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Comparative Assessment of the Antioxidant and Anticancer Activities of Plicosepalus acacia and Plicosepalus curviflorus: Metabolomic Profiling and In Silico Studies.

ABSTRACT: This study presents a comparison between two mistletoe plants-P. acacia and P. curviflorus-regarding their total phenolic contents and antioxidant and anticancer activities. P. curviflorus exhibited a higher total phenolics content (340.62 ± 19.46 mg GAE/g extract), and demonstrated higher DPPH free radical scavenging activity (IC₅₀ = 48.28 ± 3.41µg/mL), stronger reducing power (1.43 ± 0.54 mMol Fe⁺²/g) for ferric ions, and a greater total antioxidant capacity (41.89 ± 3.15 mg GAE/g) compared to P. acacia. The cytotoxic effects of P. acacia and P. curviflorus methanol extracts were examined on lung (A549), prostate (PC-3), ovarian (A2780) and breast (MDA-MB-231) cancer cells. The highest anticancer potential for the two extracts was observed on PC-3 prostate cancer cells, where P. curviflorus exhibited more pronounced antiproliferative activity (IC₅₀ = 25.83 μg/mL) than P. acacia (IC₅₀ = 34.12 μg/mL). In addition, both of the tested extracts arrested the cell cycle at the Pre-G1 and G1 phases, and induced apoptosis. However, P. curviflorus extract possessed the highest apoptotic effect, mediated by the upregulation of p53, Bax, and caspase-3, 8 and 9, and the downregulation of Bcl-2 expression. In the pursuit to link the chemical diversity of P. curviflorus with the exhibited bioactivities, its metabolomic profiling was achieved by the LC-ESI-TOF-MS/MS technique. This permitted the tentative identification of several phenolics-chiefly flavonoid derivatives, beside some triterpenes and sterols-in the P. curviflorus extract. Furthermore, all of the metabolites in P. curviflorus and P. acacia were inspected for their binding modes towards both CDK-2 and EGFR proteins using molecular docking studies in an attempt to understand the superiority of P. curviflorus over P. acacia regarding their antiproliferative effect on PC-3 cancer cells. Docking studies supported our experimental results; with all of this taken together, P. curviflorus could be regarded as a potential prospect for the development of chemotherapeutics for prostate cancer.

SUBMITTER: Eltamany EE

PROVIDER: S-EPMC9311546 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:Luffa echinata Roxb. is one of the neglected medicinal plants. It is an important source of bioactive metabolites and used in several Ayurvedic formulations. In the present analysis, mature leaves and fruits were extracted with acetone, ethanol, acetonitrile, methanol and water. Phytochemicals like total phenolic (TPC), flavonoid (TFC), tannin (TTC), alkaloid (TAC) and terpenoid (TTEC) content were analysed. Further, antioxidant (AOX) activities like 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, 2,2'-azino-bis-(3-ethyl) benzothiazoline-6-sulfonic acid (ABTS) radical scavenging, metal chelating activity (MC), ferric reducing antioxidant power (FRAP) and phosphomolybdenum assay (PMA) were studied. Highest TPC and TFC (189.57 ± 1.9 mg TAE/g extract, 30.48 ± 0.7 mg CE/g extract, respectively) were reported from acetone extract of the leaves. Ethanolic fruit extract showed the highest TTC (13.79 ± 0.2 mg CE/g extract). Acetone and acetonitrile fruit extract revealed maximum TTEC (602.79 ± 3.5 mg UAE/g extract) and moderate TAC (19.96 ± 0.9 mg GE/g extract), respectively. In AOX, highest DPPH (50.52 ± 0.03 mg AAE/g extract) and ABTS (26.78 ± 0.03 mg TE/g extract) radical scavenging reported in methanolic extract of fruit; however, acetone extract of leaf showed highest FRAP (376.89 ± 1.95 mg Fe(II)/g extract) and PMA (326.54 ± 4.73 mg AAE/g extract). In contrast, aqueous extract of leaf and fruit revealed highest metal chelating activity (41.67 ± 0.49 mg EDTA/g extract). In anti-diabetic studies, acetonitrile extract of leaves and fruits exhibited appreciable inhibition of α-amylase (83.33%) and α-glycosidase (77.42%) enzymes. Similarly, acetyl cholinesterase (AChE) inhibition was highest in water (88.91%) and acetone (81.87%) extracts of leaf and fruits. Fruit extracts showed potent anticancer activity against breast (MCF-7) and colon (HT-29) cancer cell lines (LC50 329.36 and 385.17 µg/mL, respectively). RP-HPLC analysis revealed highest cucurbitacin B (CuB) (196.24 ± 1.4 mg/g DW), followed by cucurbitacin I (CuI) and cucurbitacin E (CuE) in the fruits (57.14 ± 4.9 and 2.03 ± 0.03 mg/g DW, respectively). RP-HPLC analysis of extracts revealed presence of gallic acid (GA), catechin (CA), vanillic acid (VA), chlorogenic acid (CHLA) and coumaric acid (COA), in which highest GA found in the fruits (1.26 ± 0.07 mg/g DW). Liquid chromatography and mass spectrometry (LC-MS) and gas chromatography-mass spectrometry (GC-MS) analysis revealed presence of bioactive compounds from various groups. Based on the present findings, it was revealed that the fruit and leaf of L. echinata can be used as potent bioresource for natural antioxidants, anti-diabetic, and anticancer drug.

Project description:Breonadia salicina (Vahl) Hepper and J.R.I. Wood is widely used in South Africa and some other African countries for treatment of various infectious diseases such as diarrhea, fevers, cancer, diabetes and malaria. However, little is known about the active constituents associated with the biological activities. This study is aimed at exploring the metabolomics profile and antioxidant constituents of B. salicina. The chemical profiles of the leaf, stem bark and root of B. salicina were comprehensively characterized using proton nuclear magnetic resonance (1H-NMR) spectroscopy and ultra-performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS). The antioxidant activities of the crude extracts, fractions and pure compounds were determined using the DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging and reducing power assays. A total of 25 compounds were tentatively identified using the UPLC-QTOF-MS. Furthermore, the 1H-NMR fingerprint revealed that the different parts of plant had differences and similarities among the different crude extracts and fractions. The crude extracts and fractions of the root, stem bark and leaf showed the presence of α-glucose, β-glucose, glucose and fructose. However, catechin was not found in the stem bark crude extracts but was found in the fractions of the stem bark. Lupeol was present only in the root crude extract and fractions of the stem bark. Furthermore, 5-O-caffeoylquinic acid was identified in the methanol leaf extract and its respective fractions, while the crude extracts and fractions from the root and dichloromethane leaf revealed the presence of hexadecane. Column chromatography and preparative thin-layer chromatography were used to isolate kaempferol 3-O-(2″-O-galloyl)-glucuronide, lupeol, d-galactopyranose, bodinioside Q, 5-O-caffeoylquinic acid, sucrose, hexadecane and palmitic acid. The crude methanol stem bark showed the highest antioxidant activity in the DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging activity with an IC50 value of 41.7263 ± 7.6401 μg/mL, whereas the root crude extract had the highest reducing power activity with an IC0.5 value of 0.1481 ± 0.1441 μg/mL. Furthermore, the 1H-NMR and UPLC-QTOF-MS profiles showed the presence of hydroxycinnamic acids, polyphenols and flavonoids. According to a literature survey, these phytochemicals have been reported to display antioxidant activities. Therefore, the identified hydroxycinnamic acid (caffeic acid), polyphenol (ellagic acid) and flavonoids (catechin and (epi) gallocatechin) significantly contribute to the antioxidant activity of the different parts of plant of B. salicina. The results obtained in this study provides information about the phytochemistry and phytochemical compositions of Breonadia salicina, confirming that the species is promising in obtaining constituents with medicinal potential primarily antioxidant potential.

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Comparative Assessment of the Antioxidant and Anticancer Activities of Plicosepalus acacia and Plicosepalus curviflorus: Metabolomic Profiling and In Silico Studies.

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