8 research outputs found

    UHPLC-MS characterisation of principal triterpene glycosides and biological activities of different solvent extracts of <i>Allochrusa gypsophiloides</i> (Caryophyllaceae)

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    A crude methanol extract of the roots of Allochrusa gypsophiloides (syn. Acanthophyllum gypsophiloides) (collected from the Tashkent region of Uzbekistan) was chemically characterised by UHPLC-ESI-QTOF-MS/MS analysis. The results indicate the presence of six major bisdesmosidic saponins derived from gypsogenin, gypsogenic and quillaic acids, including five compounds reported for the first time for this species. The chloroform, methanol and water extracts of A. gypsophiloides showed weak antioxidant and anthelmintic activities. Among the tested extracts, the water extract exhibited the highest level of cytotoxicity in CCRF-CEM and CEM/ADR5000 cell lines with IC50 values of 23.6 and 31.9 µg/mL, respectively.</p

    Lycorine suppresses the malignancy of breast carcinoma by modulating epithelial mesenchymal transition and β-catenin signaling

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    Lycorine, an isoquinoline alkaloid can exhibit significant anti-cancer effects. The present study was conducted to illustrate the underlying mechanisms of action of lycorine on breast carcinoma under in vitro and in vivo settings Tandem Mass Tag assay and Kyoto Encyclopedia of Genes and Genomes analysis revealed that 20 signaling pathways were closely related to tumorigenesis, especially Wnt signaling pathway and tight junctions. The results demonstrated that lycorine evidently inhibited the proliferation of MDA-MB-231 and MCF-7 cells with IC50 values of 1.84 ± 0.21 μM and 7.76 ± 1.16 μM, respectively. It also blocked cell cycle in G2/M phase, caused a decrease in mitochondrial membrane potential, and induced apoptosis pathways through regulating caspase-3, caspase-8, caspase-9, and PARP expression. Moreover, lycorine effectively repressed the β-catenin signaling and reversed epithelial-mesenchymal transition (EMT) process. Furthermore, 4T1/Luc homograft tumor model was used to further demonstrate that lycorine significantly inhibited the growth and metastasis of breast tumor. These findings highlight the significance of lycorine as potential anti-neoplastic agent to combat breast cancer

    Berberine inhibits breast carcinoma proliferation and metastasis under hypoxic microenvironment involving gut microbiota and endogenous metabolites

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    A potential role of berberine, a benzyl isoquinoline alkaloid, in cancer therapy is apparent. Its underlying mechanisms of berberine against breast carcinoma under hypoxia have not been elucidated. We focused on the doubt how berberine restrains breast carcinoma under hypoxia in vitro and in vivo. A molecular analysis of the microbiome via 16 S rDNA gene sequencing of DNA from mouse faeces confirmed that the abundances and diversity of gut microbiota were significantly altered in 4T1/Luc mice with higher survival rate following berberine treatment. A metabolome analysis liquid chromatography-mass spectrometer/mass spectrometer (LC-MS/MS) revealed that berberine regulated various endogenous metabolites, especially L-palmitoylcarnitine. Furthermore, the cytotoxicity of berberine was investigated in MDA-MB-231, MCF-7, and 4T1 cells. In vitro to simulate under hypoxic environment, MTT assay showed that berberine inhibited the proliferation of MDA-MB-231, MCF-7, and 4T1 cells with IC50 values of 4.14 ± 0.35 μM, 26.53 ± 3.12 μM and 11.62 ± 1.44 μM, respectively. Wound healing and trans-well invasion studies revealed that berberine inhibited the invasion and migration of breast cancer cells. RT-qPCR analysis shed light that berberine reduced the expression of hypoxia-inducible factor-1α (HIF-1α) gene. Immunofluorescence and western blot demonstrated that berberine decreased the expression of E-cadherin and HIF-1α protein. Taken together, these results provide evidence that berberine efficiently suppresses breast carcinoma growth and metastasis in a hypoxic microenvironment, highlighting the potential of berberine as a promising anti-neoplastic agent to combat breast carcinoma

    Biological characteristics of <i>Edgeworthia tomentosa</i> (Thunb.) Nakai flowers and antimicrobial properties of their essential oils

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    <p><i>Edgeworthia tomentosa</i> (Thunb.) Nakai belongs to Thymelaeaceae family<i>,</i> its alabastrum is used as the traditional Chinese medicine ‘<i>Buddleja Officinalis Maxim’</i>. The present study was to elucidate the ultrastructure characteristics of the flower, the phytochemical composition of the aroma essential oils (EOs) and the relevant antimicrobial properties. There were exclusive characters of calyx, ovule, anther and pollen grain of the flowers under scanning electron microscopy. A total of 40 phytochemical components representing 98% of the EOs were successfully identified: monoterpenes and sesquiterpenes were the dominant terpenoids according to Kovats retention index and MS database. EOs exhibited a broad spectrum antimicrobial activity against Gram-positive and Gram-negative bacteria, the best bacteriostatic effect was against <i>Diplococcus pneumonia</i> with MIC and MBC values ranging between 7.8 and 62.5 and 26.0–71.0 μg/mL, respectively. These results demonstrate that the surface microscopic morphological characteristics of <i>Edgeworthia chrysantha</i> Lindl. flowers, are full-scale chemical composition and antimicrobial properties of the EOs.</p

    Volatile Secondary Metabolites with Potent Antidiabetic Activity from the Roots of Prangos pabularia Lindl.—Computational and Experimental Investigations

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    (1) Background: Almost 500 million people worldwide are suffering from diabetes. Since ancient times, humans have used medicinal plants for the treatment of diabetes. Medicinal plants continue to serve as natural sources for the discovery of antidiabetic compounds. Prangos pabularia Lindl. is a widely distributed herb with large reserves in Tajikistan. Its roots and fruits have been used in Tajik traditional medicine. To our best knowledge, there are no previously published reports concerning the antidiabetic activity and the chemical composition of the essential oil obtained from roots of P. pabularia. (2) Methods: The volatile secondary metabolites were obtained by hydrodistillation from the underground parts of P. pabularia growing wild in Tajikistan and were analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). Protein tyrosine phosphatase 1B (PTP-1B) inhibition assay and molecular docking analysis were carried out to evaluate the potential antidiabetic activity of the P. pabularia essential oil. (3) Results: The main constituents of the volatile oil of P. pabularia were 5-pentylcyclohexa-1,3-diene (44.6%), menthone (12.6%), 1-tridecyne (10.9%), and osthole (6.0%). PTP-1B inhibition assay of the essential oil and osthole resulted in significant inhibitory activity with an IC50 value of 0.06 &plusmn; 0.01 and 0.93 &plusmn; 0.1 &mu;g/mL. Molecular docking analysis suggests volatile compounds such as osthole inhibit PTP-1B, and the results are also in agreement with experimental investigations. (4) Conclusions: Volatile secondary metabolites and the pure isolated compound (osthole) from the roots of P. pabularia exhibited potent antidiabetic activity, twenty-five and nearly two times more than the positive control (3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-(4-(thiazol-2-ylsulfamyl)-phenyl)-amide)) with an IC50 value of 1.46 &plusmn; 0.4 &mu;g/mL, respectively
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