- Research Article
2
- 10.1080/22311866.2025.2465679
- Jan 2, 2025
- Journal of Biologically Active Products from Nature
- Nada N Mustafa + 3 more
The current study aims to study the therapeutic effects of ascorbic acid on Caco-2 cancer cell inhibitory mechanisms. The cytotoxicity of ascorbic acid on Caco-2 cells was determined by MTT and LDH assays. Also, apoptosis induction in ascorbic acid-treated Caco-2 cells was tested through annexin and DNA fragmentation techniques. Cell cycle arrest, ROS generation, RT-PCR, and western plot analyses were conducted to identify the apoptosis mechanisms of Caco-2 cells after treatment with ascorbic acid. According to the data, ascorbic acid demonstrated selective efficacy in inhibiting Caco-2 cell growth, with the most effective IC50 value (53.6 μg/ml) attained after 48 hours of incubation. Also, compared to the untreated control cells, the ascorbic acid-treated Caco-2 cells displayed a much higher rate of LDH leakage. Additionally, the ascorbic acid IC50 value found a considerable rise in early and late apoptotic Caco-2 cells with an intensive comet nucleus as a marker of DNA fragmentation. Moreover, flow cytometry analysis of the apoptosis process in Caco-2 treated cells revealed cell cycle arrest in the S phase with an increase in apoptotic cells in the sub-G1 phase. Also, real-time PCR and Western blot analysis showed that ascorbic acid significantly changed protein expression levels linked with cell cycle arrest in the S phase and the induction of apoptosis. Consequently, our data indicated that ascorbic acid would be a promising therapy candidate for colon cancer in people.
- Research Article
- 10.1080/22311866.2025.2465677
- Jan 2, 2025
- Journal of Biologically Active Products from Nature
- Ochuko L Erukainure + 1 more
Oxidative stress contributes the pathogenesis and progression of renal toxicity. This study investigated the protective effect of kolaviron, the principal phytochemical of Garcinia kola seed on major dysmetabolic activities, vis-à-vis oxidative imbalance, purinergic dysfunctions, and glucose dysmetabolism in oxidative renal toxicity using Vero cell lines. Fixed Vero cells were treated with kolaviron extracted from G. kola seeds, then subjected to an MTT assay that revealed a non-cytotoxic effect of kolaviron on Vero cells. Fixed Vero cells were further pretreated for 25 minutes before incubating with FeSO4 for 30 minutes to induce oxidative injury. Induction of oxidative injury significantly depleted glutathione level and catalase activity while concomitantly elevating malondialdehyde level, ATPase, ENTPDase, glycogen phosphorylase, glucose 6-phosphatase, and fructose-1,6-biphosphatase activities. These activities and levels were significantly reversed in kolaviron pretreated cells. Molecular docking analysis revealed strong molecular interactions of kolaviron with ATPase, ENTPDase. fructose-1,6-biphosphatase and glycogen phosphorylase. The results indicate that kolaviron is safe and non-toxic to cells and protected against iron-induced oxidative renal injury as depicted by its ability to mitigate oxidative imbalance, modulate purinergic activities and glucose metabolism in Vero cells.
- Research Article
2
- 10.1080/22311866.2025.2463024
- Jan 2, 2025
- Journal of Biologically Active Products from Nature
- Hieu Tran Trung + 9 more
The present study described the characterization of chemical composition of essential oil of Blumea eberhardtii aerial parts and its cytotoxic activities and molecular docking. The gas chromatography coupled with mass spectrum (GC-MS) analysis on the essential oil indicated that thymohydroquinone dimethyl ether (34.15 %), β-caryophyllene (19.95 %), and γ-muurolene (8.65 %) were determined to be the major components. The essential oil was also shown to exhibit potential cytotoxic effects against several cancer cell lines, including MCF-7, HepG2 and SK-LU-1 with the IC50 values of 8.32±0.21, 6.42±0.34 and 10.31±0.46 μg/mL, respectively in in vitro cellular assays. The molecular docking was also performed on EGFR and HER2, which are the two receptors belonging to the ErbB family, for better understanding of the anti-cancer mechanisms. The major compounds, β-caryophyllene, γ-muurolene and thymohydroquinone dimethyl ether, were estimated to possess strong binding affinities towards EGFR and HER2 with binding energies ranging from -6.021 to -6.102 kcal/mol for EGFR and from -5.511 to -6.439 kcal/ mol for HER2. The present study demonstrated the potential cytotoxicity of chemical scaffolds from B. eberhardtii against cancer cells, which could be beneficial for developing anti-cancer agents in the future.
- Research Article
- 10.1080/22311866.2025.2468494
- Jan 2, 2025
- Journal of Biologically Active Products from Nature
- Gertrude Eléonore Djiobie Tchienou + 4 more
Roots of Securidaca longipedunculata have been used for their medicinal properties. These roots are rich in bioactive compounds with many pharmacological properties, such as anti-inflammatory and anti-oxidant effects. This research investigated the effects of microwave-assisted extraction parameters on the anti-oxidant activity of extract from S. longipedunculata roots. The influences of irradiation time, microwave power, and solvent-to-material ratio on the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity, and the ferrous ion chelating activity, as well as total xanthones, were used to optimize extraction parameters and to investigate their interactions through Response Surface Method (RSM). The optimal combined conditions for extracting maximum xanthones (2888 μgEDMX/gP) and anti-oxidant activity (DPPH 82.24%, chelating Iron 88.28%) were irradiation time 78.34 s, microwave power 529 W, solid to liquid ratio 1.01 g/20 mL. The extract obtained at optimal conditions has a very high anti-oxidant activity compared to an extract obtained with conventional method extraction. Furthermore, Higher Performance Liquid Chromatography (HPLC) analysis of optimal conditions with MAE showed remarkable differences in peak than in traditional extraction. Scanning electron micrograph (SEM) of roots of S. longipedunculata showed morphological changes and cellular damage compared to the initial powder. The results indicate the total uzes of the extract from S. longipedunculata roots. This study design guides future efficient use of this method for other valuable species or bioactive compounds.
- Research Article
- 10.1080/22311866.2025.2463020
- Jan 2, 2025
- Journal of Biologically Active Products from Nature
- Reda El Boukhari + 3 more
Pulegone, a natural biomolecule found in the essential oils of many Lamiaceae family plants, is notable for its minty aroma and therapeutic potential, despite its recognized toxicity. This study examines trends in pulegone applications by analyzing patents. Analyzing patent trends in this space can shed light on emerging opportunities and innovation hotspots. Results show the United States as the leading jurisdiction with 46.15% of patents, likely due to its large pharmaceutical and consumer items industries, as well as a sound patent system. Three major innovation areas are highlighted: daily-use cleaning, health, and hygiene products leveraging pulegone’s aroma (127 patents); plant protection products utilizing their pesticidal properties (62 patents); and pharmacological and recreational uses with cannabinoids (43 patents). Pulegone’s versatility spans perfumes, body care, odor neutralization, and natural pest repellents. The review of 9 recent patents as key trending areas reveals that pulegone has diverse applications ranging from flavors and fragrances to potential medicinal uses. Emerging trends are focused on the combination of pulegone with other natural compounds for synergistic effects, microen-capsulation and controlled-release formulations, biosynthetic production routes using engineered microorganisms, and exploration of pulegone’s potential in agricultural applications like biopesticides. The last parts of this study present a critical analysis of key patents related to the pulegone biomolecule, focusing on their impact, strategies to address major challenges, and identifying limitations and gaps. A detailed examination of patents highlights their influence on advancing pulegone’s applications, from medicinal formulations to industrial uses. However, several challenges persist, including toxicity and safety concerns, regulatory barriers and issues related to stability and scalability in production. Furthermore, future directions for innovation include the development of toxicity mitigation strategies, alignment with regulatory frameworks and bioprospecting ethics and exploring sustainable production methods.
- Research Article
- 10.1080/22311866.2024.2444337
- Nov 1, 2024
- Journal of Biologically Active Products from Nature
- Orawan Theanphong + 2 more
The rhizomes of plants in the genus Alpinia (Zingiberaceae) have been used as food, spices, and traditional medicine in Thailand. The crude ethanolic extracts from the fresh rhizomes of selected Alpinia species, including A. galanga var. galanga, A. galanga var. pyramidata, A. oxymitra, and A. siamensis, were proposed to be explored for their active principles and in vitro antioxidant and antidiabetic performance. The fresh rhizomes were extracted with 95% ethanol using a Soxhlet apparatus, and crude extracts were subsequently analyzed for amounts of flavonoids using quercetin and kaempferol as chemical markers by high-performance liquid chromatography. All flavonoid-containing extracts were evaluated for their antioxidant and antidiabetic effects using free radical scavenging and α-glucosidase inhibitory tests. The results demonstrated that the examined extracts included active flavonoid markers, predominantly quercetin, which ranged from 11.05% to 13.79% w/w and was approximately 10 times more prevalent than kaempferol. Extracts that consisted of these active flavonoids exhibited strong antioxidant and α-glucosidase inhibitory activities. Pearson’s correlation study was used to determine the association between flavonoid quantity and possessed activities. The findings indicated a substantial correlation between quercetin levels and free radical scavenging activity. This work implies that raw ethanolic extracts from the fresh rhizomes of these rare Alpinia plants have the potential to be developed into functional nourishment and remedies that could benefit diabetics in alternative ways.
- Research Article
- 10.1080/22311866.2024.2437018
- Nov 1, 2024
- Journal of Biologically Active Products from Nature
- Omilla Ragavan + 6 more
Background: The red cultivar of Alternanthera sessilis (ASR), a medicinal weed traditionally consumed by Asians, reduces risk of cardiovascular disease with established athero-protective effects from previous studies. However, the underlying mechanisms of ASR against atherosclerosis remains unknown. Objective: This investigation aims to discover the potential mechanisms of ASR in treating atherosclerosis using network pharmacology and molecular docking. Methods: Phytochemicals of ASR were collected via ultra-high performance liquid chromatography analysis and literature search. Screening of their pharmacokinetic properties aligned with Traditional Chinese Medicine System Pharmacology database’s criteria of oral bioavailability ≥30% and drug-likeness ≥0.18. Subsequently, a network pharmacology approach was developed, encompassing the collection of ASR and atherosclerosis possible targets, establishment of protein-protein interaction (PPI) network, construction of compound-target network, analysis of intersecting gene set and identification of hub genes. Molecular docking validated binding affinities between bioactive compounds and the hub genes. Results: Among 179 compounds identified from ASR, only 4 (Dehydrodieugenol, Luteolin, Quercetin and Xanthosine) emerged as key bioactive compounds meeting the criteria. PPI network between ASR and atherosclerosis targets revealed 192 intersecting genes, from which 4 hub genes were discovered: AKT1, HSP90AA1, SRC and ESR1. Kyoto Encyclopedia of Genes and Genomes pathway analysis revealed lipid and atherosclerosis were among the significantly enriched pathways in the top 10 list. Molecular docking results demonstrated Dehydrodieugenol-ESR1 complex exhibiting the highest binding affinity at −8.56 kcal/mol. Conclusion: Although, this study uncovers probable molecular pathways for atherosclerosis therapy using ASR, experimental validation in vitro and in vivo is necessary to confirm these computational findings.
- Research Article
- 10.1080/22311866.2024.2439927
- Nov 1, 2024
- Journal of Biologically Active Products from Nature
- Napaporn Lakkana + 4 more
This study explored the antimicrobial activity and potential synergistic effects of three essential oils—bergamot, lime, and lemongrass—to determine their optimal ratios. Antimicrobial activity was tested against three common pathogens: Staphylococcus aureus, Escherichia coli, and Candida albicans. A simplex lattice design was used to evaluate potential synergic effects among the three essential oils. Most individual and combined essential oil formulations exhibit antimicrobial activity, as indicated by the clear zones observed with all tested pathogens. When tested individually, lemongrass oil demonstrated the greatest inhibition efficacy against S. aureus, E. coli, and C. albicans, while bergamot and lime oils showed no inhibition against S. aureus and E. coli. Using the simplex lattice design, the synergistic effects of different essential oil formulations were assessed by calculating the combination index (CI) based on their clear zones. Almost all essential oil formulations had a CI of <1. Notably, formula 4, composed of bergamot and lime essential oils at a ratio of 0.5:0.5, had the lowest CI against S. aureus and E. coli, indicating the best synergistic potential. In conclusion, this study effectively identified optimal ratios of essential oils using the simplex lattice design, highlighting their synergistic potential and enhanced antimicrobial activity against common pathogens.
- Research Article
- 10.1080/22311866.2024.2446936
- Nov 1, 2024
- Journal of Biologically Active Products from Nature
- Khirabdhi Tanaya Dash + 4 more
Piper nigrum (Black pepper), popularly called the “King of Spices” is one of nature’s most ancient and miraculous traditional plants to treat several deadly maladies. The essential oil of P. nigrum is highly considered to have illustrious therapeutic significance in domestic and industrial applications. To validate the traditional claim of its essential oil’s efficacy, the proposed study was designed to analyze the volatile profile and assess the antimicrobial and antiproliferative effect of P. nigrum fruit essential oil. This is the first study on the analysis of essential oil of P. nigrum collected from Eastern India. The Gas chromatography-mass spectrometry analysis of P. nigrum essential oil revealed β-caryophyllene (25.6%), limonene (15.7%), sabinene (11.6%), β-pinene (11.1%) and δ-carene (8.6%) as its major constituents. In antibacterial assays, P. nigrum essential exhibited significant activity against multiple microbial pathogens like Salmonella enterica serovar Typhi (ZOI-19±0.4 mm; MIC-0.781 μg/ml), Escherichia coli (ZOI-18±0.4 mm; MIC-1.562 μg/ml) and Staphylococcus saprophyticus (ZOI-18±0.4 mm; MIC-1.562μg/ml). MTT assay demonstrated selective cytotoxicity against cancerous cells such as HepG-2 (IC50-71.2±1.3 μg/ml); PC-3 (IC50-68.38±1.2 μg/ml) as compared to noncancerous 3T3L-1 cells (IC50- 235.77±1.6 μg/ml).To the best of our knowledge, this is the first-ever study from India on the cytotoxic potential of P. nigrum essential oil against the above two robust cancerous cell lines. The present findings revealed that P. nigrum essential oil exhibited remarkable therapeutic potential, which could enhance its medicinal worth and commercial significance in current scenario and in future perspectives for designing antimicrobial and anticancer drugs.
- Research Article
- 10.1080/22311866.2024.2442621
- Nov 1, 2024
- Journal of Biologically Active Products from Nature
- Nadia Aliouche + 2 more
Due to their safety and health-promoting benefits, exopolysaccharides (EPS) secreted by lactic acid bacteria (LAB) have recently attracted considerable interest. Therefore, this study aims to investigate the in vitro antioxidant, anti-inflammatory and anti-diabetic activities, as well as the human compatibility of crude EPS produced by three novel strains of Lactiplantibacillus plantarum, specifically E1K2R2, E2AT5 and E1K1R2 isolated from infant faeces. The antioxidant activity was measured using various radical scavenging assays. The anti-inflammatory activity was evaluated through protein denaturation inhibition, antiproteinase and erythrocyte membrane stabilization assays. The anti-diabetic potential was assessed by measuring the α-amylase inhibitory activity and the biocompatibility of the produced EPS was investigated using the hemolysis assay. The results demonstrated that all crude EPS exhibited significant, concentration-dependent capacity (0.1 to 2 mg/mL) for antioxidant, anti-inflammatory and anti-diabetic activities. Among the strains, EPS from L. plantarum E1K2R2 followed by E2AT5, showed the highest efficacy against oxidative stress, inflammation and diabetes, as indicated by their lower IC50 values (0.78 to 7.65 mg/mL and 0.72 to 9.84 mg/mL, respectively) compared to EPS from L. plantarum strain E1K1R2 (0.79 to 11.59 mg/mL). This suggests a promising potential for health improvement. Additionally, all EPS were found to be biocompatible, displaying minimal hemolytic activity (<4%) at high concentrations. These findings provide strong evidence for the health and safety benefits of EPS in human applications.