The inhibitory effect of sodium baicalin on oseltamivir-resistant influenza A virus via reduction of neuraminidase activity

Jin, Jing; Chen, Yuanjin; Wang, Dechuan; Ma, Lingman; Guo, Min; Zhou, Changlin; Dou, Jun

doi:10.1007/s12272-018-1022-6

Cited by 35 publications

(28 citation statements)

References 22 publications

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“…This indicated that the drug was rapidly eliminated after i.v. injection in piglets and was much slower than the rate reported in mice (Jin et al, 2018) Abbreviations: AUC 0-∞ , area under the curve from time 0 to infinity; CL, body clearance; C max , peak plasma concentration; F, absolute bioavailability; t 1/2Ka , absorption half-life; t 1/2α , distribution halflife; t 1/2β , elimination half-life; T max , time of peak concentration; V d , apparent volume of distribution. a Mean ± SD, n = 8.…”

mentioning

confidence: 60%

“…This indicated that the drug was rapidly eliminated after i.v. injection in piglets and was much slower than the rate reported in mice (Jin et al, ) but faster than for rats (Li et al, ; Xing et al, ; Yang et al, ; Zhang et al, ) and rabbits (Wei et al, ). The V d was 1.63 ± 0.23 L/kg indicating that baicalin was widely distributed into body tissues.…”

Section: Pharmacokinetic Parameters Of Baicalin Following Single Intrmentioning

confidence: 83%

“…The pharmacokinetic properties of baicalin have been investigated in mouse (Jin et al, ), rat (Huang, Liu, & Zhang, ; Li et al, ; Xing, Chen, & Zhong, ; Yang, Li, Xin, Wang, & Zhang, ) and rabbit (Wei et al, ) models but not in pigs. After oral administration, baicalin displays a distinct pharmacokinetic profile that includes gastrointestinal hydrolysis (Noh et al, ), enterohepatic recycling (Xing et al, ), carrier‐mediated transport (Kalapos‐Kovács et al, ) as well as a complex metabolism (Huang et al, ; Kang et al, ).…”

Section: Pharmacokinetic Parameters Of Baicalin Following Single Intrmentioning

confidence: 99%

“…and intramuscular (i.m.) administration using its sodium salt to increase water solubility (Jin et al, ). Pharmacokinetic data reported in this study will provide information for the design of future studies involving the use of baicalin in pigs.…”

Section: Pharmacokinetic Parameters Of Baicalin Following Single Intrmentioning

confidence: 99%

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Pharmacokinetics of sodium baicalin following intravenous and intramuscular administration to piglets

Liu

Zhao

et al. 2019

Vet Pharm & Therapeutics

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The purpose of this study was to determine the pharmacokinetics of baicalin after intravenous and intramuscular administration of sodium baicalin at 50 mg/kg to piglets. Plasma baicalin levels were determined by high‐performance liquid chromatography. The plasma concentration–time data of baicalin for both administration routes were best described by two‐compartmental open model. The area under the plasma concentration–time curve and the elimination half‐lives were 77.47 ± 6.14 µg/ml × h and 1.73 ± 0.16 hr for intravenous and 64.85 ± 5.67 µg/ml × h and 2.42 ± 0.15 hr for intramuscular administration, respectively. The apparent volume of distribution and body clearance were 1.63 ± 0.23 L/kg and 2.74 ± 0.30 L h−1 kg−1 for intravenous and 0.51 ± 0.10 L/kg and 0.78 ± 0.08 L h−1 kg−1 for intramuscular routes, respectively. An intramuscular injection of sodium baicalin in piglets resulted in rapid and complete absorption, with a mean maximal plasma concentration of 77.28 ± 7.40 µg/ml at 0.17 hr and a high absolute bioavailability of 83.73 ± 5.53%.

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confidence: 60%

Section: Pharmacokinetic Parameters Of Baicalin Following Single Intrmentioning

confidence: 83%

Section: Pharmacokinetic Parameters Of Baicalin Following Single Intrmentioning

confidence: 99%

Section: Pharmacokinetic Parameters Of Baicalin Following Single Intrmentioning

confidence: 99%

See 2 more Smart Citations

Pharmacokinetics of sodium baicalin following intravenous and intramuscular administration to piglets

Liu

Zhao

et al. 2019

Vet Pharm & Therapeutics

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“…Baicalin (Figure ) is isolated from the dried roots of S. baicalensis , it contains electron‐rich carbonyl and carboxyl groups, which can form the complexes with metal ions, emerged the higher bioactivity. It has been reported that the combination of baicalin with zinc(II) showed better anti‐HIV‐1 activities than baicalin, baicalin‐oxidovanadium(IV) improved its action in decreased the number of viable human lung cancer cells, baicalin‐sodium (I) exhibited a higher inhibitory rate, baicalin‐Copper(II) decreased the growth of HepG2 cell tumor xenografts in nude mice by inhibiting cell proliferation . However, because of the limitations of the extraction method, baicalin complexes have not been detected in organism, the acquisition of this kind of compounds can only from the artificial synthesis method .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization of a Baicalin‐Strontium(II) Complex and Its BSA‐Binding Activity

Wang

Xiong

et al. 2019

ChemistrySelect

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Baicalin is one of the major bioactive constituents of Scutellaria baicalensis Georgi, possessed anti‐inflammation, antimicrobial and anticancer activity, has been attained extensive attention. In the present work, a new baicalin‐Sr(II) complex (Sr[baic]⋅3H2O) was synthesized to enhance its biological activity. A series of experiments were carried out to give the satisfying reaction conditions: pH=8.3 and the molar ratio of L:M ≤ 1:1. The obtained complex Sr[baic]⋅3H2O was characterized by IR, ES‐MS UV‐vis, atomic absorption, elemental analysis and thermogravimetric analysis. The interactions between baicalin/Sr[baic] and bovine serum albumin were also researched through fluorescence spectrum, which accord with the static quenching mechanism, Sr[baic] has higher binding ability than baicalin. Thermodynamic parameters ΔG°<0, ΔH°<0 and ΔS°>0, indicated that electrostatic forces is the major interaction forces in Sr[baic]‐bovine serum albumin system. Furthermore, the synchronous fluorescence experiments were carried out. The studies revealed that both baicalin and Sr[baic] quench the intrinsic fluorescence of bovine serum albumin, and the possible binding site is located on Trp residues. In circular dichroism spectrum, the binding of baicalin and Sr[baic] to bovine serum albumin lead to a loss in helical stability, by contrast, Sr[baic] increases baicalin's binding ability.

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Discovery and pharmacodynamic evaluation of the novel butene lactone derivativeM355against influenza A virus in vitro and in vivo

Geng

Zhang

et al. 2022

Journal of Medical Virology

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A new series of butene lactone derivatives were designed according to an influenza neuraminidase target and their antiviral activities against H1N1 infection of Madin-Darby canine kidney cells were evaluated. Among them, a compound that was given the name M355 was identified as the most potent against H1N1 (EC 50 = 14.7 μM) with low toxicity (CC 50 = 538.13 μM). It also visibly reduced the virus-induced cytopathic effect. Time-of-addition analysis indicated that H1N1 was mostly suppressed by M355 at the late stage of its infectious cycle. M355 inhibited neuraminidase in a dose-dependent fashion to a similar extent as oseltamivir, which was also indicated by a computer modeling experiment. In a mouse model, lung lesions and virus load were reduced and the expression of nucleoprotein was moderated by M355. The enzyme-linked immunosorbent assay and quantitative real-time polymerase chain reaction analyses revealed that the levels of interferon-γ, interferon regulatory factor-3, Toll-like receptor-3, tumor necrosis factor-α, interleukin (IL)-1β, IL-6, and IL-8 were downregulated in the M355-treated groups, whereas the levels of IL-10 and IL-13 were upregulated. Similarly, IgG was found to be increased in infected mice plasma. These results demonstrate that M355 inhibit the expression of H1N1 in both cellular and animal models. Thus, M355 has the potential to be effective in the treatment of influenza A virus infection.

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The inhibitory effect of sodium baicalin on oseltamivir-resistant influenza A virus via reduction of neuraminidase activity

Cited by 35 publications

References 22 publications

Pharmacokinetics of sodium baicalin following intravenous and intramuscular administration to piglets

Pharmacokinetics of sodium baicalin following intravenous and intramuscular administration to piglets

Synthesis, Characterization of a Baicalin‐Strontium(II) Complex and Its BSA‐Binding Activity

Discovery and pharmacodynamic evaluation of the novel butene lactone derivativeM355against influenza A virus in vitro and in vivo

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