JOURNAL OF ETHNOPHARMACOLOGY
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2024
·
IF 4.8
Danilo de Souza Costa,Rayssa A. Cajas,Carla Monteiro Leal,Lara S. Aleixo de Carvalho,Lara Cruz de Souza,Lucas Fukui-Silva,Josué de Moraes,Ademar A. Da Silva Filho
Ethnopharmacological relevance Acmella oleracea (L.) R. K. Jansen, commonly referred to as “Jambu”, is a valuable medicinal plant native to the Amazon regions. Inflorescences of A. oleracea is utilized as local anesthetic properties and for its insecticidal, antiparasitic, and anthelmintic attributes. Aims of this study This study aimed to evaluate the in vitro and in vivo antiparasitic properties of A. oleracea extract and spilanthol (SPL) against Schistosoma mansoni . Materials and methods The ethanolic extract of A. oleracea inflorescences (AoE) was prepared, analyzed by HPLC-DAD, and characterized by UHPLC-HRMS/MS. SPL was isolated from AoE by chromatographic fractionation. The antischistosomal properties of AoE and SPL were evaluated in vitro against adult schistosomes and in preclinical assays using murine models of patent S. mansoni infection. Results Through UHPLC-HRMS/MS analysis, 14 alkamides were annotated in AoE. HPLC-DAD analysis of AoE revealed a peak with a substantial relative area of ∼85%, which was isolated and identified as SPL. AoE and SPL caused mortality of adult schistosomes ex vivo , showing EC 50 values of 32.6 μg/mL and 27.8 μM, respectively, without affected Vero cells or Caenorhabditis elegans . In preclinical studies, the oral administration (400 mg/kg) of AoE and SPL resulted in significant reductions in worm burden of 28% and ∼42%, respectively. Additionally, SPL exhibits remarkable effects on oogram, decreasing egg burden and the number of immature eggs by over 80%, while also promoting significant reductions in hepato- and splenomegaly. Conclusions The research underscores the antischistosomal activity of A. oleracea highlighting the potential of SPL as a lead for the development of new schistosomicidal drugs and encouraging further studies to validate the traditional anthelmintic use of A. oleracea inflorescences.
研究领域:
药理学
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寄生虫学
·
药物开发
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Jiang Xin,Junyin Zhang,Caihong Li,Yaling Deng,Yu Yang,Erfang Jishi,Rui Li,Xiu Gu,Kaifeng Hu
This study reports the structural characterization and in vitro antioxidant activity of a novel polysaccharide, PFH-3a from Fritillariae hupehensis bulbus (FHB) with a weight-average molecular weight (Mw) of about 92.34 KDa, which exhibits a unique glycosidic linkage pattern that has not been previously reported in FHB. Structure of PFH-3a was elucidated through NMR spin system assignment based on comprehensive analyses of 1D and 2D NMR spectroscopy, identification of sugar residue types by iterative matching against a self-constructed NMR database containing 1875 diverse sugar residues, monosaccharide composition analysis, 1D 1 H qNMR analysis, and glycosidic linkage determination. It revealed that PFH-3a comprises a backbone of β-D-Xyl p -( 1 →[3, 6 )-β-D-Gal p -( 1 →3, 6 )-β-D-Gal p -(1→] n , with two branches α-L-Ara f -(1→ and α-L-Ara f -(1→5)-α-L-Ara f -(1→ attached to position 3 of the main chain → 3 ,6)-β-D-Gal p -(1→. In vitro bioactivity assays demonstrated that PFH-3a exhibits dose-dependent antioxidant activity, indicating its potential as a natural antioxidant. However, further investigation is needed to explore the in vivo efficacy and the underlying mechanisms.
研究领域:
植物化学
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药理学
·
食品科学
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DOI
PubMed
高影响因子
JOURNAL OF INSECT SCIENCE
·
2014
·
IF 0.921
Wenping Xu,Qingchun Huang,Xiwei Wu,Xiaoqin Yu,Xuexiao Wang,Liming Tao
Midgut α-amylase is an important digestive enzyme involved in larval energy metabolism and carbohydrate assimilation. In this article, the properties of midgut α-amylase from the Oriental armyworm, Mythimna separata (Lepidoptera: Noctuidae), larvae were characterized, and its in vitro responses to chemical inhibitors were also determined. The kinetic parameters Km and Vmax of midgut α-amylase were 0.064 M, 4.81 U mg pro(-1) in phosphate buffer, and 0.128 M, 1.96 U mg pro(-1) in barbiturate-acetate buffer; α-amylase activity linearly increased as starch concentration increased. α-Amylase activity was not influenced by amino acids such as Pro, Met, Try, His, Ala, and Phe but was strongly activated by antioxidants. Reduced glutathione, 1,4-dithiothreitol, β-mercaptoethanol, and ascorbic acid improved the activity of α-amylase about 2.06, 3.46, 3.37, and 6.38 times, respectively, relative to the control. Ethylenediaminetetraacetic acid, sodium dodecyl sulfonate, and N-bromosuccinimide (NBS) strongly inhibited α-amylase. α-, β-, and γ-cyclodextrin were not the preferred substrates for α-amylase. Kinetic analysis showed that IC50 value of NBS against α-amylase was 1.52 (±0.26) µM, and the mode of action of NBS with Ki as 2.53 (0.35) µM was a mixed-type inhibition that indicated a combination of partial competitive and pure noncompetitive inhibition. The midgut α-amylase of armyworm larvae may be a potential target for novel insecticide development and pest control.
研究领域:
昆虫生理学
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酶学
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害虫控制
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生物化学
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分子生物学
✓ 已验证
DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2017
·
IF 4.811
Chun Chen,Qiang Huang,Li-Jun You,Xiong Fu
Three polysaccharides (MFP-1, MFP-2, and MFP-3) were fractioned from mulberry fruits with 30%, 60%, and 90% (v/v) ethanol, respectively. The MFP-1 had the largest molecular weight of 838 kDa, followed by MFP-2 from 49.5 to 163 kDa, and then MFP-3 from 1.41 to 15.30 kDa. The three polysaccharides were composed of arabinose, galactose, glucose, mannose, xylose, and galacturonic acid but with different molar ratio. They also exhibited different surface morphology and thermogravimetric properties. In addition, the impact of the three polysaccharides on the digestion of lipid in a simulated saliva and gastrointestinal tract was investigated. The results indicated MFP-2 had the strongest ability to reduce the rate and extent of lipid digestion. These results have important implications for understanding the influence of polysaccharides on lipid digestion. The effect on retarding lipid digestion within the gastrointestinal tract might be important for the development functional food rich in oil to promote health.
研究领域:
食品科学
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营养学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
SYNTHETIC COMMUNICATIONS
·
2021
·
IF 2.007
Xiaoyun Ma,Daoping Wang,Gang Wei,Qingdi Zhou,Xiuhai Gan
Two series of quinoxaline–chalcone conjugates have been prepared by aldolic condensation and aromatic nucleophilic substitution reaction, and their anticancer activity against three cancer cell lines including benign prostatic hyperplasia epithelial cell (BPH-1), neuron-like rat pheochromocytoma cell line (PC12) and human breast cancer cell line (MCF-7) were evaluated in vitro. All of the synthesized compounds exhibited moderate to good activity against the cancer cell lines selected. Particularly, Compound A5 showed the excellent potent activity against BPH-1 and MCF-7 with IC50 values of 10.4 and 9.1 μM, respectively, which is similar to doxorubicin (14.1 and 9.2 μM, respectively). As well as compound B6 exhibited most excellent activity toward PC12 with IC50 values of 16.4 μM. Compound A10 exhibited 55.4, 36.8 and 54.5 folds higher selectivity for BPH-1, PC12 and MCF-7 cells than for HEK-293 cell, respectively. In addition, theoretical biological activities of compounds A5 and A10 were evaluated by SwissADME.
研究领域:
药物化学
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肿瘤学
·
有机合成
✓ 已验证
产品关联
DOI
高影响因子
CELL BIOCHEMISTRY AND BIOPHYSICS
·
2023
·
IF 2.6
Zheng Yilin,Wang Jun,Chen Haijun,Gao Yu
The effects of ultrasonic parameters and treatment conditions on the in vitro cellular experiments of sonodynamic therapy (SDT) have not been fully studied. Exploring the factors that affect the efficacy of SDT can provide a reference for screening effective sonosensitizers in vitro. The aim of this work is to investigate the factors that affected the SDT effects in cancer cells. Cancer cells in culture plates were exposed to ultrasound and sonosensitizers. The intracellular drug concentration was measured by using flow cytometry and the cell viability was determined by MTT assay. The SDT effects of cancer cells treated with different ultrasonic parameters under the same sonosensitizer concentration were different. The ultrasonic parameters, intracellular drug concentration, drug treatment time, cell amount, and cell status could affect the sonodynamic therapeutic effects. It is necessary to select appropriate ultrasound conditions and optimize the cellular status to make the results of the in vitro cellular experiments more reliable.
研究领域:
肿瘤学
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生物医学工程
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
Biomolecules
·
2019
·Vol. 9
·期 6
·219
·
IF 4.694
Stoyan Dirimanov,Petra Högger
Polyphenols exert beneficial effects in type 2 diabetes mellitus (T2DM). However, their mechanism of action remains largely unknown. Endothelial Akt-kinase plays a key role in the pathogenesis of cardiovascular complications in T2DM and therefore the modulation of its activity is of interest. This work aimed to characterize effects of structurally different polyphenols on Akt-phosphorylation (pAkt) in endothelial cells (Ea.hy926) and to describe structure-activity features. A comprehensive screening via ELISA quantified the effects of 44 polyphenols (10 µM) on pAkt Ser473. The most pronounced inhibitors were luteolin (44 ± 18%), quercetin (36 ± 8%), urolithin A (35 ± 12%), apigenin, fisetin, and resveratrol; (p< 0.01). The results were confirmed by Western blotting and complemented with corresponding experiments in HUVEC cells. A strong positive and statistically significant correlation between the mean inhibitory effects of the tested polyphenols on both Akt-residues Ser473 and Thr308 (r = 0.9478,p= 0.0003) was determined by immunoblotting. Interestingly, the structural characteristics favoring pAkt inhibition partially differed from structural features enhancing the compounds’ antioxidant activity. The present study is the first to quantitatively compare the influence of polyphenols from nine different structural subclasses on pAkt in endothelial cells. These effects might be advantageous in certain T2DM-complications involving over-activation of the Akt-pathway. The suggested molecular mode of action of polyphenols involving Akt-inhibition contributes to understanding their effects on the cellular level.Keywords:Akt/PKB;endothelium;diabetes;polyphenols;in vitro;structure-activity relationships;screening
研究领域:
药理学
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细胞生物学
·
糖尿病研究
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营养科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
LANGMUIR
·
2025
·
IF 3.9
Yifeng Chen,Yiduo Chen,Wenzhong Cao,Jing Wang,Peng Zhang,Jian Ji
Implantable cardiovascular devices have revolutionized the treatment of cardiovascular diseases, yet their long-term functionality without causing thrombosis is a persistent challenge. Although the surface modification of anticoagulant coating has greatly improved the biocompatibility of the devices, its long-term stability in complex physiological environments still remains questionable. Herein, the stability of three anticoagulant hydrogel coatings, poly(2-methacryloyloxyethyl phosphorylcholine) (PMPC), poly(sodium 2-acryloyl-2-methylpropanesulfonate) (PAMPS), and poly(4-styrenesulfonate sodium) (PSS), is studied. The fabrication of these coatings onto device surfaces is validated by using X-ray photoelectron spectroscopy (XPS) and attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy. In vitro anticoagulation assays confirm the coatings’ significant anticoagulant effects. Among all three coatings, the PSS coating demonstrated superior chemical and mechanical stability in the comprehensive tests, showing great potential for improving the long-term anticoagulant performance of implantable cardiovascular devices.
研究领域:
生物医学工程
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材料科学
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心血管医学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF FOOD PROCESSING AND PRESERVATION
·
2015
·Vol. 40
·期 3
·447-452
·
IF 1.159
Jike Lu,Guofeng Gu,Limin Hao,Zenan Jin,Xu Wang
The characteristics and antioxidant activities of C ordyceps sobolifera polysaccharide (CSP) were investigated. Results from high-performance gel filtration chromatography showed that the average molecular weight of CSP was 1.53 × 10 4 kDa, while this polysaccharide was mainly composed of mannose, glucose and galactose in the molar ratio of 1.7:8.9:1 as determined by high-performance liquid chromatography after pre-column derivatization with 1-phenyl-3-methyl-5-pyrazolone. Fourier-transform infrared spectrum of CSP indicated the typical functional groups of polysaccharide. Antioxidant activity results showed that CSP had reducing power (OD700 was 0.87 at 1.5 mg/mL), and it also exhibited scavenging activities on hydroxyl (·OH scavenging rate was 47.6% at 5 mg/mL) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals (scavenging rate was 55.6% at 1 mg/mL) in a concentration-dependent manner. These results indicate that CSP has good in vitro antioxidant activity and can potentially be used for functional foods. Practical Applications C ordyceps sobolifera is a pricy traditional Chinese herb and it has been used in China for a long time. Polysaccharide extracted from C . sobolifera was characterized, and the antioxidant activities of this polysaccharide were investigated. The result may lay the foundation for the development of antioxidant functional foods from C . sobolifera .
研究领域:
食品科学
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生物化学
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产品关联
DOI
高影响因子
Scientific Reports
·
2024
·Vol. 14
·期 1
·1-8
·
IF 3.8
Luo Cheng,Li Xuying,Yan Hongyang,Guo Qitao,Liu Jiarong,Li Yan
Iron oxide nanoparticles (IONPs) have the potential to be utilized in a multitude of fields, including biomedicine. Consequently, the potential health risks associated with their use must be carefully considered. Most biosafety evaluations of IONPs have focused on examining the impact of the material’s distinctive physicochemical attributes. However, the specific attributes of individual cells are frequently disregarded, particularly under the oxidative stress conditions. This may result in an underestimation of potential risk and impede the clinical translation of IONPs. The present study thus sought to evaluate the potential cytotoxicity and underlying mechanisms of IONPs in a pathological state characterized by mild oxidative stress. A cell model of mild oxidative stress was initially established in vitro. Subsequently, a series of indicators, including cell viability, live/dead ratio, mitochondrial membrane potential, and oxidative damage, were measured to assess the cytotoxicity of IONPs. Finally, a series of ferroptosis regulators were used to elucidate the involvement of ferroptosis. Preincubation with IONPs resulted in a significant reduction in cellular viability, morphological degeneration, elevated numbers of dead cells, impaired mitochondrial function, and increased oxidative damage under mild oxidative stress conditions in vitro. The cytotoxic effects of IONPs under mild oxidative stress are largely dependent on ROS and iron ions and are strongly associated with ferroptosis, which is based on the effects of ferroptosis regulators. The present in vitro study indicated that IONPs are toxic to cells under mild oxidative stress, which is linked to ferroptosis.
研究领域:
纳米医学
·
毒理学
·
细胞生物学
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DOI
PubMed
高影响因子
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
·
2020
·
IF 2.69
Min Wang,Jianghao Zhan,Laijun Xu,Yanjun Wang,Dan Lu,Zhen Li,Jiehua Li,Feng Luo,Hong Tan
Polyurethane nanomicelle is a promising functional drug delivery system. In this work, the polyurethane (P3-PU) was synthesized from PLGA1200-PEG1450-PLGA1200 (P3, a thermosensitive and biodegradable triblock copolymer) and L-lysine ester diisocyanate (LDI). Then, reactive benzaldehyde was further imported to terminate P3-PU to obtain benzaldehyde modified polyurethane (P3-PUDA). The micelles, temperature-sensitive P3-PU nanomicelle and P3-PUDA nanomicelle, were systematically investigated, including the size, stability, temperature sensitivity, drug loading and release behavior, cytotoxic on human hepatocytes (L02), and inhibitory effect on human hepatocellular carcinoma cells (HepG2). The results show the thermosensitive behavior of the micelles can be adjusted by the terminal group. The polyurethane micelles with a uniform size between 20 nm and 30 nm showed excellent stability and good biocompatibility to L02 cells. Besides, in vitro experiments showed that Dox-loaded P3-PUDA micelles exhibited faster and higher release rate at 37 °C and better inhibitory effect on HepG2 than the Dox-loaded P3-PU micelles. Moreover, the achieved benzaldehyde modified polyurethanes also provides various possibilities to adjust further to enlarge its applications. Therefore, the polyurethane micelles will have great potential in the field of drug carriers.
研究领域:
生物材料学
·
药剂学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACTA PHARMACOLOGICA SINICA
·
2016
·Vol. 37
·期 7
·941-949
·
IF 3.166
Sun Hui-ping,Su Jing-han,Meng Qing-shuo,Yin Qi,Zhang Zhi-wen,Yu Hai-jun,Zhang Peng-cheng,Wang Si-ling,Li Ya-ping
Aim: To improve the therapeutic efficacy of cancer treatments, combinational therapies based on nanosized drug delivery system (NDDS) has been developed recently. In this study we designed a new NDDS loaded with an anti-metastatic drug silibinin and a photothermal agent indocyanine green (ICG), and investigated its effects on the growth and metastasis of breast cancer cells in vitro . Methods: Silibinin and ICG were self-assembled into PCL lipid nanoparticles (SIPNs). Their physical characteristics including the particle size, zeta potential, morphology and in vitro drug release were examined. 4T1 mammalian breast cancer cells were used to evaluate their cellular internalization, cytotoxicity, and their influences on wound healing, in vitro cell migration and invasion. Results: SIPNs showed a well-defined spherical shape with averaged size of 126.3±0.4 nm and zeta potential of −10.3±0.2 mV. NIR laser irradiation substantially increased the in vitro release of silibinin from the SIPNs (58.3% at the first 8 h, and 97.8% for the total release). Furthermore, NIR laser irradiation markedly increased the uptake of SIPNs into 4T1 cells. Under the NIR laser irradiation, both SIPNs and IPNs (PCL lipid nanoparticles loaded with ICG alone) caused dose-dependent ablation of 4T1 cells. The wound healing, migration and invasion experiments showed that SIPNs exposed to NIR laser irradiation exhibited dramatic in vitro anti-metastasis effects. Conclusion: SIPNs show temperature-sensitive drug release following NIR laser irradiation, which can inhibit the growth and metastasis of breast cancer cells in vitro .
研究领域:
肿瘤学
·
药剂学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）