JOURNAL OF ETHNOPHARMACOLOGY
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2023
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IF 5.4
Yan Cao,Jinpeng Lv,Yan Tan,Ruolin Chen,Xiaoxue Jiang,Duo Meng,Kun Zou,Min Pan,Liming Tang
Ethnopharmacological relevance Tribuloside, a natural flavonoid extracted from Chinese medicine Tribulus terrestris L., has shown potent efficacy in treating various diseases. In China, the fruits of Tribulus terrestris L. have long been utilized for relieving headache, dizziness , itchiness, and vitiligo . Water-based extract derived from Tribulus terrestris L. can enhance melanogenesis in mouse hair follicle melanocytes by elevating the expression of α-melanocyte stimulating hormone (α-MSH) and melanocortin-1 recepter (MC-1R). Nevertheless, there is a lack of information regarding the impact of tribuloside on pigmentation in both laboratory settings and living organisms. Aim of the study The present research aimed to examine the impact of tribuloside on pigmentation, and delve into the underlying mechanism. Materials and methods Following the administration of tribuloside in human epidermal melanocytes (HEMCs), we utilized microplate reader, Masson-Fontana ammoniacal silver stain, transmission electron microscopy (TEM) and scanning electron microscopy (SEM) to measure melanin contents, dendrite lengths, melanosome counts; L-DOPA oxidation assay to indicate tyrosinase activity, Western blotting to evaluate the expression of melanogenic and associated phosphodiesterase (PDE)/cyclic adenosine monophosphate (cAMP)/cyclic-AMP dependent protein kinase A (PKA) pathway proteins. A PDE-Glo assay to verify the inhibitory effect of tribuloside on PDE was also conducted. Additionally, we examined the impact of tribuloside on the pigmentation in both zebrafish model and human skin samples. Results Tribuloside had a notable impact on the production of melanin in melanocytes, zebrafish, and human skin samples. These functions might be attributed to the inhibitory effect of tribuloside on PDE, which could increase the intracellular level of cAMP to stimulate the phosphorylation of cAMP-response element binding (CREB). Once activated, it induced microphthalmia-associated transcription factor (MITF) expression and increased the expression of tyrosinase, Rab27a and cell division cycle protein 42 (Cdc42), ultimately facilitating melanogenesis, melanocyte dendricity, and melanin transport. Conclusion Tribuloside acts on the PDE/cAMP/PKA pathway to enhance melanogenesis, melanocyte dendricity, and melanosome transport; meanwhile, tribuloside does not have any toxic effects on cells and may be introduced into clinical prescriptions to promote pigmentation.
研究领域:
药理学
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细胞生物学
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分子生物学
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民族药理学
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DOI
PubMed
高影响因子
ANALYTICAL AND BIOANALYTICAL CHEMISTRY
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2023
·Vol. 415
·期 14
·2677-2692
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IF 4.3
Meng Xin,Zong Hou,Zheng Zhong,Xing Junpeng,Liu Zhiqiang,Song Fengrui,Liu Shu
α-Glucosidase inhibitors in natural products are one of the promising drugs for the treatment of type 2 diabetes. However, due to the complexity of the matrix, it is challenging to comprehensibly clarify the specific pharmacodynamic substances. In this study, a novel high-throughput inhibitor screening strategy was established based on covalent binding of α-glucosidase on chitosan-functionalized multi-walled carbon nanotubes coupled with high-resolution mass spectrometry. The synthesized MWCNTs@CS@GA@α-Glu was characterized by TEM, SEM, FTIR, Raman, and TG. Performance studies showed that the microreactor exhibited stronger thermostability and pH tolerance than that of the free one while maintaining its inherent catalytic activity. Feasibility study applying a model mixture of known α-glucosidase ligand and non-ligands indicated the selectivity and specificity of the system. By integrating ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-QTOF-MS) with ion mobility mass spectrometry (IMS), 15 ligands were obtained and tentatively identified from Tribulus terrestris L., including 8 steroidal saponins, 4 flavonoids, and 3 alkaloids. These inhibitors were further validated by in vivo experiments and molecular docking simulation.
研究领域:
药理学
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分析化学
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纳米技术
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植物科学
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DOI
PubMed
高影响因子
Journal of Analysis and Testing
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2023
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IF 4.7
Yang Jingxuan,Guo Wenjun,Xu Xiaohang,Zhao Liang,Xu Yajuan,Wang Yang
Fatty acids (FAs) are an important class of functional small molecules and participate in a variety of life biological processes. This experiment proposed a liquid chromatography–quadrupole-Qrbitrap mass spectrometry (LC–Q-Orbitrap MS) method to perform FA profiling under parallel reaction monitoring (PRM) acquisition mode. The FA was derivatized by 2-dimethylaminoethylamine (DMED) to increase the ionization efficiency and provide the characterized fragment pattern. The mass spectra obtained from full scan, multiple ion monitoring (MIM), and PRM were compared. The results showed that the protonated ion of FA + DMED–H 2 O was detected and the neutral loss of 45.06 Da was observed in the tandem mass spectrum. The PRM method provided the highest selectivity and sensitivity for FA detection with the help of accurate mass weight and specific neutral loss-based fragments. The method validation was performed using the FA standards and pooled quality control serum sample, which showed that the established method had good repeatability, stability, and linearity. Finally, the developed method was successfully applied to analyze the rat serum and brain tissue samples for the drug efficacy evaluation of gross saponin of Tribulus terrestris L. fruit (GSTTF) against middle cerebral artery occlusion (MCAO)-induced ischemic stroke. This method has extensive practicability and great potential in the detection of FA, especially for the analysis of samples with complex matrices.
研究领域:
分析化学
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药理学
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神经科学
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生物化学
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DOI
高影响因子
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