressive chronic liver disease, is a serious threat to global public health. The lack of preventive and therapeutic strategies has created an urgent need for effective anti-fibrosis agents. There is growing evidence that natural products might provide safe and effective interventions for HF.
View Article and Find Full Text PDFRole of Epigallocatechin Gallate in Selected Malignant Neoplasms in Women.
Nutrients
January 2025
Department of Medical Chemistry, Faculty of Chemistry, Adam Mickiewicz University, 61-614 Poznań, Poland.
Tea is a significant source of flavonoids in the diet. Due to different production processes, the amount of bioactive compounds in unfermented (green) and (semi-)fermented tea differs. Importantly, green tea has a similar composition of phenolic compounds to fresh, unprocessed tea leaves.
View Article and Find Full Text PDFPlant-Based Functional Foods from Borneo.
Nutrients
January 2025
School of Pharmacy and Medical Sciences, Griffith University, Gold Coast, QLD 4222, Australia.
Borneo, the third-largest island in the world, is shared between Malaysia (Sabah and Sarawak), Indonesia (Kalimantan) and Brunei. As a biodiversity hotspot, it is home to about 15,000 flowering plants and 3000 tree species, of which many are endemic to the region. Locally derived plant-based foods are gaining popularity due to their lower environmental impact, contribution to food sustainability and health benefits.
View Article and Find Full Text PDFDistribution, Phytochemical Insights, and Cytotoxic Potential of the Genus: A Comprehensive Review of , , and .
Pharmaceuticals (Basel)
January 2025
Department of Botany and Microbiology, Faculty of Science, Alexandria University, Alexandria 21511, Egypt.
This review evaluates the cytotoxic potential of the genus, with a focus on , , and . These species, known for their diverse phytochemical compositions, exhibit notable cytotoxic effects that suggest their utility in natural cancer treatments. Compounds such as quercetin, kaempferol, and sesbagrandiforian A and B have been highlighted for their strong antioxidant and antiproliferative effects, further emphasizing their therapeutic potential.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!