JOURNAL OF ETHNOPHARMACOLOGY
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2013
·
IF 2.755
Linling Lu,Dawei Qian,Jianming Guo,Yefei Qian,Boyi Xu,Mei Sha,Jinao Duan
Aim Abelmoschi Corolla is a well-known herbal medicine used for the treatment of chronic renal disease . Flavonoids are the major bioactive ingredients of Abelmoschi Corolla, but some non-flavonoid components also exist in this herb. In order to clarify the influences of non-flavonoid components on the pharmacokinetics profile of the flavonoid fraction from Abelmoschi Corolla (FFA), an investigation was carried out to compare the pharmacokinetic parameters of seven flavonoid components after administration of FFA and after administration of FFA combined with different non-flavonoid fractions. Materials and methods A selective and sensitive UPLC–MS/MS method was established to determine the plasma concentrations of the seven compounds. Sprague-Dawley rats were allocated to four groups which orally administered FFA, FFA combined with macromolecular fraction (FFA–MF), FFA combined with small molecule fraction (FFA–SF) and FFA combined with MF–SF (FFA–MF–SF) with approximately the same dose of FFA. At different time points, the concentration of rutin (1), hyperoside (2), isoquercitrin (3), hibifolin (4), myricetin (5), quercetin-3′- O -glucose (6), quercetin (7) in rat plasma were determined and main pharmacokinetic parameters including T 1/2 , T max , AUC and C max were calculated using the DAS 2.0 software package. The statistical analysis was performed using the Student's t -test with P <0.05 as the level of significance. Results Flavonoids almost had similar pharmacokinetics profile that were rapidly absorbed, reached the peak concentration at 30–60 min in group A, but the pharmacokinetic profiles and parameters of these flavonoids changed when co-administered with non-flavonoid components. It was found that AUC of five flavonoids but not hibifolin and quercetin in group FFA–SF and group FFA–MF–SF increased ( P <0.05) in comparison with group FFA while the tendency was not observed in group FFA–MF. Moreover, seven flavonoids had varying degrees of differences in the pharmacokinetics parameters such as C max , T max and T 1/2 ( P <0.05) in group FFA–MF, FFA–SF and FFA–MF–SF by comparison with group FFA. Conclusion These results indicate that non-flavonoid components could improve the bioavailability and delay the elimination of some flavonoids in rat.
研究领域:
中药学
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药理学
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生物化学
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产品关联
DOI
PubMed
高影响因子
PHYTOCHEMISTRY
·
2024
·
IF 3.2
Xiaojie Fan,Jiaxin Guo,Dongyan Feng,Dahong Li,Huiming Hua
Plants of the Garcinia genus were rich in structurally diverse and naturally bioactive components, while limited studies have been reported for Garcinia pedunculata Roxb. and G. nujiangensis C. Y. Wu & Y. H. Li. Four previously undescribed compounds including three chromones , garpedunchromones A-C ( 1 – 3 ), and one biflavonoid , nujiangbiflavone A ( 14 ), along with fifteen known analogs ( 4 – 13 , 15 – 19 ) were isolated from G. pedunculata and G. nujiangensis . The structures of the isolated compounds were determined based on their HRESIMS data, extensive NMR spectroscopic analyses , and ECD calculations. The chromone derivatives were isolated from Garcinia for the first time. Compound 14 was a rare biflavonoid with C-3─C-6″ linkage. The biological evaluation of these isolates against NO production was conducted in the LPS-induced RAW 264.7 cells, resulting in the identification of a series of potent NO inhibitors, of which garpedunchromone B ( 2 ) was the most active with an IC 50 value of 18.11 ± 0.96 μM. In the network pharmacology studies, the potential targets of compounds and inflammation were obtained from PharmMapper and GeneCards database. GO and KEGG enrichment analysis revealed that the overlapped targets were closely related to the major pathogenic processes linked to inflammation. Garpedunchromone B and proteins binding sites were being predicted.
研究领域:
植物化学
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药理学
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天然产物研究
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2020
·
IF 5.162
Jiali Yang,Ting Zhou,Yueming Jiang,Bao Yang
Prenylated flavonoids are good drug candidates due to multiple biological activities and health benefits. Prenyltransferase is an important enzyme involved in the biosynthesis of prenylated flavonoids. In this work, a flavonoid prenyltransferase (AhPT1) from Artocarpus heterophyllus showed an unexpectedly metal ion-induced specificity to flavonoid substrates. AhPT1 could catalyse 6- C -prenylation of genistein when Mg 2+ serving as cofactor. Its catalytic activity to 6-hydroxyflavone was undetectable. However, when Mn 2+ was used instead of Mg 2+ , 5- C -prenylated 6-hydroxyflavone was generated with a high conversion rate. Mn 2+ altered the regiospecificity of AhPT1 and turned it into a 5- C -prenyltransferase. 2′-Hydroxyl could improve the conversion rate of 6-hydroxyflavone, whereas 3′- or 4′-hydroxyl impaired the catalysis efficiency of AhPT1. NQIFDADID174 and DLTDVEGD305 were active motifs involved in substrate binding and catalysis. Asn166, Asp170, Asp174, Asp298, Asp301 and Asp305 in the active center were critical to the prenylation reaction.
研究领域:
生物化学
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酶学
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药理学
✓ 已验证
DOI
PubMed
高影响因子
BMC Complementary and Alternative Medicine
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2017
·Vol. 17
·期 1
·1-11
·
IF 2.288
Jiang Qian,Li Xican,Tian Yage,Lin Qiaoqi,Xie Hong,Lu Wenbiao,Chi Yuguang,Chen Dongfeng
Background
Mori Fructus and Mori Ramulus are two traditional Chinese herbal medicines from mulberries. The present work explores their beneficial effects on •OH–treated mesenchymal stem cells (MSCs) and discusses possible mechanisms.Methods Lyophilized aqueous extracts of Mori Fructus (LAMF) and Mori Ramulus (LAMR) were prepared and analyzed using HPLC. LAMF and LAMR (along with morin) were further investigated for their effects on •OH-treated MSCs using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl (MTT) assay. The direct antioxidation mechanisms were studied using 2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide (PTIO•)-scavenging, 2,2′-azino-bis (3-ethylbenzo-thiazoline-6-sulfonic acid (ABTS+•)-scavenging and 1,1-diphenyl-2-picryl-hydrazl (DPPH•)-scavenging, as well as Cu2+-reducing and Fe3+-reducing antioxidant power. Finally, the indirect antioxidant mechanism was investigated based on the UV-vis spectra of Fe2+-chelation.Results In each LAMF and LAMR, seven phytophenols were successfully measured by HPLC, including five flavonoids (morin, rutin, astragalin, isoquercitrin and luteolin) and two non-flavonoids (chlorogenic acid and maclurin). MTT assays revealed that LAMF, LAMR and morin could effectively increase the survival of •OH-treated MSCs at 10–100 μg/mL, and could effectively scavenge PTIO• (IC 50 6609.7 ± 756.6, 4286.9 ± 84.9 and 103.4 ± 0.9 μg/mL, respectively), DPPH• (IC 50 208.7 ± 3.0, 97.3 ± 3.1 and 8.2 ± 0.7 μg/mL, respectively) and ABTS+• (IC 50 73.5 ± 5.8, 34.4 ± 0.1 and 4.2 ± 0.2 μg/mL, respectively), and reduce Cu2+ (IC 50 212.5 ± 7.0, 123.2 ± 0.9 and 14.1 ± 0.04 μg/mL, respectively) & Fe3+ (IC 50 277.0 ± 3.1, 191.9 ± 5.2 and 5.0 ± 0.2 μg/mL, respectively). In the Fe2+-chelating assay, the five flavonoids produced much stronger shoulder-peaks than the two non-flavonoids within 420–850 nm.Conclusion
Mori Fructus and Mori Ramulus, can protect MSCs from •OH-induced damage. Such beneficial effects can mainly be attributed to the antioxidant action of phytophenols, which occurs via direct (ROS-scavenging) and indirect mechanism (Fe2+-chelating). The ROS-scavenging mechanism, however, include at least a H+-transfer and an electron-transfer (ET), and possibly includes a hydrogen-atom-transfer (HAT). In the Fe2+-chelating, flavonoids are more effective than non-flavonoids. This can be attributed to several adjacent planar chelating-sites between the 3-OH and 4-C = O, between the 4-C = O and 5-OH, or between the 3′-OH and 4′-OH in flavonoids. Such multiple-Fe2+-chelating reactions cause overlap in the UV-vis absorptions to deepen the complex color, enhance the peak strength, and form shoulder-peaks. By comparison, two non-flavonoids with catechol moiety produce only a weak single peak.
研究领域:
药理学
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细胞生物学
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中药学
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生物化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2018
·
IF 3.115
Hongyan Ma,Qi Huang,Wenshan Qu,Linyuan Li,Min Wang,Shao Li,Fujiang Chu
Ethnopharmacological relevance The dried roots of Sophora flavescens Ait. (Leguminosae) is traditionally used as antipyretic medicine to reduce inflammation. It is well known that alkaloids and flavonoids are the main constituents of S. flavescens . However, the clinical researches and applications of S. flavescens is mainly based on its water-extracted alkaloids, its flavonoids may still remain in residues and have been underused. With development and manufacturing of S. flavescens in recent years, more herb residues are being produced. Since they are typically treated as waste and dumped openly in landfill sites, which can cause pollution, there is a great need to explore these wastes as recyclable resources and increase their added value. To date, whether other bioactive components would be found in the residues of S. flavescens is still unknown. If the extraction method of these active ingredients was established, the residues of S. flavescens could be turned from the harm to a benefit and make great sense of the comprehensive utilization of S. flavescens resources. This study aimed to establish an extraction method of the residues of S. flavescens and investigate the anti-inflammatory effect of it both in vivo and in vitro . Materials and methods Dried S. flavescens were decocted with distilled water firstly, then the residues were powdered and extracted with ethyl acetate by using ultrasonic wave. HPLC was utilized to analyze the chemical constituents of the water extracts of S. flavescens (WSF) and the ethyl acetate extracts of residues of S. flavescens (RSF). In vivo , the anti-inflammatory effect of WSF and RSF were evaluated using the xylene-induced auricle edema, acetic acid-induced peritoneal permeability and carrageenan-induced hind paw edema methods. In vitro, the inhibitory activities of WSF and RSF on NO, TNF-α, IL-6 and MCP-1 production of LPS-treated RAW264.7 cells were measured. Results The major ingredients of RSF were flavonoids, while WSF almost had no flavonoids. In vivo , WSF and RSF (200 mg/kg) could significantly inhibit the edema in the xylene-induced mice auricle edema and carrageenan-induced hind paw edema as well as the peritoneal permeability increased by acetic acid. They can also lower production levels of PGE 2 in inflamed paw tissues. In vitro experimental results showed that RSF (25-100 μg/mL) could significantly inhibit the release of pro-inflammatory cytokines NO, TNF-α, IL-6 and MCP-1 on LPS-induced RAW264.7 cells. The in vitro suppress effect of WSF had no dose-response relationship. Conclusions The residues of S. flavescens had obvious flavonoids with anti-inflammatory activity. This study provided evidence for the reuse of residues from S. flavescens in the food additive , medicine and cosmetic industries.
研究领域:
药理学
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民族药理学
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化学
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DOI
PubMed
高影响因子
ENERGY CONVERSION AND MANAGEMENT
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2022
·
IF 11.533
Tan Li,Kai Miao,Zhigang Zhao,Yuqing Li,Huiyuan Wang,Atsushi Watanabe,Norio Teramae,Kaige Wang
The product distributions of cellulose pyrolysis under different pressures, temperatures, and atmospheres were investigated using a high-pressure micropyrolyzer to clarify the pyrolysis reaction mechanism of cellulose decomposition with hydrogen. EGA-MS results shows that the increase in hydrogen pressure prolonged the second stage of cellulose pyrolysis, which was dominated by decarboxylation. Pyrolysis products of cellulose under helium mainly included levoglucosan, furfural, and acids, while cellulose hydropyrolysis mainly produced C5-C7 ketones, besides small amount of alcohols, aromatics and aliphatic hydrocarbons, and even small amount of phenolics. Carbon yield of ketones was as high as 27.2% from cellulose hydropyrolysis under 2.5 MPa hydrogen and 500 °C. The yield of liquid products and non–condensable hydrocarbons increased with elevated hydrogen pressure. The formation mechanisms of aromatics, phenolics, aliphatic hydrocarbons, aldehydes, ketones, and alcohols under hydrogen atmosphere were discussed. Acetaldehyde was produced by acids through a HDO reaction. C5-C7 chain ketones and cyclic ketones were generated by furfural through HDO and hydrocracking reactions. The Diels–Alder reaction to generate aromatics was enhanced by increasing pyrolysis temperature under hydrogen atmosphere. The reaction network of cellulose hydropyrolysis was also proposed.
研究领域:
化学工程
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能源科学
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DOI
高影响因子
JOURNAL OF CHEMICAL AND ENGINEERING DATA
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2011
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IF 2.089
Xia Gui,ZhiGang Tang,Weiyang Fei
The constant-volume method is used to determine the solubility of CO2 in methanol, ethanol, n-propanol, n-butanol, n-propanol, ethylene glycol, propylene glycol, acetone, 2-butanone, ethylene glycol monomethyl ether, and ethylene glycol monoethyl ether under the pressure of 6 MPa and the temperature variations from (288.15 to 318.15) K in this paper. It is found by contrast that ketones have a greater ability to dissolve CO2 than alcohols, ethers, and glycols, which also indicate that both the carbonyl group and the ether bond in solvents can promote the CO2 absorption, but hydroxyl group will inhibit the CO2 absorption.
研究领域:
化学工程
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环境科学
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产品关联
DOI
高影响因子
Horticulture Research
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2024
·
IF 7.6
Yuan Ziyu,Li Gu,Zhang Huixian,Peng Zhaoxin,Ding Wenyu,Wen Huan,Zhou Hanxin,Zeng Jiwu,Chen Jiajing,Xu Juan
Citrus fruits have abundant flavonoid glycosides (FGs), an important class of natural functional and flavor components. However, there have been few reports about the modification of UDP-glycosyltransferases (UGTs) on flavonoids in citrus. Notably, in flavonoid biosynthesis, 7-O-glucosylation is the initial and essential step of glycosylation prior to the synthesis of flavanone disaccharides, the most abundant and iconic FGs in citrus fruits. Here, based on the accumulation of FGs observed at the very early fruit development stage of two pummelo varieties, we screened six novel flavonoid 7-O-glucosyltransferase genes (7GlcTs) via transcriptomic analysis and then characterized them in vitro. The results revealed that four Cg7GlcTs possess wide catalytic activities towards various flavonoid substrates, with CgUGT89AK1 exhibiting the highest catalytic efficiency. Transient overexpression of CgUGT90A31 and CgUGT89AK1 led to increases in FG synthesis in pummelo leaves. Interestingly, these two genes had conserved sequences and consistent functions across different germplasms. Moreover, CitUGT89AK1 was found to play a role in the response of citrus to Huanglongbing infection by promoting FG production. The findings improve our understanding of flavonoid 7-O-glucosylation by identifying the key genes, and may help improve the benefits of flavonoid biosynthesis for plants and humans in the future.
研究领域:
植物科学
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生物化学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2016
·
IF 3.055
Zhong-Yan Zhou,Li-Yun Huan,Wai-Rong Zhao,Nuo Tang,Yu Jin,Jing-Yi Tang
Ethnopharmacological relevance Spatholobi Caulis is a traditional blood-activating and stasis-dispelling herb medicine, which has been used to treat diseases related to blood stasis syndrome (BSS) by inhibiting platelet aggregation, stimulate hematopoiesis, etc. It has been demonstrated that pro-angiogenesis could improve BSS. However, the pro-angiogenic activity of Spatholobi Caulis was not well elucidated Aim of study To determine the potential pro-angiogenic activity of Spatholobi Caulis and elucidate its underlying mechanism. The active fractions of Spatholobi Caulis were further screened. Material and methods Gelatin precipitation and reversed-phase liquid chromatography (RPLC) were used to purify the methanol extracts of Spatholobi Caulis , respectively. The RPLC was also used to prepare fractions. Total flavonoids of purified methanol extracts of Spatholobi Caulis (PSC) were determined using ultraviolet spectrophotometry. The morphological observation of subintestinal vessel plexus (SIVs) and tyrosine kinase inhibitor II (VRI)-induced intersegmental blood vessels (ISVs) loss in transgenic zebrafish Tg(fli-1a: EGFP)y1 were selected to evaluate the pro-angiogenic activity of PSC in vivo. Cell proliferation by MTT assay and cell migration assay were used to evaluate the pro-angiogenesis effect of PSC in human umbilical vein endothelial cells (HUVECs) in vitro . Both zebrafish and HUVECs were used in screening active fractions of PSC. The mechanism of PSC promoting angiogenesis were studied by real-time PCR in zebrafish and western blotting in HUVECs. Results Co-treatment PSC dramatically rescued VRI-induced ISVs loss in zebrafish embryos in a dose-dependent manner and 80% of the defective vascular recovered at the concentration of 30 μg/ml compared with VRI-only group. PSC also concentration-dependently increased average sprouting number and diameter of SIVs in zebrafish embryo. Real-time PCR assay proved that PSC significantly restored the down regulation of VEGFRs including Flt-1, Kdr and Kdrl induced by VRI in zebrafish (P<0.001). Furthermore, PSC not only promoted proliferation and migration of normal HUVECs but also ameliorated VRI-induced HUVECs cytotoxicity. Western blotting assay showed that co-treatment of PSC increased the expression of VEGFRs and phosphorylation of MAPKs which decreased by VRI treatment. In addition, quality evaluation experiments showed that the content of total flavonoids of PSC reached 56.36% and the main pro-angiogenic fractions of PSC were F3, F4 and F5 both in zebrafish and HUVECs. Conclusions Our data demonstrated that PSC presented pro-angiogenic activity both in zebrafish and HUVECs, and principal pro-angiogenic active components were likely flavonoids. Thus, the current study provided evidence for the clinical usage of Spatholobi Caulis in promoting blood circulation and removing stasis in traditional Chinese medicine (TCM).
研究领域:
民族药理学
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分子生物学
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心血管研究
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DOI
PubMed
高影响因子
Foods
·
2022
·Vol. 11
·期 16
·2527
·
IF 5.561
Ruilian Lai,Chaogui Shen,Xin Feng,Minxia Gao,Yongyan Zhang,Xiaoxia Wei,Yiting Chen,Chunzhen Cheng,Rujian Wu
Canarium albumfruit has great potential to be consumed as a raw material not only for food but also medicine. The diverse active metabolites composition and content ofC. albumfruits greatly affect their pharmacological effects. However, up to now, there has been no report on the global metabolome differences among fruits from distinctC. albumcultivars. In our present study, by using non-targeted metabolomics techniques, we identified 87 DAMs (differentially accumulated metabolites) including 17 types of flavonoids from fruits of four differentC. albumcultivars. KEGG (Kyoto Encyclopedia of Genes and Genomes) pathway enrichment analysis revealed that the flavone and flavonol biosynthesis- and flavonoid biosynthesis-related DAMs were major factors determining their metabolome differences. Comparative transcriptomic analysis revealed that 15 KEGG pathways were significantly enriched by genes of the identified 3655 DEGs (differentially expressed genes) among differentC. albumcultivars. Consistent with the metabolome data, flavonoid biosynthesis-related DEGs, including eight key structural genes (such asFLS,CCoAOMT,CHI,C4H,DFR,LAR, andC3′H, etc.) and several regulatory transcription factor (TF) genes (including 32MYBsand 34bHLHs, etc.), were found to be significantly enriched (p< 0.01). Our study indicated that the differential expression of flavonoid biosynthesis-related genes and accumulation of flavonoids played dominant roles in the various metabolome compositions of fruits from differentC. albumcultivars.Keywords:Canarium album;flavonoid;metabolomics;transcriptomics;gene expression
研究领域:
植物学
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遗传学
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分子生物学
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药理学
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产品关联
DOI
PubMed
高影响因子
IMMUNOPHARMACOLOGY AND IMMUNOTOXICOLOGY
·
2022
·
IF 3.712
Sa-sa Zhang,Yi-jin Wu,Shu Pan,Qi-hai Wang,Wen-gang Chen,Zhong-fang Wang,Jin-ying Xu,Jian Zuo,Qin Yin
Background The first-line anti-rheumatic drug methotrexate (MTX) is used in the combination. Because of the unpredictable adverse reactions, optimization of relevant regimens is necessary and meaningful. This study aimed to study the possible interaction between Securidaca inappendiculate Hassk. Derived xanthones and MTX.Methods We established adjuvant-induced arthritis (AIA) model, which was treated with MTX and MTX + xanthone-rich fraction (XRF). The clinical efficacy was evaluated by histopathological examination, and LC-MS was used to monitor the blood concentration of MTX. Western blotting and immunohistochemistry were used to detect protein expression. In vitro, we assessed the activity of related transporters by cellular uptake assay based on HEK-293T cells.Results Compared with MTX-treated rats, inflammation in the immunized rats in the MTX + XRF group was obvious, indicating that XRF antagonized the anti-rheumatic effect of MTX. Meanwhile, XRF reduced liver and kidney injuries caused by MTX in addition to MTX. Results from immunohistochemical and nappendiculat assays suggested that XRF may reduce uptake of MTX by down-regulating reduced folate carrier 1 (RFC1).Conclusion This study indicated that XRF could reduce the plasma concentration of MTX by inhibiting the expression of RFC1, antagonize the therapeutic effect of MTX on AIA rats, and reduce its oral bioavailability. The combination of S. inappendiculate and MTX should be further optimized to achieve the goal of increasing efficiency and reducing toxicity.
研究领域:
药理学
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风湿病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Foods
·
2023
·Vol. 13
·期 1
·31
·
IF 5.2
Zongjie Li,Yinyin Jin,Xingyu Wang,Liudong Xu,Liyan Teng,Kang Fu,Baoling Li,Yulu Li,Ying Huang,Ning Ma,Feng Cui,Tingting Chai
Intensive aquaculture combatting the decline of large yellow croaker populations can trigger bacterial outbreaks, resulting in extensive antibiotic use. In this study, we screened 5 aquaculture sites in the coastal areas of Zhejiang and identified 17 antibiotics in large yellow croakers using UPLC-MS/MS. The distribution and occurrence of antibiotic pollutants were different in the different tissues of large yellow croakers, being primarily dominated by quinolones. Relatively higher average residue levels of enrofloxacin and ciprofloxacin were detected in the inedible parts, specifically the gills (37.29 μg/kg). Meanwhile, relatively high average residue levels of enrofloxacin and ciprofloxacin were also found in the edible parts, particularly in the muscle (23.18 μg/kg). We observed that the residue levels detected in the swim bladder exceeded the prescribed limit for fish muscle, but there is currently no specific regulatory limit established for this particular tissue. Despite the HI values of enrofloxacin and ciprofloxacin being below 0.01, the health risks should not be disregarded. The findings of this research provide significant practical implications for assessing antibiotic contamination and enhancing the risk management of coastal regions.Keywords:quinolones;large yellow croaker;edible parts;health risk
研究领域:
水产养殖
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环境健康
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食品安全
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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）