Phytochemical Characterization and Mechanistic Insights into the Cytotoxic Effects of Bougainvillea glabra Bract Extract in Caco-2 Colorectal Adenocarcinoma Cells
Aug 2026· Plant Foods for Human Nutrition· Vol 81· 0 citations· 35 references
Medicine
TL;DR
Overall, B. glabra extract exhibited antioxidant and cytotoxic activities, supporting its potential as a source of bioactive compounds for colorectal cancer research.
Abstract
Bougainvillea glabra Choisy (Nyctaginaceae) is a traditional medicinal plant and a source of betalains and phenolic compounds with potential antioxidant and cytotoxic properties that still remains underexplored. This study characterized a B. glabra extract (BGE) and evaluated its antioxidant capacity, cytotoxic effects, and modulation of intracellular ROS levels in Caco-2 cells. UPLC-MS identified 21 phenolic compounds, including rutin and quercetin, and two major betacyanins. BGE exhibited ABTS radical scavenging activity (156–188 µM TE), reduced intracellular ROS levels under basal and LPS-stimulated conditions, decreased Caco-2 cell viability, and enhanced the cytotoxic effect of cisplatin. These effects were associated with apoptosis- and autophagy-related markers, including p53 and Bcl-2 expression, and differential regulation of genes involved in caspase activation and NF-kB signaling. Overall, BGE exhibited antioxidant and cytotoxic activities, supporting its potential as a source of bioactive compounds for colorectal cancer research.
Echinophora tenuifolia subsp. sibthorpiana is an aromatic and traditionally used plant whose phytochemical diversity and pharmacological potential remain incompletely characterized. This study aimed to integrate comprehensive chemical profiling with antioxidant, antimicrobial, and antiproliferative evaluations of an acidified methanolic extract prepared from its aerial parts. Phenolic constituents, volatile compounds, and fatty acids were characterized using LC–MS/MS, GC–MS, and GC–FID, respectively. Antioxidant capacity was assessed using DPPH and ABTS assays, antimicrobial effects were evaluated by disc diffusion and broth microdilution methods, and antiproliferative activity was investigated in six human cancer cell lines and non-cancerous BEAS-2B cells. Apoptosis induction and cell-cycle alterations were further examined by flow cytometry. The extract contained a high total phenolic content of 181.78 ± 5.03 mg GAE/g and exhibited substantial DPPH and ABTS radical scavenging activities of 333.65 ± 2.94 and 262.18 ± 6.80 mg TE/g, respectively. LC–MS/MS analysis identified rutin hydrate, quinic acid, chlorogenic acid, narcissin, and vicenin-2 as the predominant non-volatile constituents. The essential oil was dominated by methyl eugenol (51.10%) and Δ-3-carene (32.23%), whereas lauric acid (29.71%) was the major fatty acid. The extract also exhibited measurable antimicrobial activity and concentration-dependent cytotoxicity, with the greatest sensitivity observed in MCF-7 breast cancer cells (IC50 = 32.96 ± 4.80 μg/mL), followed by A549 and MDA-MB-231 cells. However, the relatively close IC50 values observed in cancer and non-cancerous BEAS-2B cells indicated limited cancer-cell selectivity under the tested conditions. Flow-cytometric analyses demonstrated marked apoptosis induction in MCF-7 cells, reaching 57.93 ± 1.80%, together with a cell-line-dependent accumulation in the G2/M phase. Collectively, these findings indicate that E. tenuifolia subsp. sibthorpiana is a chemically diverse source of plant-derived bioactive compounds with notable radical scavenging and measurable antimicrobial and cytotoxic effects. Further bioactivity-guided fractionation and mechanistic studies are required to identify the active constituents and clarify their pharmacological relevance and selectivity.
Y. Uğur, Turgay Kolaç, Muhammed Dündar et al.· International Journal of Mol...· 0 citations
Epilobium parviflorum Schreb. is a medicinal plant used traditionally against inflammatory disorders whose cytotoxic potential is still incompletely revealed. The current study investigates the phytochemical composition and in vitro cytotoxic activity of four hydroalcoholic extracts prepared from the aerial parts of E. parviflorum by using maceration and Soxhlet extraction. The extracts were characterized in terms of total phenolic, flavonoid and tannins composition and LC-MS was used to identify its individual polyphenols. Their biological effects were assessed against four cancer cell lines (A375 melanoma, HT-29 colorectal adenocarcinoma, PANC-1 pancreatic carcinoma and SK-OV-3 ovarian adenocarcinoma cells), while using HaCaT keratinocytes as healthy cells in order to assess selectivity. Cell viability, cytoskeletal and nuclear morphology, mitochondrial respiration and network pharmacology were further investigated. A complex phenolic profile was revealed, with hyperoside being identified as the main component in all extracts while the extraction parameters strongly influenced the recovery of various phenolic compounds. All extracts reduced cancer cell viability in a dose-dependent manner after 24 h exposure, with the most pronounced effects observed at 720 and 1000 μg/mL, while HaCaT cells were left relatively unaffected. The morphological assessment indicated nuclear condensation, fragmentation and cytoskeletal disruption following the application of extracts. Moreover, high-resolution respirometry showed reduced oxidative phosphorylation and electron transfer system capacity thus indicating that early mitochondrial dysfunction may contribute to the cytotoxic effects. Network pharmacology revealed that ERBB2, CTNNB1, HSP90AA1 and HDAC6 might act as molecular targets in melanoma. Thus, these findings support the hypothesis that E. parviflorum hydroalcoholic extracts, particularly the 40% ethanol Soxhlet extract, may serve as important sources of bioactive phytocompounds with antiproliferative and apoptotic properties.
Christian Goldiș, Roxana Racoviceanu, Mihaela Jorgovan et al.· Scientia Pharmaceutica· 0 citations
Species belonging to the genus Seseli have long been known to be used as herbal remedies in traditional medicine for various purposes such as colds, inflammation, pain, and gastrointestinal disorders. Therefore, in this study, the flower parts of Seseli transcaucasicum (Schischk.) Pimenov & Sdobnina were extracted using methanol and acetone to investigate their phytochemical composition and antioxidant, antimicrobial, and cytotoxic activities. For this purpose, total phenolic content (TPC), DPPH free radical scavenging activity (RSA), phenolic component (PCs) profile, volatile component composition, antimicrobial effect, and cytotoxic potential on the HT29 human colorectal adenocarcinoma cell line were evaluated. When the results were examined, HPLC analysis of phenolic components revealed that both extracts contained particularly high levels of rosmarinic acid, catechin, and quercetin. Among these, rosmarinic acid was detected in the highest amount, with 15.195 mg/g in the methanol extract and 14.929 mg/g in the acetone extract. The volatile components of this plant were determined by GC-MS, and a total of 29 volatile compounds were identified. Among these, β-pinene (220.792 mg/kg), Δ3-carotene (81.898 mg/kg), α-sedrene (63.331 mg/kg), elixen (44.535 mg/kg), sabinene (40.822 mg/kg), and D-limonene (38.422 mg/kg) were identified as the most dominant compounds. It was observed that the methanol extract had a higher total phenolic content (77.389 ± 1.389 mg gallic acid equivalent/g extract) and higher free radical scavenging activity (40.933 ± 0.067 mg trolox equivalent/g extract) compared to the acetone extract. Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Candida albicans strains were used to determine the antimicrobial activities of plant extracts, and moderate inhibitory effects were observed against these microorganisms. The highest antimicrobial activity was determined by the 16 mm inhibition zone created against S. aureus by the methanol extract at a concentration of 100 mg/mL. The cytotoxic activity of the plant was determined by measuring its dose-dependent antiproliferative effect on HT29 cells. When the difference between solvents was examined, it was observed that the acetone extract at a concentration of 500 µg/mL reduced cell viability by 18.03%, while the methanol extract at the same concentration reduced viability by 30.56%. According to the results, S. transcaucasicum is rich in phenolic and terpenic compounds and exhibits antioxidant, antimicrobial, and cytotoxic effects. Therefore, this plant species is considered a promising resource for the development of naturally occurring biologically active compounds.
Mehmet Şirin Karan, Mustafa Yunus Emre· Plants· 0 citations
Cinnamaldehyde (CA), a bioactive compound derived from
Cinnamomum
species, has gained attention for its potential anticancer properties. Preclinical evidence suggests that CA exerts antitumor effects through multiple mechanisms, including the induction of apoptosis, modulation of redox homeostasis, inhibition of cell proliferation, and disruption of key signaling pathways such as PI3K/Akt/mTOR and MAPK/ERK. Its selective cytotoxicity toward cancer cells, with minimal effects on normal cells, further supports its therapeutic relevance. This review evaluated current evidence regarding the anticancer activity of CA, with a focus on its molecular mechanisms, structure–activity relationships, semisynthetic derivatives, and potential for combinatorial therapy. Relevant experimental and preclinical studies were examined to assess CA's efficacy in various cancer types, its pharmacokinetic limitations, and strategies for improved delivery, including nanoparticle and liposomal formulations. Findings indicate that CA affects several hallmarks of cancer, including apoptosis resistance, sustained proliferation, and metastasis. Enhanced anticancer activity has been reported when CA is used in combination with standard chemotherapeutic agents or other natural compounds. Nanotechnological approaches have demonstrated potential in overcoming CA's low bioavailability and rapid metabolism. CA shows promise as a multitargeted, low‐toxicity compound suitable for adjuvant cancer therapy. Further investigation, particularly through clinical trials and advanced delivery systems, is required to confirm its efficacy and support clinical application.
G. Moriasi, S. Kamau, G. Seitimova et al.· Food Frontiers· 0 citations
Black goji berry (Lycium ruthenicum Murr.) has been recognized for its immune-regulating and anti-cancer potentials, but its key active components and underlying mechanisms remain unclear. Here, we applied LC–MS/MS to characterize the metabolite profile of L. ruthenicum and performed in vitro assays to evaluate its anti-inflammatory and anti-cancer activities. A total of 149 metabolites were identified, with organic acids, carbohydrates, and amino acid derivatives as the dominant components. Isorhamnetin was identified as a representative flavonoid. In LPS-stimulated Calu3 cells, isorhamnetin reduced the secretion and mRNA expression of pro-inflammatory cytokines (IL-6, TNF-alpha, IL-1beta). In cancer cells, isorhamnetin induces ROS accumulation, DNA damage, mitochondrial dysfunction, and caspase-3-dependent apoptosis, with modulation of the AKT signaling pathway. These findings suggest that isorhamnetin may contribute to the anti-inflammatory and anti-cancer effects of L. ruthenicum observed in vitro, providing preliminary experimental evidence for its potential as a functional food ingredient. However, this study is limited by the use of a single cell line (Calu3) and the absence of in vivo validation and pharmacokinetic evaluation; further studies are needed to confirm these observations.
Lei Jiang, Ji-Deng Ma, Zhi-Yuan Li et al.· Frontiers in Nutrition· 0 citations
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