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SEPARATION AND PURIFICATION TECHNOLOGY · 2020 · IF 5.774

Selective extraction of quinolizidine alkaloids from Sophora flavescens Aiton root using tailor-made deep eutectic solvents and magnetic molecularly imprinted polymers

Xun Kang,Linlin Deng,Tian Quan,Manjie Gao,Kailian Zhang,Zhining Xia,Die Gao

In this study, an eco-friendly extraction method that used tailor-made deep eutectic solvents (DESs) for the extraction of oxymatrine and matrine from Sophora flavescens Aiton root was implemented for the first time. The extraction parameters, including the DES type, DES water content, solid-to-liquid ratio, extraction time, and extraction temperature, which affected the extraction efficiencies of oxymatrine and matrine were optimised. High-performance liquid chromatography with a diode-array detector and quantitative analysis of the DES components was conducted. The highest oxymatrine and matrine extraction yields (21.04 and 1.53 mg·g −1 , respectively) were obtained using DES-2 (comprising choline chloride and malonic acid; molar ratio of 1:2) with 50% water and DES-8 (comprising choline chloride and ethylene glycol; molar ratio of 1:2) with 30% water as the extraction solvents, respectively. Furthermore, magnetic molecularly imprinted polymers (MMIPs) were successfully synthesised using oxymatrine, acrylic acid, ethylene glycol dimethylacrylate, azobisisobutyronitrile, and acetonitrile–methylbenzene (3:1, v/v) as the template, functional monomer, cross-linker, initiator, and porogen, respectively. The MMIPs were characterised using transmission electron microscopy, Fourier-transform infrared spectroscopy, and X-ray diffraction analyses, and the results demonstrated the successful preparation of MMIPs. The adsorption properties of MMIPs were further analysed using static and dynamic adsorption experiments, and the results indicated that MMIPs presented good adsorption capacities for oxymatrine and matrine (110.8 and 63.4 mg·g −1 , respectively). Lastly, MMIPs were used as sorbents for the extraction and enrichment of oxymatrine and matrine from DES extracts of S. flavescens roots. The extraction efficiencies of oxymatrine and matrine (80.21–89.15% and 85.33–95.28%, respectively) were satisfactory. The proposed DES-based extraction followed by MMIPs secondary enrichment appeared to be an effective method for the selective extraction of specific components from complex samples.

研究领域: 植物化学 · 分析化学
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2013 ·Vol. 14 ·期 12 ·23751-23761 · IF 2.464

Antiepileptic Potential of Matrine via Regulation the Levels of Gamma-Aminobutyric Acid and Glutamic Acid in the Brain

Jun Xiang,Yugang Jiang

Our present study aimed to determine the antiepileptic activity of matrine, and explore the possible molecular mechanism. To evaluate the antiepileptic activity of matrine, seizures in mice induced by PTZ and MES were established, then the pentobarbital sodium-induced anaesthetizing time and locomotor activity tests in mice were also carried out. For the molecular mechanism investigations, contents of aspartic acid (Asp), gamma-aminobutyric acid (GABA), glutamic acid (Glu), glycine (Gly) in seizures mice were determined; then, the chronic seizures rats induced by PTZ were prepared, and western blotting was used to determine the expressions of GAD 65, GABAAand GABABin the brains. In the results, matrine showed significant antiepileptic effects on seizures mice induced by MES and PTZ. Moreover, the pentobarbital sodium-induced anaesthetizing time and locomotor activity tests were also demonstrated that matrine had obvious antiepileptic effects. Additionally, our results revealed that after treatment with matrine, contents of GABA can be elevated, and the contents of Glu were obviously decreased. Furthermore, western blotting revealed that the mechanism regarding the antiepileptic effect of may be related to the up-regulations of GAD 65 and GABAAin the brain. Collectively, we suggested that matrine can be developed as an effective antiseptic drug.Keywords:antiepileptic;matrine;gamma-aminobutyric acid;glutamic acid

研究领域: 药理学 · 神经科学
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EXPERIMENTAL PARASITOLOGY · 2016 · IF 1.623

Antiparasitic effects of oxymatrine and matrine against Toxoplasma gondii in vitro and in vivo

Xiaochuan Zhang,Lili Jin,Zhe Cui,Changhao Zhang,Xue Wu,Hyun Park,Hongmei Quan,Chunmei Jin

Toxoplasma gondii ( T . gondii ) is an important pathogen which can causes serious public health problems. Since the current therapeutic drugs for toxoplasmosis present serious host toxicity, research on effective and new substances of relatively low toxicity is urgently needed. This study was carried out to evaluate the anti-parasitic effect of oxymatrine (OM) and matrine (ME) against T . gondii in vitro and in vivo . In our study, the anti- T . gondii activities of ME and OM were evaluated in vitro using cell counting kit-8 assay, morphological observation and trypan blue exclusion assay. In vivo , mice were sacrificed four days post-infection and ascites were drawn out to determine the extent of tachyzoite proliferation. Viscera indexes and liver biochemical parameters, such as alanine aminotransferase (ALT), aspartate aminotransferase (AST), glutathione (GSH) and malondialdehyde (MDA), were examined to evaluate the toxicity of compounds to mice. As a result, OM and ME showed anti- T . gondii activity but low selectivity toxicity to HeLa cells. Both compounds also significantly decreased the number of tachyzoites in peritoneal cavity and recovered the levels of ALT, AST, GSH and MDA in liver. Moreover, the mice treated with OM or ME achieved better results in viscera index and survival rate than that of spiramycin. These results suggest that OM and ME are likely the sources of new drugs for toxoplasmosis, and further studies will be necessary to compare the efficacy of drug combination, as well as identify its action of mechanism.

CAS / MDL: 8025-81-8
研究领域: 寄生虫学 · 药理学 · 传染病学
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Journal of Cancer Research and Therapeutics · 2020 ·Vol. 16 ·期 2 ·209 · IF 1.326

Matrine inhibits proliferation and migration of HepG2 cells by downregulating ERK1/2 signaling pathways

Yu Haipeng,Zhu Bolan,Yang Wan,Zhang Qian,Wang Wei,Zhai Weichun,Lu Lixia,Zheng Ying,Dang Zheng,Li Bin,Li Chuyi,Liang Bin,Zhang Jiucong,Yu Xiaohui

Objective: To research the effect of matrine on the proliferation and migration of HepG2 cells through extracellular signal-regulated kinase 1/2 (ERK1/2) signaling pathway. Methods: HepG2 cell was selected and divided into blank control group, experimental group ( matrine 1, 2, and 4 mg/mL), and positive control group (PD98059, ERK1/2 inhibitor). MTT measure was used to detect the effective time and concentration which matrine inhibits HepG2 cells. After 24 h, the effect of effective concentration of matrine on the of morphological changing HepG2 cells was observed. The invasion ability was assayed by transwell method, the expression of ERK1/2 and pERK1/2 were detected through Western blot, and reverse transcription polymerase chain reaction was used to test the expression level of ERK1/2 mRNA. Results: With the increase of matrine concentration, the number of adherent HepG2 cells gradually decreased, the morphologic changes gradually became spherical, some cell morphology was incomplete, and even cell fragments appeared. The proliferation and invasion ability of HepG2 cells decreased. The expression of ERK1/2, pERK1/2, and ERK1/2 mRNA downregulated with the increase of matrine concentration (P < 0.05). Conclusion: Matrine inhibits the proliferation and migration of HepG2 cells by downregulating the ERK1/2 signaling pathway.

CAS / MDL: 519-02-8
研究领域: 肿瘤学 · 细胞生物学 · 药理学
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Biomed Research International · 2021 · IF 3.411

Analgesic and Anti-Inflammatory Activities of Sophocarpine from Sophora viciifolia Hance

F. L. Wang,H. Wang,J. H. Wang,D. X. Wang,Y. Gao,B. Yang,H. J. Yang,Y. B. Ji,G. S. Xin

Sophora viciifolia Hance is an edible plant used in traditional Chinese medicine. Sophocarpine, a tetracyclic quinolizidine alkaloid, is one of the most abundant active ingredients in Sophora viciifolia Hance. Here, we study the analgesic and anti-inflammatory effects, as well as the acute toxicity of sophocarpine from Sophora viciifolia Hance in mice. Sophocarpine (20, 40, and 80 mg/kgbw) significantly prolonged the delay period before a hot plate reaction occurred (all ), and the delay before a tail-flick response was induced by a warm bath (; ). Sophocarpine (40, 80 mg/kg) resulted in dose-dependent inhibition of the writhing reaction induced by acetic acid in mice (; , respectively). Sophocarpine (80 mg/kg) reduced the total duration of a formalin-induced pain response (). Sophocarpine prolonged the foot-licking latency of mice after the hot plate reaction, and this effect was antagonized by calcium chloride and enhanced by verapamil. Sophocarpine (20, 40, and 80 mg/kg) significantly inhibited xylene-induced ear edema (; ; , respectively) and the penetration of acetic acid-induced dye into the peritoneal cavity (; ; , respectively). It also reduced the levels of proinflammatory cytokine interleukin (IL)-1β, IL-6, and prostaglandin E2 (, , ) and those of serum nitric oxide (). The results of this study suggest that sophocarpine possesses certain analgesic and anti-inflammatory activities, which may be related to calcium and inhibition of the secretion of inflammatory factors.

研究领域: 药理学 · 中药学
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SENSORS · 2018 ·Vol. 18 ·期 10 ·3358 · IF 2.475

Construction of Multiple Switchable Sensors and Logic Gates Based on Carboxylated Multi-Walled Carbon Nanotubes/Poly(N,N-Diethylacrylamide)

Xuemei Wu,Xiaoqing Bai,Yang Ma,Jie Wei,Juan Peng,Keren Shi,Huiqin Yao

In this work, binary hydrogel films based on carboxylated multi-walled carbon nanotubes/poly(N,N-diethylacrylamide) (c-MWCNTs/PDEA) were successfully polymerized and assembled on a glassy carbon (GC) electrode surface. The electroactive drug probes matrine and sophoridine in solution showed reversible thermal-, salt-, methanol- and pH-responsive switchable cyclic voltammetric (CV) behaviors at the film electrodes. The control experiments showed that the pH-responsive property of the system could be ascribed to the drug components of the solutions, whereas the thermal-, salt- and methanol-sensitive behaviors were attributed to the PDEA constituent of the films. The CV signals particularly, of matrine and sophoridine were significantly amplified by the electrocatalysis of c-MWCNTs in the films at 1.02 V and 0.91 V, respectively. Moreover, the addition of esterase, urease, ethyl butyrate, and urea to the solution also changed the pH of the system, and produced similar CV peaks as with dilution by HCl or NaOH. Based on these experiments, a 6-input/5-output logic gate system and 2-to-1 encoder were successfully constructed. The present system may lead to the development of novel types of molecular computing systems.Keywords:electrocatalysis;encoder;logic gate;matrine;sophoridine

CAS / MDL: 7775-27-1
研究领域: 材料科学 · 生物医学工程
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CRYSTAL GROWTH & DESIGN · 2021 · IF 4.076

Cocrystals of Oxymatrine: Reducing Hygroscopicity and Affecting the Dissolution Rate

Ming-Hui Qi,Heng Li,Bin Zhu,Minghuang Hong,Guo-Bin Ren

Oxymatrine (OMT) is mainly used for the treatment of hepatitis B. In this work, one anhydrous form and three hydrates of OMT are reported and their transformational relationship is clarified. It is revealed that OMT has high hygroscopicity and fast release characteristics. In order to improve these physical properties, cocrystallization of OMT was performed. Five cocrystals of OMT with urea (OMT-Urea-DH), sulfanilamide (OMT-SUA), theophylline (OMT-THP), 2-ketoglutaric acid (OMT-KTA-MH), and 3-hydroxy-2-naphthoic acid (OMT-HNA) were obtained and characterized. According to the DVS tests, OMT-SUA, OMT-KTA-MH, and OMT-HNA enhance the hydroscopic stability of OMT by forming new hydrogen bonds. The dissolution rate of OMT has been drastically reduced through cocrystallization with THP and HNA.

CAS / MDL: 92-70-6
研究领域: 药学 · 化学
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Cancer Management and Research · 2023 · IF 3.3

Puerarin Enhances the Anti-Tumor Effect of Cisplatin on Drug-Resistant A549 Cancer in vivo and in vitro Through Activation of the Wnt Signaling Pathway

Ping Huang,Shi-Xia Du

Objective The effect of PUE on enhancing the anti-cancerous efficacy of DDP on drug-resistant A549/DDP cancer and the underlying mechanisms were thoroughly investigated.Materials and Methods The cytotoxicity of PUE, DDP, and PUE + DDP to A549 cells and A549/DDP cells, respectively, is determined by cell apoptosis experiments. Anti-proliferation effect of PUE, DDP, and PUE + DDP on A549 cells and A549/DDP cells is evaluated by the cell cloning assay. Qualitative and quantitative analysis of the levels of PUE, DDP, and PUE + DDP of cell proliferation-related genes and proteins expressions in A549/DDP cells are determined by Western blot assay. The levels of VEGF in A549/DDP cells after different treatment strategies are determined by ELISA assay. Qualitative and quantitative determination of VEGF expression in tumor tissues are done by immunohistochemical staining.Results In vitro cellular experiments revealed that co-incubation of A549/DDP cells with PUE and DDP led to a dramatically decreased cell viability and cell survival rate compared with the cells only treated by DDP. Such a stimulating effect of PUE on DDP was further confirmed in vivo with results shown that the A549/DDP cancer-bearing mice treaded by combination therapy achieved the lowest tumor growth rate and longest survival time.Conclusion Taking these results together, we can draw the conclusion that the PUE enhances the anti-tumor effect of DDP on the drug-resistant A549 cancer in vivo and in vitro through activation of the Wnt signaling pathway.

CAS / MDL: 3681-99-0
研究领域: 肿瘤学 · 药理学 · 分子生物学
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Smart Medicine · 2025 ·Vol. 4 ·期 1 ·e136 · IF 11.6

Natural Matrine-Integrated Pollen Delivery Systems for Allergic Contact Dermatitis Treatment

Yuwei Wang,Lijun Cai,Yuanyuan Zhang,Yan Cong,Yuanjin Zhao

Allergic contact dermatitis (ACD) is an inflammatory dermatitis with a high morbidity and recurrence rate. Scientific attention is focused on the development of safe and comfortable therapeutics of ACD. Herein, we propose a natural matrine-integrated pollen delivery system for the ACD treatment. Sunflower pollens were collected and defatted to serve as adhesive drug carriers for matrine. Specifically, the exquisite porous and hollow structures of the pollen shells can absorb matrine and realize the sustained drug release. Besides, the prickly surface morphology can strongly adhere to the inflamed skin sites, which can prolong the duration of the drug. By utilizing them in an ACD model and an acute pruritus model of mice, we have demonstrated that these matrine-integrated pollen shells can decrease the swelling degree of mice ears and weight loss, down-regulate inflammatory response, and improve the scratching times. These results indicate that our matrine-integrated pollen delivery systems have great potential to serve as natural topical preparations for skin disease therapy.

研究领域: 皮肤病学 · 药物递送 · 生物材料 · 天然产物
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ANALYTICAL LETTERS · 2013 · IF 0.965

Determination of Matrine and Oxymatrine in Sophora Flavescens by Nonaqueous Capillary Electrophoresis-Electrospray Ionization-Ion Trap-Mass Spectrometry

Juan Zhang,Zilin Chen

A simple, rapid, and sensitive nonaqueous capillary electrophoresis-electrospray ionization-ion trap-mass spectrometry (NACE-ESI-IT-MS) method was developed for determination of matrine and oxymatrine in Sophora Flavescens and medicinal preparations. The conditions for NACE separation and MS detection were systematically optimized. The optimum NACE buffer contained 30 mM ammonium acetate, 1% acetic acid, and 15% acetonitrile in methanol and the applied voltage on separation capillary was set at 25 kV. Berberine was selected as internal standard. In order to generate a stable electrospray, a sheath liquid (isopropanol/H2O, 2/1, v/v) was used, which could also boost the flow through the ESI needle. The matrine and oxymatrine solutions were introduced into MS detection by a syringe pump for collecting the MSn spectra to investigate the main fragment ions and its possible cleavage pathways. Both matrine and oxymatrine showed good linearity in the concentration ranges from 0.5 to 400 µg/mL, with linear correlation coefficient R > 0.99 and the limit of detections were 37.5 ng/mL for matrine and 50.0 ng/mL for oxymatrine, respectively. The recoveries at different content of Sophora Flavescens were 98.3%–102.9% for MT and 95.3%–100.6% for OMT, which indicates the reliability of this method.

研究领域: 分析化学 · 药学
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JOURNAL OF FISH DISEASES · 2023 ·Vol. 46 ·期 9 ·977-986 · IF 2.5

In vivo antibacterial activity of medicinal plant Sophora flavescens against Streptococcus agalactiae infection

Fa-Li Zhang,Liu Yang,Wei-Hao He,Ling-Jun Xie,Fei Yang,Ying-Hui Wang,Ai-Guo Huang

Streptococcosis disease caused by Streptococcus agalactiae (Group B Streptococcus, GBS) results in a huge economic loss of tilapia culture. It is urgent to find new antimicrobial agents against streptococcosis. In this study, 20 medicinal plants were evaluated in vitro and in vivo to obtain medicinal plants and potential bioactive compounds against GBS infection. The results showed that the ethanol extracts of 20 medicinal plants had low or no antibacterial properties in vitro, with a minimal inhibitory concentration ≥256 mg/L. Interestingly, in vivo tests showed that 7 medicinal plants could significantly inhibit GBS infection in tilapia, and Sophora flavescens (SF) had the strongest anti-GBS activity in tilapia, reaching 92.68%. SF could significantly reduce the bacterial loads of GBS in different tissues (liver, spleen and brain) of tilapia after treated with different tested concentrations (12.5, 25.0, 50.0 and 100.0 mg/kg) for 24 h. Moreover, 50 mg/kg SF could significantly improve the survival rate of GBS-infected tilapia by inhibiting GBS replication. Furthermore, the expression of antioxidant gene cat , immune-related gene c-type lysozyme and anti-inflammatory cytokine il-10 in liver tissue of GBS-infected tilapia significantly increased after treated with SF for 24 h. Meanwhile, SF significantly reduced the expression of immune-related gene myd88 and pro-inflammatory cytokines il-8 and il-1β in liver tissue of GBS-infected tilapia. The negative and positive models of UPLC-QE-MS, respectively, identified 27 and 57 components of SF. The major components of SF extract in the negative model were α, α-trehalose, DL-malic acid, D- (−)-fructose and xanthohumol, while in the positive model were oxymatrine, formononetin, (−)-maackiain and xanthohumol. Interestingly, oxymatrine and xanthohumol could significantly inhibit GBS infection in tilapia. Taken together, these results suggest that SF can inhibit GBS infection in tilapia, and it has potential for the development of anti-GBS agents.

研究领域: 水产养殖 · 药理学 · 微生物学
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MOLECULES · 2022 ·Vol. 27 ·期 15 ·4974 · IF 4.927

Synthesis of Halopyrazole Matrine Derivatives and Their Insecticidal and Fungicidal Activities

Xingan Cheng,Huiqing He,Fangyun Dong,Chunbao Charles Xu,Hanhui Zhang,Zhanmei Liu,Xiaojing Lv,Yuehua Wu,Xuhong Jiang,Xiangjing Qin

Matrine is a traditional botanical pesticide with a broad-spectrum biological activity that is widely applied in agriculture. Halopyrazole groups are successfully introduced to the C13 of matrine to synthesize eight new derivatives with a yield of 78–87%. The insecticidal activity results show that the introduction of halopyrazole groups can significantly improve the insecticidal activity of matrine onPlutella xylostella,Mythimna separataandSpodoptera frugiperdawith a corrected mortality rate of 100%, which is 25–65% higher than matrine. The fungicidal activity results indicate that derivatives have a high inhibitory effect onCeratobasidium cornigerum,Cibberella sanbinetti,Gibberrlla zeaeandCollectot tichum gloeosporioides. Thereinto, 4-Cl-Pyr-Mat has the best result, with an inhibition rate of 23–33% higher than that of matrine. Therefore, the introduction of halogenated pyrazole groups can improve the agricultural activity of matrine.

研究领域: 植物化学 · 农药科学 · 有机合成
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