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1.
Curr Pharm Des ; 29(42): 3400-3407, 2023.
Article in English | MEDLINE | ID: mdl-38053351

ABSTRACT

BACKGROUND: Peripheral neuropathy is a common complication that affects individuals with diabetes. Its development involves an excessive presence of oxidative stress, which leads to cellular damage in various tissues. Schwann cells, which are vital for peripheral nerve conduction, are particularly susceptible to oxidative damage, resulting in cell death. MATERIALS AND METHODS: Gamma-mangostin (γ-mangostin), a xanthone derived from Garcinia mangostana, possesses cytoprotective properties in various pathological conditions. In this study, we employed S16Y cells as a representative Schwann cell model to investigate the protective effects of γ-mangostin against the toxicity induced by tert-Butyl hydroperoxide (tBHP). Different concentrations of γ-mangostin and tBHP were used to determine non-toxic doses of γ-mangostin and toxic doses of tBHP for subsequent experiments. MTT cell viability assays, cell flow cytometry, and western blot analysis were used for evaluating the protective effects of γ-mangostin. RESULTS: The results indicated that tBHP (50 µM) significantly reduced S16Y cell viability and induced apoptotic cell death by upregulating cleaved caspase-3 and cleaved PARP protein levels and reducing the Bcl- XL/Bax ratio. Notably, pretreatment with γ-mangostin (2.5 µM) significantly mitigated the decrease in cell viability caused by tBHP treatment. Furthermore, γ-mangostin effectively reduced cellular apoptosis induced by tBHP. Lastly, γ-mangostin significantly reverted tBHP-mediated caspase-3 and PARP cleavage and increased the Bcl-XL/Bax ratio. CONCLUSION: Collectively, these findings highlight the ability of γ-mangostin to protect Schwann cells from apoptotic cell death induced by oxidative stress.


Subject(s)
Apoptosis , Poly(ADP-ribose) Polymerase Inhibitors , Xanthones , Humans , tert-Butylhydroperoxide/toxicity , Caspase 3/metabolism , Caspase 3/pharmacology , bcl-2-Associated X Protein/metabolism , bcl-2-Associated X Protein/pharmacology , Poly(ADP-ribose) Polymerase Inhibitors/pharmacology , Oxidative Stress , Schwann Cells/metabolism , Cell Survival
2.
Environ Technol ; : 1-10, 2022 Nov 15.
Article in English | MEDLINE | ID: mdl-36315008

ABSTRACT

A novel platform of a polydiacetylene combined with rhodamine B (PDA-Rho) colorimetric chemosensor array was prepared from a diacetylene monomer and rhodamine B derivative. Rhodamine B derivative as the ion-recognition element was embedded in the polydiacetylene matrix. To fabricate chemosensor, diacetylene monomer connected rhodamine B derivatives (DA-Rho) was coated onto a filter paper surface via drop-casting technique and transformed to polydiacetylene by polymerisation through ultraviolet (UV) irradiation. From the result, PDA-Rhoen exhibited high sensitivity and selectivity for Au3+ and could be monitored directly by naked eyes providing a fast, portable and easy-to-use as a molecular device in the real system. The DFT calculation results showed a stable complex between PDA-Rho and Au3+. We believe that, this method offers a sensitive and accurate process for Au3+ ion detection in real environmental and biological applications.

3.
Molecules ; 27(4)2022 Feb 15.
Article in English | MEDLINE | ID: mdl-35209099

ABSTRACT

Natural compounds have been recognized as valuable sources for anticancer drug development. In this work, different parts from Momordica cochinchinensis Spreng were selected to perform cytotoxic screening against human prostate cancer (PC-3) cells. Chromatographic separation and purification were performed for the main constituents of the most effective extract. The content of the fatty acids was determined by Gas Chromatography-Flame Ionization Detector (GC-FID). Chemical structural elucidation was performed by spectroscopic means. For the mechanism of the apoptotic induction of the most effective extract, the characteristics were evaluated by Hoechst 33342 staining, sub-G1 peak analysis, JC-1 staining, and Western blotting. As a result, extracts from different parts of M. cochinchinensis significantly inhibited cancer cell viability. The most effective stem extract induced apoptosis in PC-3 cells by causing nuclear fragmentation, increasing the sub-G1 peak, and changing the mitochondrial membrane potential. Additionally, the stem extract increased the pro-apoptotic (caspase-3 and Noxa) mediators while decreasing the anti-apoptotic (Bcl-xL and Mcl-1) mediators. The main constituents of the stem extract are α-spinasterol and ligballinol, as well as some fatty acids. Our results demonstrated that the stem extract of M. cochinchinensis has cytotoxic and apoptotic effects in PC-3 cells. These results provide basic knowledge for developing antiproliferative agents for prostate cancer in the future.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Apoptosis/drug effects , Drug Resistance, Neoplasm/drug effects , Momordica/chemistry , Plant Extracts/pharmacology , Plant Stems/chemistry , Antineoplastic Agents, Phytogenic/chemistry , Apoptosis/genetics , Biomarkers, Tumor , Cell Line, Tumor , Cell Proliferation/drug effects , Cell Survival/drug effects , Dose-Response Relationship, Drug , Gene Expression Regulation, Neoplastic/drug effects , Humans , Models, Molecular , Molecular Structure , Phytochemicals/chemistry , Phytochemicals/pharmacology , Plant Extracts/chemistry , Structure-Activity Relationship
4.
Biomed Pharmacother ; 147: 112577, 2022 Mar.
Article in English | MEDLINE | ID: mdl-35078092

ABSTRACT

Cowanin, a xanthone derivative extracted from the Garcinia fusca plant, has been recognized for various biological activities including, antimicrobial, anti-inflammatory, and anticancer activities. However, the mechanism to induce cancer cell death in cancer cells remains to be fully elucidated. Our previous report showed that other xanthones from these plants could act as histone deacetylase inhibitors (HDACi), so we deeply analyzed the role of cowanin, a major compound of G.fusca, and investigated through the mode of cell death both apoptosis and autophagy that have never been reported. As a result, it was demonstrated that cowanin indicated the role of HDACi as other xanthones. The molecular docking analysis showed that cowanin could interact within the catalytic pocket region of HDAC class I (HDAC2, 8) and II (HDAC4, 7) proteins and inhibit their activity. Also, the level of protein expression of HDAC2, 4, 7, and 8 was distinctly decreased, and the level of histone H3 and H4 acetylation increased in cowanin treated cells. For the mode of cell death, cowanin demonstrated both apoptosis and autophagy activation in Jurkat cells. Besides, cowanin significantly suppressed phosphorylation of PI3K, Akt, and mTOR signaling. Therefore, these findings revealed that cowanin represents a new promising candidate for development as an anticancer agent by inducing apoptosis and autophagy via PI3K/AKT/mTOR pathway and effectively inhibiting HDAC activity.


Subject(s)
Garcinia , Histone Deacetylase Inhibitors , Plant Extracts , Humans , Apoptosis/drug effects , Autophagy/drug effects , Histone Deacetylase Inhibitors/chemistry , Histone Deacetylase Inhibitors/pharmacology , Histone Deacetylase Inhibitors/therapeutic use , Jurkat Cells/drug effects , Phosphatidylinositol 3-Kinases/metabolism , Phytotherapy , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Proto-Oncogene Proteins c-akt/metabolism , Signal Transduction/drug effects , TOR Serine-Threonine Kinases/metabolism
5.
Fitoterapia ; 146: 104637, 2020 Oct.
Article in English | MEDLINE | ID: mdl-32470371

ABSTRACT

Three new oxygenated xanthones, fuscaxanthones L-N (1-3), and 14 known xanthones 4-17, together with the other known metabolites 18-20 were isolated from the stem barks of Garcinia fusca Pierre. Their chemical structures were determined based on NMR and MS spectroscopic data analysis, as well as single X-ray crystallography. The geranylated compounds, cowanin (13), cowagarcinone E (15), norcowanin (16) and cowanol (17) exhibited potent inhibitions against acetylcholinesterase (AChE) (IC50 0.33-1.09 µM) and butyrylcholinesterase (BChE) (IC50 0.048-1.84 µM), which were more active than the reference drug, galanthamine. Compound 15 was highly potent BChE inhibitor (IC50 0.048 µM) and was 76-fold more potent than the drug. Structure-activity relationship studies indicated that the C-2 prenyl and C-8 geranyl substituents in the tetraoxygenated scaffold are important for high activity. Molecular docking studies revealed that the leads 13 and 15-17 showed similar binding orientations on both enzymes and very well-fitted at the double binding active sites of PAS and CAS with strong hydrophobic interactions from both isoprenyl side chains.


Subject(s)
Cholinesterase Inhibitors/pharmacology , Garcinia/chemistry , Plant Bark/chemistry , Xanthones/pharmacology , Acetylcholinesterase , Butyrylcholinesterase , Cholinesterase Inhibitors/isolation & purification , Molecular Docking Simulation , Molecular Structure , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Structure-Activity Relationship , Thailand , Xanthones/isolation & purification
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