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1.
Artigo em Inglês | WPRIM | ID: wpr-922765

RESUMO

Guided by cell-based anti-anaphylactic assay, eighteen cage-like monoterpenoid glycosides (1-18) were obtained from the bioactive fraction of P. lactiflora extract. Among these, compounds 1, 5, 6, 11, 12, 15, and 17 significantly reduced the release rate of β-HEX and HIS without or with less cytotoxicity. Furthermore, the most potent inhibitor benzoylpaeoniflorin (5) was selected as the prioritized compound for the study of action of mechanism, and its anti-anaphylactic activity was medicated by dual-inhibiting HDC and MAPK signal pathway. Moreover, molecular docking simulation explained that benzoylpaeoniflorin (5) blocked the conversion of L-histidine to HIS by occupying the HDC active site. Finally, in vivo on PCA using BALB/c mice, benzoylpaeoniflorin (5) suppressed the IgE-mediated PCA reaction in antigen-challenged mice. These findings indicated that cage-like monoterpenoid glycosides, especially benzoylpaeoniflorin (5), mainly contribute to the anti-anaphylactic activity of P. lactiflora by dual-inhibiting HDC and MAPK signal pathway. Therefore, benzoylpaeoniflorin (5) may be considered as a novel drug candidate for the treatment of anaphylactic diseases.


Assuntos
Animais , Camundongos , Glucosídeos , Camundongos Endogâmicos BALB C , Simulação de Acoplamento Molecular , Monoterpenos , Paeonia , Raízes de Plantas
2.
Artigo em Chinês | WPRIM | ID: wpr-237938

RESUMO

<p><b>OBJECTIVE</b>To explore the effect of Compound Tongtu Granule (CTG) on intestinal permeability in elderly sepsis patients.</p><p><b>METHODS</b>Eighty elderly sepsis patients were randomly assigned to the experimental group and the control group by randomized double blinded method, 40 in each group. On the basis of conventional antiseptic treatment program, patients in the experimental group took CTG, while those in the control group took placebos. The dosage for CTG or placebos was 14.3 g each package, one package each time, twice daily for 14 successive days. Patients' abdominal symptoms and signs, levels of serum inflammatory factors (high-sensitivity C-reactive protein and procalcitonin), levels of plasma endotoxin, and the intestinal permeability (IP, represented by urinary lactulose/mannitol excretion rate) were compared between the two groups before and after treatment.</p><p><b>RESULTS</b>After 14-day treatment, patients in the experimental group had improved abdominal symptoms, increased frequency of defecation, significantly decreased levels of plasma endotoxin and IP, when compared with the control group (P < 0.05).</p><p><b>CONCLUSION</b>CTG could improve the intestinal barrier function in elderly sepsis patients.</p>


Assuntos
Idoso , Humanos , Proteína C-Reativa , Metabolismo , Calcitonina , Metabolismo , Peptídeo Relacionado com Gene de Calcitonina , Defecação , Medicamentos de Ervas Chinesas , Farmacologia , Usos Terapêuticos , Endotoxinas , Metabolismo , Intestinos , Metabolismo , Permeabilidade , Precursores de Proteínas , Metabolismo , Sepse , Tratamento Farmacológico
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