Arabian Journal of Chemistry
·
2022
·
IF 6.212
Fei Huang,Xiaoyu Zhang,Wenhui Li,Yuting Zhao,Qixuan Mu,Xinhui Wang,Yuefei Wang
Scutellariae Radix (SR), the dried root of Scutellaria baicalensis Georgia, is a famous Chinese materia medica that has been widely employed. Raw Scutellariae Radix (RSR), steamed Scutellariae Radix (SSR), and wine Scutellariae Radix (WSR) are adopted for use in clinical practice. Because of their easily confused appearance, they are always misused. Aiming at this problem, an ultra performance liquid chromatography coupled with photodiode array detector (UPLC-PDA) method was established to survey misuse of the RSR and the processed SR (SSR and WSR) in the market by employing baicalin (BC), wogonoside (WS), baicalein (BN), and wogonin (WN) as quality indicators. Fortunately, β -glucuronidase, which mediates conversion from flavone glycoside to aglycone, was identified in the RSR samples by the sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) analysis. The significant production of BN and WN was witnessed in the RSR samples, which did not occur in the SSR and WSR samples in virtue of the inactivated β -glucuronidase. Besides, the different capacities of β -glucuronidase were evaluated in the tested samples. In general, we provided the first evidence to scientifically identify RSR from SSR and WSR.
研究领域:
药用植物学
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分析化学
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中医药
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DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2024
·
IF 7.7
Yucheng Yan,Safdar Ali Amur,Hong Liu,Ruoyao Shen,Huaiqing Sun,Yunlin Pei,Chaowan Guo,Hao Liang
With the extensive application of baicalein in the treatment of cardiovascular and cerebrovascular diseases, its clinical and market demand has gradually expanded. But the natural yield of baicalein is very low, and it is mainly prepared by the deglycosylation of baicalin. However, the insolubility of baicalin in water significantly limits the deglycosylation of it under biocatalysis. To make biocatalysis of baicalin more efficient and environmental, a strategy was designed to enhance its water solubility through the solubilization mechanism of endogenous biological macromolecules, and the effect on the activity of glucuronidase was further explored. The results showed that wrapping with Scutellaria baicalensis polysaccharide (SBP) significantly improved the solubility of baicalin in water (the water solubility of baicalin increased by 23 times, BI/SBP = 1/12, w/w ). It was not only contributed to the efficient production of baicalein by one-pot method, but also effectively improved the deglycosylation rate of baicalin (increase by 47.04 % in aqueous solution). With the help of the solubilization of endogenous polysaccharide on baicalin in aqueous solution, a green, low-cost and efficient method (one-pot method) was designed to simultaneously extract and enzymatic hydrolyze baicalin to prepare baicalein. Under the same conditions, the yield of one-pot method is 87.17 %, which was much higher than that of the conventional method (29.38 %). In addition, one-pot method with the aid of endogenous polysaccharide could simply and conveniently prepare aglycone of other insoluble natural flavonoids, which has a wide range of industrial application value.
研究领域:
药理学
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生物技术
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化学工程
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DOI
PubMed
高影响因子
PROCESS BIOCHEMISTRY
·
2021
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IF 3.757
Lingqi Wang,Changyong Cai,Jiajia Liu,Zhijian Tan
To explore convenient and efficient techniques for the extraction and separation of the active ingredients in medicinal plants is still ongoing. As a new class of molten salt, ionic liquids (ILs) are widely used in the extraction of bioactive compounds from plant resources. In this work, the IL-based biphasic system was developed for the extraction and separation of the homologues of baicalin and baicalein from Scutellaria baicalensis Georgi. The IL-water biphasic system is superior to the other organic solvents-water systems for the extraction and separation of baicalin and baicalein. The phase volume ratio of the IL-water biphasic system was studied, and the other influencing parameters of solid–liquid ratio, extraction temperature, extraction time, and ultrasonic time were optimized through the single factor experiments. The results revealed that the extraction yields were 43.3 mg/g and 14.3 mg/g for baicalin (aqueous phase) and baicalein (IL phase), respectively; and the distribution coefficients were 23.8 and 13.7 for baicalin and baicalein, respectively under the optimized conditions. Finally, the IL can be easily recycled and reused by means of its temperature-responsive characteristic. This study provides a green and efficient method for the selective separation of the homologues in natural plant resources.
研究领域:
药用植物学
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分离科学与技术
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绿色化学
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DOI
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2024
·Vol. 25
·期 7
·3654
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IF 4.9
Wencheng Zhao,Huizi Cui,Kaifeng Liu,Xiaotang Yang,Shu Xing,Wannan Li
Type 2 diabetes mellitus (T2DM) is marked by persistent hyperglycemia, insulin resistance, and pancreatic β-cell dysfunction, imposing substantial health burdens and elevating the risk of systemic complications and cardiovascular diseases. While the pathogenesis of diabetes remains elusive, a cyclical relationship between insulin resistance and inflammation is acknowledged, wherein inflammation exacerbates insulin resistance, perpetuating a deleterious cycle. Consequently, anti-inflammatory interventions offer a therapeutic avenue for T2DM management. In this study, a herb called Baikal skullcap, renowned for its repertoire of bioactive compounds with anti-inflammatory potential, is posited as a promising source for novel T2DM therapeutic strategies. Our study probed the anti-diabetic properties of compounds from Baikal skullcap via network pharmacology, molecular docking, and cellular assays, concentrating on their dual modulatory effects on diabetes through Protein Tyrosine Phosphatase 1B (PTP1B) enzyme inhibition and anti-inflammatory actions. We identified the major compounds in Baikal skullcap using liquid chromatography–mass spectrometry (LC–MS), highlighting six flavonoids, including the well-studied baicalein, as potent inhibitors of PTP1B. Furthermore, cellular experiments revealed that baicalin and baicalein exhibited enhanced anti-inflammatory responses compared to the active constituents of licorice, a known anti-inflammatory agent in TCM. Our findings confirmed that baicalin and baicalein mitigate diabetes via two distinct pathways: PTP1B inhibition and anti-inflammatory effects. Additionally, we have identified six flavonoid molecules with substantial potential for drug development, thereby augmenting the T2DM pharmacotherapeutic arsenal and promoting the integration of herb-derived treatments into modern pharmacology.
研究领域:
药理学
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糖尿病研究
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草药医学
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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
Chinese Journal of Natural Medicines
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2021
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IF 3
Dou-Dou XU,Xiao-Ying HOU,Ou WANG,Di WANG,Dan-Ting LI,Si-Yuan QIN,Bo LV,Xiao-Min DAI,Zun-Jian ZHANG,Jian-Bo WAN,Feng-Guo XU
Huang-Qin Decoction (HQD) is a classic prescription for diarrhea in Chinese medicine treatment. Recent studies have demonstrated that HQD and its modified formulation PHY906 could ameliorate irinotecan (CPT-11) induced gastrointestinal (GI) toxicity and enhance its anticancer therapeutic efficacy. Nevertheless, which constituents in HQD are effective is still unclear so far. The study aims to screen out the key bioactive components combination from HQD that could enhance the anticancer effect of CPT-11. First, the potential bioactive constituents were obtained through system pharmacology strategy. Then the bioactivity of each constituent was investigated synthetically from the aspects of NCM460 cell migration, TNF- α release of THP-1-derived macrophage and MTT assay in HCT116 cell. The contribution of each constituent in HQD was evaluated using the bioactive index E i, which taken the content and bioactivity into comprehensive consideration. And then, the most contributing constituents were selected out to form a key-component combination. At last, the bioefficacy of the key-component combination was validated in vitro and in vivo . As a result, a key-component combination (HB4) consisting of four compounds baicalin, baicalein, glycyrrhizic acid and wogonin was screened out. In vitro assessment indicated that HB4 could enhance the effect of CPT-11 on inhibiting cell proliferation and inducing apoptosis in HCT116. Furthermore, the in vivo study confirmed that HB4 and HQD have similar pharmacological activity and could both enhance the antitumor effect of CPT-11 in HCT116 xenograft model. Meanwhile, HB4 could also reduce the CPT-11 induced GI toxicity.
研究领域:
药理学
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肿瘤学
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中医
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DOI
PubMed
高影响因子
JOURNAL OF NANOBIOTECHNOLOGY
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2022
·Vol. 20
·期 1
·1-15
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IF 9.429
Huang Xuemei,Liu Xiaojing,Lin Xiaoyu,Yuan Zhihua,Zhang Yaozhi,Wang Zhijia,Pi Wenmin,Zhao Haoqiang,Lei Haimin,Wang Penglong
Through the self-assembled strategy to improve the clinical efficacy of the existing drugs is the focus of current research. Herbal formula granule is a kind of modern dosage form of traditional Chinese medicine (TCM) which has sprung up in recent decades. However, whether it is equivalent to the TCM decoction that has been used for thousands of years has always been a controversial issue. In this paper, taking the herb pair of Coptidis Rhizoma—Scutellariae Radix and its main component berberine—baicalin as examples, the differences and mechanisms of self-assemblies originated from the co-decoction and physical mixture were studied, respectively. Moreover, the relationship between the morphology and antibacterial effects of self-assemblies was illuminated via multi-technology. Our study revealed that the physical mixture’s morphology of both the herb pair and the phytochemicals was nanofibers (NFs), while their co-decoction’s morphology was nanospheres (NPs). We also found that the antibacterial activity was enhanced with the change of self-assemblies’ morphology after the driving by thermal energy. This might be attributed to that NPs could influence amino acid biosynthesis and metabolism in bacteria. Current study provides a basis that co-decoction maybe beneficial to enhance activity and reasonable use of herbal formula granule in clinic.
研究领域:
中药学
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药理学
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纳米医学
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产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2025
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IF 5.4
Fu-Qiang Shi,Yuan Zhu,Bo-Wen Li,Zi-Yi Guo,Hang Li,Xiao-Li Sun,Qing-Sheng Zhao
To enhance the extraction efficiency of baicalin (BA) from Scutellariae Radix （SR） and improve the solubility, bioactivity and stability of Scutellaria Extract (SE), a glycyrrhizic acid (GA)-assisted green extraction process for BA was developed and optimized. The results demonstrated that GA-assisted extraction significantly elevated BA yield, achieving 1.7-fold higher extraction rates and 2.1-fold higher BA content in the extracts compared to the conventional 70 % ethanol extraction method. Characterization studies confirmed the formation of an inclusion complex (SE-GA) between GA and BA, which markedly improved SE solubility and bioavailability. Notably, SE-GA exhibited reduced cytotoxicity and enhanced antibacterial and antioxidant activities relative to unmodified SE. Stability assessments further revealed superior preservation of bioactive compounds in SE-GA. Mechanistic analysis suggested that SE penetrates the GA cavity, thereby protecting its bioactive components.
研究领域:
药学
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天然产物化学
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绿色化学
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药理学
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分析化学
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产品关联
DOI
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2025
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IF 5.4
Zhen-yan Song,Wen-jing Yu,Yi-jie Jin,Meng-fen Zhou,Chun-xiang He,Ze Li,Jia-wei He,Qi Chen,Ping Li,Yaqiao Yi,Shao-wu Cheng
Ethnopharmacological relevance Derived from the plant Scutellaria baicalensis Georgi, baicalin is a naturally occurring flavonoid, has demonstrated anti-inflammatory, neuroprotective, hypoglycemic, and lipid-lowering properties. While its effects on Alzheimer's disease (AD) or type 2 diabetes mellitus (T2DM) have been studied individually, its therapeutic role in AD comorbid with T2DM remains unclear. Aim of the study This study aims to explore the potential therapeutic mechanisms associated with baicalin through a rat model featuring AD combined with T2DM. Materials and methods A dual-pathology rat model was developed using a streptozotocin (STZ) and a high-fat dietary regimen injections to induce T2DM, followed by intracerebroventricular STZ to induce AD pathology. Behavioral tests, biochemical assays, histological analyses, qPCR, and Western blotting were used to evaluate baicalin's effects. Untargeted metabolomics was applied to profile metabolic alterations, while network pharmacology and molecular docking were integrated to predict key targets and pathways. Finally, cellular thermal shift assay (CETSA) was conducted to validate the direct binding of baicalin to core proteins. Results Baicalin significantly improved cognitive performance, ameliorated glucose and lipid metabolism, and suppressed neuroinflammation in AD-T2DM rats. Metabolomics identified disruptions in energy metabolism, amino acid metabolism, and purine metabolism pathways. Network pharmacology analysis revealed ALDH2, NOS2, GOT1, GPT, and XDH as key targets associated with these metabolic disturbances. Molecular docking demonstrated strong binding affinities between baicalin and the identified targets. qPCR confirmed the regulation of ALDH2 and NOS2 gene expression by baicalin, and CETSA experiments further validated the thermal stabilization of these proteins, supporting direct interactions in vivo. Conclusions Baicalin exerts therapeutic effects by targeting ALDH2 and NOS2 to modulate arginine and proline metabolism and regulate key metabolites such as GABA and L-arginine. This mechanism improves neuronal function and insulin sensitivity, highlighting baicalin as a promising multi-target treatment for AD with T2DM.
研究领域:
药理学
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神经科学
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内分泌学
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代谢组学
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民族药理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
TALANTA
·
2017
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IF 4.162
Zhengkun Xie,Wang Lu,Lingxi Yang,Gaiping Li,Baoxian Ye
Baicalein and baicalin are the major flavonoids found in Scutellariae Radix, an essential herb which has had a presence in traditional Chinese medicine (TCMs) for more than two thousands of years. Owing to their similar characteristics and physiochemical properties, sensitive, it is a great challenge to detect both of them simultaneously. In this work, a novel, facile and sensitive electrochemical method was proposed based on tantalum oxide (Ta 2 O 5 ), niobium oxide (Nb 2 O 5 ) particles and antiseptic chitosan modified carbon paste electrode (Ta 2 O 5 -Nb 2 O 5 @CTS-CPE). Scanning electron microscope (SEM), X-ray diffraction spectroscopy (XRD), Fourier transform infrared spectroscopy (FTIR), cyclic voltammetry (CV) and electrochemical impedance spectrum (EIS) were used to characterize the properties and investigate the electrochemical response of the sensor. The electrochemical behaviors and redox mechanisms of two analytes were investigated at the target electrode. Under the optimum conditions, the highly sensitive and simultaneous determination of baicalein and baicalin was successfully achieved with a linear response range of 0.08–8.0 μM for both of them. The obtained detection limits for baicalein and baicalin were of 0.05 and 0.03 μM (S/N=3), respectively. Furthermore, the proposed sensor displayed high sensitivity, excellent stability and satisfactory results in Scutellariae Radix samples analysis and hydrolysis process analysis of baicalin in vivo .
研究领域:
分析化学
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电化学
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传统中药
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药物分析
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产品关联
DOI
PubMed
高影响因子
PHYTOCHEMICAL ANALYSIS
·
2024
·
IF 3
Kaidi Lv,Chunling Yin,Fang Li,Wenbo Chen,Liuchuang Zhao,Zhimin Liu,Leqian Hu
Introduction Quality evaluation of Huang-qin is significant to ensure its clinical efficacy. Objective This study aims to establish an accurate, rapid and comprehensive Huang-qin quality evaluation method to overcome the time-consuming and laborious shortcomings of traditional herbal medicine quality assessment methods. Methods The contents of baicalin, baicalein and scutellarin in Huang-qin from five different origins were analyzed by FT-IR and NIR spectra combined with multivariate data technology. The quality of Huang-qin from different origins was evaluated by TOPSIS and consistency analysis based on the content of three active ingredients. The correlation between ecological factors and the accumulation of active ingredients was explored. Results Satisfactory prediction results of PLS models were obtained. Relatively, the model based on FT-IR combined with the PLS regression method has higher R 2 and smaller RMSE than the NIR combined with the PLS method. TOPSIS and consistency analysis results showed that the quality of Huang-qin from different geographical origins was significantly different. The results showed that the quality of Huang-qin produced in Shanxi Province was the best among the five origins studied. The results also found that the quality of Huang-qin in different growing areas of the same origin was not completely consistent. The correlation study showed that altitude, sunshine duration and rainfall were the main factors that caused the quality difference of medicinal materials in different geographical origins. Conclusion This study provides a reference for the rapid quantitative analysis of the active components of herbal medicine and the quality evaluation of them.
研究领域:
中药学
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分析化学
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药理学
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产品关联
DOI
PubMed
高影响因子
FUNCTIONAL PLANT BIOLOGY
·
2025
·Vol. 52
·期 10
·
IF 2.7
Simeng Wan,Weiwei Wu,Chunlei Ou,Ying Cao,Xinyun Guo,Hua Liu,Lihua Yao,Hu Su
Copper treatment can lead to the accumulation of reactive oxygen species, alter the cellular redox state in plants, and trigger plant adaptive mechanisms such as changes in gene expression and shifts in secondary metabolism. We investigated the effects of copper treatment on the redox state of Scutellaria baicalensis Georgi, characterized by glutathione (GSH) and oxidized glutathione (GSSG) levels. We also determined the concentrations of baicalin and baicalein, and analyzed the correlation between the redox state and these metabolites. Moreover, we analyzed the activity of glutathione reductase (GR, EC 1.6.4.2) and the expression levels of GR, phenylalanine ammonia lyase (PAL, EC 4.3.1.5) and isochorismate synthase (ICS, EC 5.4.4.2) genes. Results indicated that copper treatment increased GSH concentration at 24 and 48h, and the ratio of GSH:GSSG, and upregulated GR expression. While the baicalin concentration showed a non-significant increase at 24h and 72h, baicalein exhibited a significant decrease at 48h and 72h. The two key genes in the salicylic acid pathway, PAL and ICS, exhibited opposite trends at 24 and 48h after copper treatment, followed by significant decreases in both PAL and ICS at 72h. Our results suggest that plants can mitigate the toxic effects of copper through increasing GSH biosynthesis. Baicalin and baicalein showed varying accumulation patterns in S. baicalensis subjected to different copper treatments.
研究领域:
植物生理学
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分子生物学
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次生代谢
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环境胁迫生物学
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药用植物学
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氧化还原生物学
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产品关联
DOI
PubMed
高影响因子
TOXICOLOGY AND APPLIED PHARMACOLOGY
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2017
·
IF 3.791
Yi Cai,Wanqing Ma,Yichuan Xiao,Bo Wu,Xiaobing Li,Fengrong Liu,Jianhua Qiu,Genshui Zhang
Baicalin is a major flavonoid compound purified from Scutellariae radix , which has been described as an herb in the Chinese Pharmacopoeia. Previous studies have suggested baicalin possessed extensive anti-inflammatory, anti-cancer, anti-viral properties. However, up to known, there have been no reports of safety and toxicity in the rats following oral administration of baicalin. In this present study, we showed the first evidence that treatment of baicalin (400, 800 and 1600 mg/kg/day) induced significantly kidney injury and fibrosis . The collagen synthesis and fibrosis-related protein expression were increased in the kidney of Sprague-Dawley (SD) rats after treatment with high doses of baicalin. We further investigated the potential molecular mechanism of baicalin-mediated renal fibrosis and revealed that baicalin activated the transforming growth factor-β (TGF-β)/Smad signaling pathway in a dose-dependent manner. Moreover, we also observed that baicalin induced Smad3 interaction with transcriptional coactivator p300 accompanying with increment of Smad3 acetylation . Our results may contribute to better understanding of the future pharmacological and toxicological studies of Scutellaria baicalensis Georgi and its active compounds on the human disease.
研究领域:
药理学
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毒理学
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分子生物学
✓ 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）