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| 1 | Anti-SARS-CoV-2 activities in vitro of Shuanghuanglian preparations and bioactive ingredients显示文摘Human infection with severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)causes coronavirus disease 2019(COVID-19)and there is no cure currently.The 3CL protease(3CLpro)is a highly conserved protease which is indispensable for CoVs replication,and is a promising target for development of broad-spectrum antiviral drugs.In this study we investigated the anti-SARS-CoV-2 potential of Shuanghuanglian preparation,a Chinese traditional patent medicine with a long history for treating respiratory tract infection in China.We showed that either the oral liquid of Shuanghuanglian,the lyophilized powder of Shuanghuanglian for injection or their bioactive components dose-dependently inhibited SARS-CoV-23CLpro as well as the replication of SARS-CoV-2 in Vero E6 cells.Baicalin and baicalein,two ingredients of Shuanghuanglian,were characterized as the first noncovalent,nonpeptidomimetic inhibitors of SARS-CoV-23CLpro and exhibited potent antiviral activities in a cell-based system.Remarkably,the binding mode of baicalein with SARS-CoV-23CLpro determined by X-ray protein crystallography was distinctly different from those of known 3CLpro inhibitors.Baicalein was productively ensconced in the core of the substrate-binding pocket by interacting with two catalytic residues,the crucial S1/S2 subsites and the oxyanion loop,acting as a“shield”in front of the catalytic dyad to effectively prevent substrate access to the catalytic dyad within the active site.Overall,this study provides an example for exploring the in vitro potency of Chinese traditional patent medicines and effectively identifying bioactive ingredients toward a specific target,and gains evidence supporting the in vivo studies of Shuanghuanglian oral liquid as well as two natural products for COVID-19 treatment. | Hai-xia Su Sheng Yao Wen-feng Zhao Min-jun Li Jia Liu Wei-juan Shang Hang Xie Chang-qiang Ke Hang-chen Hu Mei-na Gao Kun-qian Yu Hong Liu Jing-shan Shen Wei Tang Lei-ke Zhang Geng-fu Xiao Li Ni Dao-wen Wang Jian-ping Zuo Hua-liang Jiang Fang Bai Yan Wu Yang Ye Ye-chun Xu | 2020 | Acta Pharmacologica Sinica2020，41，9： | 32 |
| 2 | Baicalin prevents LPS-induced activation of TLR4/NF-κB p65 pathway and inflammation in mice via inhibiting the expression of CD14显示文摘Previous studies have shown that baicalin,an active ingredient of the Chinese traditional medicine Huangqin,attenuates LPS-induced inflammation by inhibiting the activation of TLR4/NF-κBp65 pathway,but how it affects this pathway is unknown.It has been shown that CD14 binds directly to LPS and plays an important role in sensitizing the cells to minute quantities of LPS via chaperoning LPS molecules to the TLR4/MD-2 signaling complex.In the present study we investigated the role of CD14 in the anti-inflammatory effects of baicalin in vitro and in vivo.Exposure to LPS(1μg/mL)induced inflammatory responses in RAW264.7 cells,evidenced by marked increases in the expression of MHC II molecules and the secretion of NO and IL-6,and by activation of MyD88/NF-κB p65 signaling pathway,as well as the expression of CD14 and TLR4.These changes were dose-dependently attenuated by pretreatment baicalin(12.5–50μM),but not by baicalin post-treatment.In RAW264.7 cells without LPS stimulation,baicalin dose-dependently inhibit the protein and mRNA expression of CD14,but not TLR4.In RAW264.7 cells with CD14 knockdown,baicalin pretreatment did not prevent inflammatory responses and activation of MyD88/NF-κB p65 pathway induced by high concentrations(1000μg/mL)of LPS.Furthermore,baicalin pretreatment also inhibited the expression of CD14 and activation of MyD88/NF-κB p65 pathway in LPS-induced hepatocyte-derived HepG2 cells and intestinal epithelial-derived HT-29 cells.In mice with intraperitoneal injection of LPS and in DSS-induced UC mice,oral administration of baicalin exerted protective effects by inhibition of CD14 expression and inflammation.Taken together,we demonstrate that baicalin pretreatment prevents LPS-induced inflammation in RAW264.7 cells in CD14-dependent manner.This study supports the therapeutic use of baicalin in preventing the progression of LPS-induced inflammatory diseases. | Ya-jun Fu Bo Xu Shao-wei Huang Xia Luo Xiang-liang Deng Shuang Luo Chang Liu Qing Wang Jin-yan Chen Lian Zhou | 2021 | Acta Pharmacologica Sinica2021，42，1： | 31 |
| 3 | Baicalin induces ferroptosis in bladder cancer cells by downregulating FTH1显示文摘Ferroptosis is a non-apoptotic regulated cell death caused by iron accumulation and subsequent lipid peroxidation.Currently,the therapeutic role of ferroptosis on cancer is gaining increasing interest.Baicalin an active component in Scutellaria baicalensis Georgi with anticancer potential various cancer types;however,the effects of baicalein on bladder cancer and the underlying molecular mechanisms remain largely unknown.In the study,we investigated the effect of baicalin on bladder cancer cells5637 and KU-19-19.As a result,we show baicalin exerted its anticancer activity by inducing apoptosis and cell death in bladder cancer cells.Subsequently,we for the first time demonstrate baicalin-induced ferroptotic cell death in vitro and in vivo,accompanied by reactive oxygen species(ROS) accumulation and intracellular chelate iron enrichment.The ferroptosis inhibitor deferoxamine but not necrostatin-1,chloroquine(CQ),N-acetyl-L-cysteine,L-glutathione reduced,or carbobenzoxy-valyl-alanyl-aspartyl-[O-methyl]-fluoromethylketone(Z-VAD-FMK) rescued baicalin-induced cell death,indicating ferroptosis contributed to baicalin-induced cell death.Mechanistically,we show that ferritin heavy chain1(FTH1) was a key determinant for baicalin-induced ferroptosis.Overexpression of FTH1 abrogated the anticancer effects of baicalin in both 5637 and KU19-19 cells.Taken together,our data for the first time suggest that the natural product baicalin exerts its anticancer activity by inducing FTH1-dependent ferroptosis,which will hopefully provide a prospective compound for bladder cancer treatment. | Na Kong Xiaying Chen Jiao Feng Ting Duan Shuiping Liu Xueni Sun Peng Chen Ting Pan Lili Yan Ting Jin Yu Xiang Quan Gao Chengyong Wen Weirui Ma Wencheng Liu Mingming Zhang Zuyi Yang Wengang Wang Ruonan Zhang Bi Chen Tian Xie Xinbing Sui Wei Tao | 2021 | Acta Pharmaceutica Sinica B2021，11，12： | 23 |
| 4 | Effects of baicalin in CD4 + CD29 + T cell subsets of ulcerative colitis patients显示文摘AIM:To evaluate the role of baicalin in ulcerative colitis(UC) with regard to the CD4+CD29+ T helper cell,its surface markers and serum inflammatory cytokines.METHODS:Flow cytometry was used to detect the percentage of CD4+CD29+ cells in patients with UC.Real time polymerase chain reaction was used to detect expression of GATA-3,forkhead box P3,T-box expressed in T cells(T-bet),and retinoic acid-related orphan nuclear hormone receptor C(RORC).Western blotting was used to analyze expression of nuclear factor-κB(NF-κB) p65,phosphorylation of NF-κB(p-NF-κB) p65,STAT4,p-STAT4,STAT6 and p-STAT6.The concentrations of interferon-γ(IFN-γ),interleukin(IL)-4,IL-5,IL-6,IL-10 and TGF-β in serum were determined by ELISA assay.RESULTS:The percentages of CD4+CD29+ T cells were lower in treatment with 40 and 20 μmol/L baicalin than in the treatment of no baicalin.Treatment with 40 or 20 μmol/L baicalin significantly upregulated expression of IL-4,TGF-β1 and IL-10,increased p-STAT6/STAT6 ratio,but downregulated expression of IFN-γ,IL-5,IL-6,RORC,Foxp3 and T-bet,and decreased ratios of T-bet/GATA-3,p-STAT4/STAT4 and p-NF-κB/NF-κB compared to the treatment of no baicalin.CONCLUSION:The results indicate that baicalin regulates immune balance and relieves the ulcerative colitis-induced inflammation reaction by promoting proliferation of CD4+CD29+ cells and modulating immunosuppressive pathways. | Feng-Yan Yu Shao-Gang Huang Hai-Yan Zhang Hua Ye Hong-Gang Chi Ying Zou Ru-Xi Lv Xue-Bao Zheng | 2014 | World Journal of Gastroenterology2014，20，41： | 18 |
| 5 | Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin显示文摘The aim of this study was to develop a formulation to improve the oral absorption of baicalin(BA)by combining a phospholipid complex(PC)and self-emulsifying microemulsion drug delivery system(SMEDDS),termed BA–PC–SMEDDS.BA–PC was prepared by a solvent evaporation method and evaluated by complexation percentage(CP).The physicochemical properties of BA–PC were determined.The synergistic effect of PC and SMEDDS on permeation of BA was studied in vitro with Caco-2 cells and in situ with a single pass intestinal perfusion model.The improved bioavailability of BA in BA–PC–SMEDDS was confirmed in an in vivo rat model.The CP of BA–PC reached 100%when the molar ratio of drug to phospholipid(PP)was Z1:1.The solubility of BA–PC increased in both water and octanol,and the log P o/w of BA–PC was increased significantly.BA–PC–SMEDDS could be dispersed more evenly in water,compared to BA and BA–PC.Both the Caco-2 cell uptake and single-pass intestinal perfusion models illustrated that transport of BA in BA–PC was lower than that of free BA,while improved significantly in BA–PC–SMEDDS.The relative bioavailability of BA–PC(1:2)–SMEDDS was 220.37%.The combination system of PC and SMEDDS had a synergistic effect on improving the oral absorption of BA. | Huiyi Wu Xiaoying Long Fei Yuan Li Chen Sujing Pan Yunjun Liu Yoshiko Stowell Xiaoling Li | 2014 | Acta Pharmaceutica Sinica B2014，4，3： | 14 |
| 6 | Pharmacokinetic Effects of Baicalin on Cerebral Ischemia-reperfusion after iv Administration in Rats显示文摘Objective To investigate the pharmacokinetic effects of baicalin on cerebral ischemia-reperfusion (I/R) after iv administration in rats. Methods The cerebral I/R rats were induced by occluding the bilateral carotid arteries of normal rats for 2 h, followed by reperfusion. The resultant animals were immediately iv administrated with baicalin (90 mg/kg), whilst the same dose of baicalin was injected to the normal rats. Plasma samples were collected at different time to construct pharmacokinetic profiles by plotting drug concentration vs time. Quantification of baicalin in rat plasma was achieved using a simple and rapid HPLC method. Results In normal rats, the major parameters of distribution half-life, elimination half-life, area under the plasma concentration-time (AUC), apparent volume of distribution (Vd), and clearance (CL), estimated by an open two-compartmental model, were 0.8868 min, 26.0968 min, 149.6204 mg/min·L, 4.765 L/kg, and 0.5776 L/ kg·min), respectively. However, in I/R rats, the corresponding parameters were 2.084 min, 34.4998 min, 260.0188 μg·min/L, 5.9376 L/kg, and 0.334 L/(kg·min), respectively. Conclusion The cerebral I/R could significantly increase AUC and Vd values, decrease CL values, and prolong the terminal half-life of baicalin. These findings suggest that the injuries of I/R could play an important role in pharmacokinetic process of baicalin. | Shu-wei MA Ming ZHAO Hong-xia LIU Li-yan WANG Xian-tao ZHANG | 2012 | Chinese Herbal Medicines2012，4，1： | 13 |
| 7 | Baicalin extracted from Huangqin(Radix Scutellariae Baicalensis) induces apoptosis in gastric cancer cells by regulating B cell lymphoma(Bcl-2)/Bcl-2-associated X protein and activating caspase-3 and caspase-9显示文摘OBJECTIVE:To evaluate the effects of baicalin in human gastric cancer cells, including apoptosis-inducing effects, and to investigate its underlying mechanisms of action.METHODS:Cell proliferation and apoptosis assays were performed to investigate the anti-proliferation effects of baicalin in human gastric cancer BGC-823 and MGC-803 cells.Real time-quantitative polymerase chain reaction and Western blotting analysis were performed to elucidate the molecular mechanisms underlying the anti-tumor properties of baicalin.RESULTS:In BGC-823 and MGC-803 gastric cancer cells treated with 80, 120, and 160 μmol/L baicalin for 48 h, a 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide assay showed that baicalin significantly inhibited cell proliferation in a dose-dependent manner, while flow cytometric analysis demonstrated that baicalin could induce apoptosis, also in a dose-dependent manner.Moreover, baicalin up-regulated the expression of caspase-3, caspase-9, and B cell lymphoma(Bcl-2)-associated X protein and down-regulated the expression of Bcl-2 at both the m RNA and protein level.CONCLUSION:Baicalin has potential as a therapeutic agent for gastric cancer by inducing apoptosis in cancer cells. | Wang Hongwei Li Hailong Chen Fengqin Luo Jun Gu Jing Wang Huping Wu Hongyan Xu Yan | 2017 | Journal of Traditional Chinese Medicine2017，37，2： | 13 |
| 8 | Baicalin attenuates blood-spinal cord barrier disruption and apoptosis through PI3K/Akt signaling pathway after spinal cord injury显示文摘Baicalin is a natural active ingredient isolated from Scutellariae Radix that can cross the blood-brain barrier and exhibits neuroprotective effects on multiple central nervous system diseases.However,the mechanism behind the neuroprotective effects remains unclear.In this study,rat models of spinal cord injury were established using a modified Allen's impact method and then treated with intraperitoneal injection of Baicalin.The results revealed that Baicalin greatly increased the Basso,Beattie,Bresnahan Locomotor Rating Scale score,reduced blood-spinal cord barrier permeability,decreased the expression of Bax,Caspase-3,and nuclear factorκB,increased the expression of Bcl-2,and reduced neuronal apoptosis and pathological spinal cord injury.SH-SY5 Y cell models of excitotoxicity were established by application of 10 m M glutamate for 12 hours and then treated with 40μM Baicalin for 48 hours to investigate the mechanism of action of Baicalin.The results showed that Baicalin reversed tight junction protein expression tendencies(occludin and ZO-1)and apoptosis-related protein expression(Bax,Bcl-2,Caspase-3,and nuclear factor-κB),and also led to up-regulation of PI3 K and Akt phosphorylation.These effects on Bax,Bcl-2,and Caspase-3 were blocked by pretreatment with the PI3 K inhibitor LY294002.These findings suggest that Baicalin can inhibit bloodspinal cord barrier permeability after spinal cord injury and reduce neuronal apoptosis,possibly by activating the PI3 K/Akt signaling pathway.This study was approved by Animal Ethics Committee of Xi'an Jiaotong University on March 6,2014. | Rui Zhao Xue Wu Xue-Yuan Bi Hao Yang Qian Zhang | 2022 | Neural Regeneration Research2022，17，5： | 9 |
| 9 | Nerve protective effect of Baicalin on newborn HIBD rats显示文摘Objetive:To investigate the nerve protective effect and mechanism of baicalin on newborn rats with hypoxic ischemic brain damage(HIBD).Methods:A total of 64 SD newborn rats were randomlu divided into control group.model group.nerve growth factor group and baicalin group.with 16 in each group.Left carotid artery ligation method was adopted to establish the HIBD model except fou in control group,which was treatde with intraperitoneal injection of salin e10mL/kg for 3 d.After oxygen recovery on hypoxia ischemia rats.intraperitoneal injectionof salin 10mL/kg was adopted in model group for 3 d.Intraperitoneal injection of nerve growth factor injection50μg/kg per day was adopted in nerve growth factor group for 3 d:intraperitoneal injection of radix scutellariae 16mg/kg per day was adopted in baicalin group for 3 d after modeeling.Four rats of each group were sacrificed at Day 1,2,3,7 for microscopic observation of pathological morphological changes in brain tissus aften HE staining,S-P immunohistochemical method was used for observation of Fas and FasL expression in brain cells.Results:Neat structure of cells was observed in control group;edema cells in disordered arrangement was observed in model group,with some cells necrosis and cavity change;tissue injury in nerve growth factor group and baicalin group was significantly lighter than that in model group;Fas and FasL expression in model group,nerve growth factor group and baicalin group were significantiy higher than that in control group at different time points(P<0.05):Fas and FasL expression in nerve growth factor group and baicalin group were significantly lower than that in model group at different time points(P<0.05):There was no statistical diggerence of Fas,FasL expression at each time point between nerve growth factor group and baicalin group(P>0.05).Conclusions:Baicalin can reduce expression of Fas and FasL in HIBD rats,inhibit apoptosis of nerve cells,thus achieve the protective effect on HIBD rat nerves. | Xue-Mei Liu Yi Feng Ai-Min Li | 2014 | Asian Pacific Journal of Tropical Medicine2014，7，10： | 9 |
| 10 | Baicalin Reduces Early Brain Injury after Subarachnoid Hemorrhage in Rats显示文摘Objective: To evaluate the effect of baicalin on subarachnoid hemorrhage(SAH) in rats and explore the potential mechanisms. Methods: Sprague-Dawley rats underwent experimental SAH and received treatment with baicalin at 10 or 50 mg/kg after 2 and 12 h of SAH. Neurological scores, brain water content, Evans-blue extravasation, and levels of glutathione peroxidase(GSH-Px), superoxide dismutase(SOD), myeloperoxidase(MPO), and malondialdehyde(MDA) were measured 24 h after SAH. Expression of nuclear factor erythroid-related factor 2(Nrf2), NAD(P)H: quinone oxidoreductase 1(NQO1), matrix metalloproteinase-9(MMP-9), aquaporin 4(AQP4), occludin, and zonulaoccludens-1(ZO-1) were detected in the brain by Western blot. Heme oxygenase-1(HO-1) was detected by quantitative polymerase chain reaction, and tumor necrosis factor-α(TNF-α) and interleukin-1β(IL-1β) were assessed by enzyme-linked immunosorbent assay. Results: Baicalin attenuated EBI 24 h after SAH in rats(P<0.05). Baicalin elevated neurological scores, GSH-Px, SOD, and increased the expression of Nrf2, NQO1, HO-1, occludin, and ZO-1 in SAH rats(P<0.05 or P<0.01). Baicalin reduced MPO, MDA, and the expression of MMP-9, AQP4, TNF-α, and IL-1β(P<0.05 or P<0.01). Conclusion: Baicalin reduced SAH-induced EBI, partially via activation of the Nrf2/HO-1 pathway and inhibition of MMP-9 and AQP4. | ZHANG Hua-bin TU Xian-kun SONG Shi-wei LIANG Ri-sheng SHI Song-sheng | 2020 | Chinese Journal of Integrative Medicine2020，26，7： | 5 |
| 11 | Pharmacokinetic Study of Baicalein and Its Major Metabolites after iv Administration in Dogs显示文摘Objective To develop and validate a simple,rapid,sensitive,and reproducible HPLC method for simultaneous determination of baicalein and its metabolite baicalin in dog plasma and for the subsequent pharmacokinetic study after iv administration to dogs.Methods An accurate and reproducible HPLC-UV method was developed and validated for simultaneous determination of baicalein and baicalin in dog plasma,using luteolin as internal standard.The analytes were separated by an Agilent Zorbax SB-C18 column(250 mm × 4.6 mm,5 μm) and the column temperature was maintained at 40 ℃.The mobile phase was a binary mixture of acetonitrile and water(27:73) ,containing 0.05% phosphoric acid in water,with a flow rate of 1.0 mL/min.The UV detector was set at 276 nm.Results Linear relationships were validated over the range of 0.05-25 μg/mL for baicalein and 0.05-20 μg/mL for baicalin.The intra-and inter-day precision values for all samples were within 8.0%,using relative standard deviation.This method was successfully applied to the pharmacokinetic studies in dogs after iv administration of baicalein.Baicalein was converted to baicalin quickly.Cmax values were 21.13 μg/mL at 0.05 h for baicalein and 1.57 μg/mL at 0.5 h for baicalin,areas under the plasma concentration-time curve were 4.97 h·μg/mL for baicalein and 0.63 h·μg/mL for baicalin,and the elimination half-life is 0.50 h for baicalein and 0.75 h for baicalin,respectively.Conclusion The method is able and sufficient to be used in drug metabolism and pharmacokinetic studies of baicalein. | TIAN Shuo1,DU Li-da2,WANG Shou-bao1,HE Guo-rong1,YANG Tao1,LI Xiao-xiu1,GUO Jing1,DU Guan-hua1 1.National Centre for Pharmaceutical Screening,Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China 2.School of Pharmacy,China Pharmaceutical University,Nanjing 210009,China | 2011 | Chinese Herbal Medicines2011，3，3： | 5 |
| 12 | Study on Targeting and in vitro Anti-oxidation of Baicalin Solid Lipid Nanoparticles显示文摘Objective To prepare liver-targeted baicalin solid lipid nanoparticles(BSLNs) and to study their in vitro anti-oxidative activity.Methods BSLNs were prepared by emulsification ultrasonic dispersion method and characterized by transmission electron microscopy and laser particle size distribution;The tissue in vivo distribution was detected by pharmacokinetics;In vitro anti-superoxide dismutase(SOD) activity and reduction capacity of BSLNs were determined;The ability of removing hydroxyl radical was determined by phenanthroline-Fe2+ oxidation.Results The best prescription was baicalin-soybean lecithin-glyceryl monostearate-poloxamer 188(1:5:15:30);The encapsulation efficiency and drug loading were 84.7% and 5.65%,respectively,mean size of particles was(68.6 ± 8) nm,Zeta potential was 22.13 mV;The in vitro anti-oxidant results showed that BSLNs had a significant inhibitory effect on SOD and a strong reducing capacity as well as a removing hydroxide radical ability.The targeting rate of BSLNs was 6.931 for liver.Conclusion The results demonstrate that BSLNs could enhance the liver targeting ability and in vitro anti-oxidative activity significantly. | MIYAMURA Mitsuhiko YOKOTA Junko YOSHIOKA Saburo | 2012 | Chinese Herbal Medicines2012，4，4： | 4 |
| 13 | Pathological changes in multiple organs of rats with severe acute pancreatitis treated by baicalin and octreotide显示文摘BACKGROUND:Severe acute pancreatitis(SAP)features fatal pathogenetic conditions and high mortality rate.The study of SAP complicated with multiple organ injuries is of important significance.In this study,we explored the protective effect of baicalin on multiple organs of SAP rats and compared it with that of octreotide through light and electron microscopic observations of the pathological changes. METHODS:The improved Aho method was used to prepare SAP rat models.These rats were then randomly divided into a sham-operated group(n=45),a model control group(n=45), baicalin-treated group(n=45)and octreotide-treated group (n=45).Based on the difference in time points after operation, these groups were subdivided into 3,6 and 12 hour subgroups (n=15).At the corresponding time point after operation,the mortality rate of rats was recorded,and then the rats were humanely killed to take samples of multiple organs that were subsequently examined for pathological changes under light and electron microscopy. RESULTS:At 12 hours after operation,the mortality rate of rats in the baicalin-and octreotide-treated groups was lower than that in the model control group(P<0.05).Compared to the model control group,the pathological changes and pathological scores in the baicalin-and octreotide-treated groups were mitigated and relieved to varying degrees.The pathological changes under electron microscopy were also improved.CONCLUSIONS:Both baicalin and octreotide show good protective effects on multiple organs of SAP rats.Baicalin as a new drug has good prospects in the treatment of SAP. | Zhang, Xi-Ping Tian, Hua Wu, Di-Jiong Feng, Guang-Hua Chen, Li Zhang, Jie Xu, Ru-Jun Cai, Yang Ju, Tong-Fa Xie, Qi | 2009 | Hepatobiliary & Pancreatic Diseases International2009，8，1： | 4 |
| 14 | Injectable baicalin/F127 hydrogel with antioxidant activity for enhanced wound healing显示文摘Baicalin,extracted from traditional Chinese medicine Scutellaria baicalensis Georg,possesses multiple pharmacological activities and has great potential for chronic skin wound repair.However,the poor solubility and lack of suitable vehicles greatly limit its further application.Herein,we proposed a convenient and robust strategy,employing PBS solution as solvent,to enhance the solubility of baicalin.Furthermore,we constructed injectable baicalin/F127 hydrogels to study their application in skin wound treatment.The composition and temperature sensitivity of baicalin/Pluronic®F-127 hydrogels were confirmed by FTIR and rheological testing,respectively.In vitro release measurement indicated that the first order model was best fitted with the release profile of baicalin from hydrogel matrix.Besides,MTT assay,AO/EO staining assay as well as hemolytic activity test revealed the excellent cytocompatibility of baicalin/F127 hydrogels.Antioxidant activity assay demonstrated the cytoprotective activity of baicalin/F127 hydrogels against reactive oxygen species(ROS).Furthermore,the in vivo experiments exhibited the ability of baicalin/F127 hydrogel to accelerate wound healing.In conclusion,this novel injectable baicalin/F127 hydrogel should have bright application for chronic wound treatment. | Guiting Liu Ziting Bao Jun Wu | 2020 | Chinese Chemical Letters2020，31，7： | 4 |
| 15 | Pharmacokinetics and brain distribution differences of baicalin in rat underlying the effect of Panax notoginsenosides after intravenous administration显示文摘Baicalin(BA) is the most well-known flavonoid present in Radix Scutellariae. The aim of this study was to explore whether the pharmacokinetic behavior of BA in rat brain can be affected by Panax notoginsenosides(PNS), and to assess the possible mechanism for the observed effects. Specific HPLC and HPLC/MS/MS methods were developed and validated for the determination of BA in the rat plasma and brain using carbamazepine as an internal standard. BA was found to enter rat brain quickly after a single intravenous dose. When co-administered with PNS, clearance(CL) of BA from rat plasma decreased by 50.00%, while the area under the curve AUC0-t and AUC0-∞ increased 94.69% and 87.68%, respectively. On the other hand, some pharmacokinetic parameters of BA in rat brain had obvious differences after PNS was administered, such as an increase in Tmax from 5 min to 15 min, an increase in AUC0-t and AUC0-∞ by 42.75% and 29.39%, respectively, as well as a decrease in CL by 27.95%. Together, these results indicate that PNS can decrease the elimination rate of BA from rat plasma, promote the penetration of BA into rat brain, increase the concentration and slow down the elimination of BA from rat brain. The data provide important information that compatibility with PNS can promote the consequent effects of BA for the treatment of encephalopathy. | YANG Yan-Fang LI Zhi XIN Wen-Feng WANG Yong-Yan ZHANG Wen-Sheng | 2014 | Chinese Journal of Natural Medicines2014，12，8： | 3 |
| 16 | Baicalin inhibits inflammation of lipopolysaccharide-induced acute lung injury via toll like receptor-4/myeloid differentiation primary response 88/nuclear factor-kappa B signaling pathway显示文摘OBJECTIVE:To explore the effect and mechanism of baicalin in the treatment of acute lung injury(ALI)by in vivo and in vitro experiments.METHODS:ALI was induced by instilling 10 mg/m L lipopolysaccharide(LPS)into the airway of rats.Different doses of baicalin(50 and 100 mg·kg^(-1)·d^(-1 ))were administered by gavage one day before modeling.RESULTS:Baicalin significantly reduced the permeability of the alveolocapillary membrane,alleviated tissue injury and inflammatory infiltration,and inhibited the secretion of inflammatory factors and the infiltration of neutrophils.The decline in these inflammations was related to the inhibition of the toll like receptor-4(TLR4)/myeloid differentiation factor 88(My D88)/nuclear factor-kappa B(NF-κB)/nod-like receptor pyrin containing 3(NLRP3)signaling pathway and the mitogen-activated protein kinase(MAPK)signaling pathway.CONCLUSIONS:Baicalin inhibits the secretion of inflammatory factors by inhibiting the TLR4-My D88-NF-κB/NLRP3 pathway and the MAPK signaling pathway.Thus,it reduces lung bronchial epithelial layer,alveolar damage,and pulmonary edema as detected in the in vivo and in vitro experiments.Therefore,baicalin may be a potential preventive and therapeutic drug for ALI. | ZHU Changle FENG Cuiling FENG Feng Yao Xiaoqin WANG Guishu SHI Liangtian ZHENG Jiakun | 2022 | Journal of Traditional Chinese Medicine2022，42，2： | 3 |
| 17 | Baicalin treatment regulates hyperactivity of HPA axis and alters SIRT1 related inflammation in the hypothalamus in a model of depression显示文摘OBJECTIVE Hyperactivityof hypothalamic-pituitary-adrenal(HPA) axis is an important aetiological risk factor for the development of depression. Previous studies have demonstrated that the phenolic monomer baicalin has antidepressant-like effects and decreases serum corticosterone levels.However,the mechanism by which baicalin regulates hyperactivity of HPA axis remains unclear. This work aimed to investigate the effects of baicalin on hyperactivity of HPA axis using the olfactory bulbectomised(OBX) rat model of depression. METHODS Animals were anaesthetised with 10% chloral hydrate(3.3 mL·kg^(-1),ip). Using disinfected surgical equipment,the skull covering the olfactory bulbs was exposed by a midline incision. Two burr holes(2 mm diameter) were drilled 8 mm anterior to the bregma and 2 mm lateral to the midline. Both olfactory bulbs were aspirated and the holes filled with glass ionomer cement. The scalp was sutured closed. Sham-operated rats underwent every surgical procedure except the aspiration of the bulbs. The animals received penicillin(8×10~5U) intramuscularly(0.2 mL/300 g) once per day for 3 d post-surgery to prevent infection,and were subsequently housed alone in polypropylene cages. The experiments continued after 14 d of rehabilitation. The following groups were used for experiments: sham-operated(underwent surgical procedure without aspiratedolfactory bulbs and administration of vehicle only),OBX-model(underwent every surgical procedure and administration of vehicle only),OBX-amitriptyline treated(10 mg·kg^(-1)),and OBX-baicalin treatment(20 and 40 mg·kg^(-1)). Amitriptyline and baicalin were dissolved in physiological saline. RESULTS We examined how baicalin altered OBX-induced changes in serum glucocorticoid level as wel as inflammatory responses,sirtuin 1(SIRT1) expression,and p65 acetylation in the hypothalamus. Similar experiments were performed to analyse the effects of baicalin on lipopolysaccharide-induced inflammatory responses inhypothalamus. CONCLUSION Our results indicate that activation of the SIRT1 in the hypothalamus contributes to hyperactivity of HPA axis,which can be alleviated by baicalin. | YU Hai-yang ZENG Min-jie FU Qiang MA Shi-ping | 2017 | 中国药理学与毒理学杂志2017，31，5： | 2 |
| 18 | Role of baicalin as a potential therapeutic agent in hepatobiliary and gastrointestinal disorders:A review显示文摘Baicalin is a natural bioactive compound derived from Scutellaria baicalensis,which is extensively used in traditional Chinese medicine.A literature survey demonstrated the broad spectrum of health benefits of baicalin such as antioxidant,anticancer,anti-inflammatory,antimicrobial,cardio-protective,hepatoprotective,renal protective,and neuroprotective properties.Baicalin is hydrolyzed to its metabolite baicalein by the action of gut microbiota,which is further reconverted to baicalin via phase 2 metabolism in the liver.Many studies have suggested that baicalin exhibits therapeutic potential against several types of hepatic disorders including hepatic fibrosis,xenobiotic-induced liver injury,fatty liver disease,viral hepatitis,cholestasis,ulcerative colitis,hepatocellular and colorectal cancer.During in vitro and in vivo examinations,it has been observed that baicalin showed a protective role against liver and gut-associated abnormalities by modifying several signaling pathways such as nuclear factor-kappa B,transforming growth factor beta 1/SMAD3,sirtuin 1,p38/mitogen-activated protein kinase/Janus kinase,and calcium/calmodulin-dependent protein kinase kinaseβ/adenosine monophosphate-activated protein kinase/acetyl-coenzyme A carboxylase pathways.Furthermore,baicalin also regulates the expression of fibrotic genes such as smooth muscle actin,connective tissue growth factor,β-catenin,and inflammatory cytokines such as interferon gamma,interleukin-6(IL-6),tumor necrosis factor-alpha,and IL-1β,and attenuates the production of apoptotic proteins such as caspase-3,caspase-9 and B-cell lymphoma 2.However,due to its low solubility and poor bioavailability,widespread therapeutic applications of baicalin still remain a challenge.This review summarized the hepatic and gastrointestinal protective attributes of baicalin with an emphasis on the molecular mechanisms that regulate the interaction of baicalin with the gut microbiota. | Risha Ganguly Ashutosh Gupta Abhay K Pandey | 2022 | World Journal of Gastroenterology2022，28，26： | 2 |
| 19 | High-throughput RNA sequencing reveals the anti-inflammatory mechanism of baicalin on Propionibacterium acnes-induced acne in rabbits显示文摘Objective:Propionibacterium acnes(P.acnes)plays an important role in the development of acne,an inflammatory skin disease with a high-incidence.In this study,we used high-throughput RNA sequencing(RNA-seq)to reveal the anti-inflammatory mechanism of baicalin on P.acnes-induced acne in rabbits.Methods:The Kligman method was used to induce acne in the ears of New Zealand rabbits.The effect of baicalin on the acne model was evaluated by the number of acne lesions and hematoxylin and eosin(H&E)staining of acne tissues.Enzyme-linked immunoabsorbent assay was used to measure the protein expression levels of tumor necrosis factor a(TNFA),interleukin-1 b(IL1B),IL6,and IL8 in the serum of rabbits.RNA-seq was performed to investigate the mechanism of anti-inflammatory activities of baicalin on acne.Immunohistochemical analysis and Western blot were used to validate the expression levels of related proteins in acne tissues.Results:Baicalin treatment significantly reduced the number of acne lesions and lesions of the ear as well as levels of serum inflammatory cytokines.RNA-seq data showed that baicalin treatment globally suppressed inflammation,especially the TNF signaling pathway and Staphylococcus aureus infection pathway,in the rabbit acne model.Conclusion: Baicalin effectively ameliorates P. acnes-induced acne in rabbits by suppressingthe inflammatory response in rabbits. | Xingzhe Yang Guangrui Huang Leiming You Honghao Sheng Yuxiu Sun Yuyin Feng Qingyi Lu Anlong Xu | 2019 | Journal of Traditional Chinese Medical Sciences2019，6，3： | 2 |
| 20 | Baicalin provides protection against fluoxetine-induced hepatotoxicity by modulation of oxidative stress and inflammation显示文摘BACKGROUND Fluoxetine is one of the most widely prescribed anti-depressant drugs belonging to the category of selective serotonin reuptake inhibitors.Long-term fluoxetine treatment results in hepatotoxicity.Baicalin,a natural compound obtained from the Chinese herb Scutellaria baicalensis is known to have antioxidant,hepatoprotective and anti-inflammatory effects.However,the beneficial effects of baicalin against fluoxetine-induced hepatic damage have not previously been reported.AIM To evaluate the protective action of baicalin in fluoxetine-induced liver toxicity and inflammation.METHODS Male albino Wistar rats were divided into seven groups.Group 1 was the normal control.Oral fluoxetine was administered at 10 mg/kg body weight to groups 2,3,4 and 5.In addition,groups 3 and 4 were also co-administered oral baicalin(50 mg/kg and 100 mg/kg,respectively)while group 5 received silymarin(100 mg/kg),a standard hepatoprotective compound for comparison.Groups 6 and 7 were used as a positive control for baicalin(100 mg/kg)and silymarin(100 mg/kg),respectively.All treatments were carried out for 28 d.After sacrifice of the rats,biomarkers of oxidative stress[superoxide dismutase(SOD),catalase(CAT),reduced glutathione(GSH),glutathione-S-transferase(GST),advanced oxidation protein products(AOPP),malondialdehyde(MDA)],and liver injury[alanine transaminase(ALT),aspartate transaminase(AST),alkaline phosphatase(ALP),total protein,albumin,bilirubin]were studied in serum and tissue using standard protocols and diagnostic kits.Inflammatory markers[tumor necrosis factor(TNF-α),interleukin(IL)-6,IL-10 and interferon(IFN)-γ]in serum were evaluated using ELISA-based kits.The effect of baicalin on liver was also analyzed by histopathological examination of tissue sections.RESULTS Fluoxetine-treated rats showed elevated levels of the serum liver function markers(total bilirubin,ALT,AST,and ALP)and inflammatory markers(TNF-α,IL-6,IL-10 and IFN-γ),with a decline in total protein and albumin levels.Biochemical markers of oxidative stress such as SOD,CAT,GST,GSH,MDA and AOPP in the liver tissue homogenate were also altered indicating a surge in reactive oxygen species leading to oxidative damage.Histological examination of liver tissue also showed degeneration of hepatocytes.Concurrent administration of baicalin(50 and 100 mg/kg)restored the biomarkers of oxidative stress,inflammation and hepatic damage in serum as well as in liver tissues to near normal levels.CONCLUSION These findings suggested that long-term treatment with fluoxetine leads to oxidative stress via the formation of free radicals that consequently cause inflammation and liver damage.Concurrent treatment with baicalin alleviated fluoxetine-induced hepatotoxicity and liver injury by regulating oxidative stress and inflammation. | Risha Ganguly Ramesh Kumar Abhay K Pandey | 2022 | World Journal of Hepatology2022，14，4： | 1 |
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