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Breast cancer is the most common cancer type and a primary cause of cancer mortality among females worldwide. Here, we analyzed the anticancer efficacy of a novel bromochlorinated monoterpene, PPM1, a synthetic analogue of polyhalogenated monoterpenes from Plocamium red algae and structurally similar non-brominated monoterpenes. PPM1, but not the non-brominated monoterpenes, decreased selectively the viability of several triple-negative as well as triple-positive breast cancer cells with different p53 status without significantly affecting normal breast epithelial cells. PPM1 induced accumulation of triple-negative MDA-MB-231 cells with 4N DNA content characterized by decreased histone H3-S10/T3 phosphorylation indicating cell cycle arrest in the G2 phase. Western immunoblot analysis revealed that PPM1 treatment triggered an initial rapid activation of Aurora kinases A/B/C and p21Waf1/Cip1 accumulation, which was followed by accumulation of polyploid >4N cells. Flow cytometric analysis showed mitochondrial potential disruption, caspase 3/7 activation, phosphatidylserine externalization, reduction of the amount polyploid cells, and DNA fragmentation consistent with induction of apoptosis. Cell viability was partially restored by the pan-caspase inhibitor Z-VAD-FMK indicating caspase contribution. In vivo, PPM1 inhibited growth, proliferation, and induced apoptosis in MDA-MB-231 xenografted onto the chick chorioallantoic membrane. Hence, Plocamium polyhalogenated monoterpenes and synthetic analogues deserve further exploration as promising anticancer lead compounds.

The family of polyhalogenated monoterpenes from Plocamium counts over a hundred known members. Using glyceraldehyde acetonide as a chiral-pool precursor, an enantioselective and divergent strategy was developed that provides a blueprint for the synthesis of many of the small yet complex acyclic members of this family. The broad applicability of this approach is demonstrated with the short, eight-step synthesis of four natural products and three analogues. These syntheses are the first of any members of the acyclic polyhalogenated Plocamium monoterpenes and permitted the evaluation of their selectivity against a range of tumor cell lines.

Introduction: This research explores sustainable applications for waste generated from fenugreek (Trigonella foenum‐graecum), a plant with both nutritional and medicinal uses. The study specifically targets waste components as potential sources of nutrients and bioactive compounds. Objectives: The focus is to conduct detailed metabolic profiling of fenugreek waste, assess its anti‐inflammatory properties by studying its cyclooxygenase (COX) inhibitory effect, and correlate this effect to the metabolite fingerprint. Materials and Methods: Ethanolic extracts of fenugreek fruit pericarp and a combination of leaves and stems were subjected to untargeted metabolic profiling using liquid chromatography–mass spectrometry integrated with online database searches and molecular networking as an effective dereplication strategy. The study also scrutinized the COX inhibitory capabilities of these extracts and saponin‐rich fractions prepared therefrom. Molecular docking was employed to investigate the specific interactions between the identified saponins and COX enzymes. Results: The analysis led to the annotation of 81 metabolites, among which saponins were predominant. The saponin‐rich fraction of the fruit pericarp extract displayed the strongest COX‐II inhibitory activity in the in vitro inhibition assay (IC50 value of 81.64 ± 3.98 μg/mL). The molecular docking study supported the selectivity of the identified saponins towards COX‐II. The two major identified saponins, namely, proto‐yamogenin 3‐O‐[deoxyhexosyl (1 → 2)] [hexosyl (1 → 4)] hexoside 26‐O‐hexoside and trigofenoside A, were predicted to have the highest affinity to the COX‐II receptor site. Conclusion: In the present study, we focused on the identification of COX‐II inhibitory saponins in fenugreek waste through an integrated approach. The findings offer valuable insights into potential anti‐inflammatory and cancer chemoprotective applications of fenugreek waste. The ethanolic extracts of fenugreek wastes were subjected to LC‐MS/MS untargeted metabolic profiling and molecular networking, leading to the annotation of 81 metabolites, with saponins being major constituents. A saponin‐rich fraction was prepared from each waste extract. The COX inhibitory effect of the waste extracts and saponin‐rich fractions was evaluated. The saponin‐rich fractions showed a preferential COX‐II inhibition that was stronger than the ethanolic extracts. Molecular docking proved the selectivity of the identified saponins towards COX‐II enzyme. [ABSTRACT FROM AUTHOR]

Breast cancer is the most devastating disease for women. There is a great demand for new sources to treat this disease. Medicinal plants are an indispensable source of bioactive compounds with wide range of pharmacological activities. In-vitro cytotoxic activity of Otostegia fruticosa methanolic extract against human breast cancer was studied using MCF-7 cell line. The extract showed mildly potent activity (IC50 = 51 ± 9.836 µg/mL) in comparison to the standard anticancer doxorubicin (IC50 = 7.467 ± 1.05 µg/mL). Potential compounds responsible for activity have been identified using Molecular Operating Environment (MOE) module on the major compounds detected by HPLC-MS/MS technique against estrogen alpha receptor (ERα+: PDB ID 2JF9). 3,5-di-O-dicaffeoylquinic acid, hyperoside and rutin showed similar binding and antagonistic interaction with the estrogen alpha receptor as tamoxifen in several poses. The retrieved results confirm that we can add this plant to a powerful arsenal that combats this insidious disease. [ABSTRACT FROM AUTHOR]

The ink that cephalopods secrete to hide and frighten the enemies contains a treasury rich in bioactive diverse compounds like DOPA, melanin, melanin synthase, tyrosinase, angiotensin converting enzyme, catecholamines, oligopeptides, polyphenols, flavonoids, alkaloids, polysaccharides, fatty acids and minerals. These groups of the aforementioned compounds have promising unique in-vitro and in-vivo biological activities like antioxidant activity, anti-inflammatory, vasopressin, anti-Parkinson, anti-cancer, anti-coagulant, antimicrobial, anti-retroviral, anti-ulcerogenic and immune boosting activities. Cephalopods ink can be offered in its raw state or after separation and purification of its chemical constituents for use as natural medicine to treat many diverse diseases. [ABSTRACT FROM AUTHOR]

As a result of our continuous research efforts to investigate the molecular mechanisms of Eucalyptus kino polyphenolics for healing liver solid tumors, in-vivo histopathological studies of the solid tumor tissues and in-silico molecular docking were carried out. Histopathology of female mice treated with a dose of 200 mg/kg Eucalyptus kino methanolic extract in combination with low level ionising γ-radiation (0.25 Gy) recovered a near-to-normal histological structure revealing a substantial number of cells with hyper-chromachia in nuclei, fibroblast lobules and necrotic cells. Analysis for matrix metalloproteinase-9 (MMP-9) by Western blot and also molecular docking study were conducted to evaluate and rank the potential of the individual components dominated in the extract to inhibit MMP-9 and TGF-β. The current study presents new lead compounds for the design of novel MMP-9 and TGF-β strong inhibitors of natural origin. [ABSTRACT FROM AUTHOR]

This correction notice emphasizes that the experiments conducted in the original publication were done simultaneously with several plant species, and identical control groups were used for both articles. This decision was made to minimize animal usage and ensure reliable results. The authors apologize for not disclosing this similarity in the original submission. Additionally, there was a mistake in the legend for Figure 11 in the original publication. The authors state that the scientific conclusions are unaffected, and the original publication has been updated. [Extracted from the article]

Withania somnifera, Angelica sinensis, Glycyrrhiza glabra, and Simmondsia chinensis were acquired from the Egyptian market, profiled for their chemical constituents, screened for the in-vitro MAO-B inhibitory activity and evaluated for the total phenolic content. Thirty compounds were characterized in the selected herbs using HPLC-MS/MS. In-vitro MAO-B inhibitory activity and total phenolic content of the acquired herbs were compared with those of a prepared herbal formula consisting of a mixture of equal amounts of the four mentioned herbs. The most potent MAO-B inhibitory activity was exerted by the methanol extract of the prepared formula (IC50 of 712.19 ± 13.90 ng/mL) compared to selegiline (IC50 of 581.69 ± 11.35 ng/mL). The highest value of the total phenolic content was shown by Angelica sinensis methanolic extract (76.15 ± 0.1 mg/g) followed by Glycyrrhiza glabra methanolic extract (65.74 ± 0.1 mg/g), then the mixture's methanolic extract of the four herbs (37.04 ± 0.1 mg/g). [ABSTRACT FROM AUTHOR]

30 secondary polyphenolic metabolites were characterised in Eucalyptus kino methanol extract using HPLC-MS/MS. The antitumor activity of the extract in combination with low level ionising radiation in female mice with solid tumors from inoculated Ehrlich ascites carcinoma cells was investigated. Tumor cell-inoculated mice received daily extract doses (100 mg/kg, 200 mg/kgBW) with or without a single exposure to 0.25 Gy γ-rays, and cis-platin as a reference anticancer drug. Changes in the tumor volume, oxidative state, levels of caspase-3, TGF-β and Nf-κB were assessed by q-PCR. Surprisingly, a dose of 200 mg/kg extract together with γ-radiation remarkably reduced the tumor volume, improved the oxidative and apoptotic biomarker levels. In conclusion, results showed that a combination of kino extract with low level γ-radiation synergistically reduced tumor progression due to the antioxidant and anti-proliferative activities of the polyphenolics in the extract. [ABSTRACT FROM AUTHOR]

Turraea fischeri is an East African traditional herb, which is widely used in traditional medicine. In this study, we profiled the secondary metabolites in the methanol extract of T. fischeri bark using HPLC-PDA-ESI-MS/MS, and 20 compounds were tentatively identified. Several isomers of the flavonolignan cinchonain-I and bis-dihydroxyphenylpropanoid-substituted catechin hexosides dominated the extract. Robust in vitro and in vivo antioxidant properties were observed in 1,1-diphenyl-2-picrylhydrazyl radical scavenging assay (DPPH) and ferric reducing antioxidant power (FRAP) assay, and in the model organism Caenorhabditis elegans. Additionally, the extract exhibited promising hepatoprotective activities in D-galactosamine (D-GaIN) treated rats. A significant reduction in the elevated levels of aspartate aminotransferase (AST), total bilirubin, gamma-glutamyltransferase (GGT), and malondialdehyde (MDA) and increase of glutathione (GSH) was observed in rats treated with the bark extract in addition to D-galactosamine when compared with rats treated with D-galactosamine alone. In conclusion, T. fischeri is apromising candidate for health-promoting and for pharmaceutical applications. [ABSTRACT FROM AUTHOR]

As part of our continued search for bioactive secondary metabolites from marine sources using a bioassay-guided fractionation technique (Cytotoxic and anti-trypanosome activities), we have examined the organic extract of Papua New Guinean collection of the green alga Udotea orientalis growing on the Gorgonian coral Pseudopterogorgia rigida. Successive HPLC investigations resulted in isolation of three new compounds, (+) curcuepoxide A, (+) curcuepoxide B and (+)-10α-hydroxycurcudiol. Analysis of different spectroscopic data e.g. UV, IR, LRMS, HRMS, 1D NMR and 2D NMR on the isolated compounds allowed for construction of the planar structures. Stereochemistry assignment at C-7 and C-10 in the new compounds was discussed. Isolated compounds were found to be active in an in vitro assay of antitrypanosome activity. The isolated compounds were found to have variable cytotoxic activity in human lung cancer cell lines. [ABSTRACT FROM AUTHOR]