Research progress in drugs for treating sepsis / 药学学报

Sepsis is a refractory disease with high mortality in which the host's immune response to the infection is dysfunctional, resulting in life-threatening organ function damage. The pathogenesis of sepsis is complex, involving systemic inflammation, immunosuppressive and coagulation abnormalities, and endothelial barrier damage caused by the infecting pathogenic microorganisms and their toxins. The pathogenesis of sepsis is closely related to multiple systems disorder and multiple organ dysfunction and failure. In recent years, the incidence of sepsis has been increasing globally, with an annual increase of 9%. Since the development of sepsis does not depend on the infecting pathogenic microorganisms and the late inflammatory reaction can be life-threatening, clinical treatment of sepsis can be very difficult. However, the current antibiotic treatments for sepsis are not ideal. Most clinical treatments are not curative, so researchers seek new drug designs based on exploring molecular mechanisms of the pathophysiological process in sepsis patients. This paper reviews the recent development of drugs designed according to the sepsis pathophysiological process.

Non-targeted metabolomics in septic mice infected with Klebsiella pneumoniae / 药学学报

UHPLC-QTOF-MS was applied to non-targeted metabolomics study of mice infected with K. pneumoniae ATCC® BAA 2146 to discover potential biomarkers and metabolic pathways that are associated with sepsis. Fifty-eight metabolites were identified by principal components analysis (PCA) and partial least-squares discriminant analysis (OPLS-DA), which was combined with variable projection importance (VIP) and nonparametric test. Eighteen of the 58 metabolites were further found to be involved in 8 metabolic pathways, including nicotinate and nicotinamide metabolism, pyrimidine metabolism, vitamin B6 metabolism, taurine and hypotaurine metabolism, arginine and proline metabolism, alanine, aspartate and glutamate metabolism, D-glutamine and D-glutamate metabolism and glycerophospholipid metabolism.

Correlation study on Chinese medical syndrome types of chronic hepatitis B patients and HLA-DR13 gene, BCP mutation, and T-lymphocyte subsets / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To explore the correlation between the HLA-DR13, basic core promoter (BCP), changes of T lymphocyte subset and clinical Chinese medical syndromes of chronic hepatitis B (CHB).</p><p><b>METHODS</b>Totally 102 CHB patients were syndrome typed as Gan depression Pi deficiency syndrome (GDPDS), Pi-Shen yang deficiency syndrome (PSYDS), Gan-gallbladder dampness heat syndrome (GGDHS), Gan-Shen yin deficiency syndrome (GSYDS), and static blood blocking collaterals syndrome (SBBCS). Besides, 30 healthy subjects were recruited as the normal control group. The blood HBV-DNA level and HLA-DR13 gene were detected with real time fluorescent PCR. The expression of CD4+ and CD8+ in T lymphocytes was detected using flow cytometry. The mutation of serum A1762T/G1764A was detected using PCR sequencing. Hepatitis Be antigen (HBeAg) was detected with ELISA, and correlation between various Chinese medical syndrome types and objective indicators were analyzed.</p><p><b>RESULTS</b>There was no statistical difference in HBV-DNA quantitative results among various syndrome types (P > 0.05). HBeAg positive rate was higher in GDPDS than in other syndrome types (P < 0.05). It was sequenced as GDPDS > GSYDS > SBBCS > GGDHS > PSYDS. Compared with the normal control group, percentages of CD3+ and CD3+ CD4+ were lower in PSYDS (P < 0.05). The ratio of CD3+ CD4+/CD3+ CD8 was lower in GGDHS and PSYDS than in the normal control group (P < 0.05). There was no statistical difference in the CD3+ CD8+ percentage among various syndrome types (P > 0.05). The quantitation of HLA-DR13 gene was lower in GDPDS and GSYDS than in the normal control group (P < 0.05). The positive rate of BCP mutation was higher in GSYDS than in other syndrome types (P < 0.05).</p><p><b>CONCLUSION</b>Co-detection results of HLA-DR13 and BCP could be used as reference indices of Chinese medical syndrome typing of CHB.</p>

Euphorbia kansui roots induced-diarrhea in mice correlates with inflammatory response / 中国天然药物

AIM@#Euphorbia kansui (E. KS) is a traditional medicine used in China for thousands of years with the effect of propulsion in the gastrointestines. However, there is no reported study of E. KS on gastrointestinal motility until now. The aim of this work is to study the effect of E. KS on the propulsion of gastrointestines, and to elucidate the possible mechanism of action.@*METHODS@#E.KS was prepared as a 30% ethanol extract and used for the experiment of small and large intestines of mice by oral administration with three different dosages (1.2, 0.6 and 0.3 g·kg(-1)). The feces were observed in vivo. The morphology was carried out to detect if there are any changes in the intestines after the extract of E. KS administration. The assays of mRNA and protein expression were employed to observe IL-1β, TNFα and caspase 3.@*RESULTS@#It was shown that the extract of E.KS promoted diarrhea in mouse feces after administration, inhibited the contraction of smooth muscle of mouse small intestine and caused the inflammatory exudation on the mucosa of the intestines, enhanced the expression of both mRNA and the protein levels of IL-1β and TNFα in the small or large intestines.@*CONCLUSION@#The results showed that the extract of E. KS acted on the intestinal smooth muscle with propulsion of feces involving the irritation of the intestines with acute inflammatory reactions.

Treatment of complicated cavernous venous malformation with retained copper wires combined with pingyangmycin injection / 中华整形外科杂志

<p><b>OBJECTIVE</b>To evaluate the therapeutic effect of retained copper wires combined with pingyangmycin (PYM) injection for complicated cavernous venous malformation.</p><p><b>METHODS</b>The location of venous malformation was detected by physical examination and MRI. The copper wires in 0.2 mm width were used to puncture the lesion repeatedly and retained in the lesion to form a net. After that, 8 mg PYM was injected into the residue malformed veins. 8-10 days later, the copper wires were taken out and necrotic tissue was squeezed out. The wounds of punctual holes healed through dressing. The patients received postoperative MRI to evaluate the therapeutic effect.</p><p><b>RESULTS</b>From Jan. 2002 to Dec. 2008, 45 cases were treated. The patients were followed up for 1-3 years. 51.1% (23/45) of the lesions shrinked markedly or even disappeared. 42.2% (19/45) of the lesions reduced. 6.67% (3/45) of the lesions didn't change. There was no complication like invasive infection.</p><p><b>CONCLUSIONS</b>It is very effective to treat complicated cavernous venous malformation with retained copper wires combined with pingyangmycin injection.</p>

Antivirus effects of extract from gardenia / 中国中药杂志

<p><b>OBJECTIVE</b>To observe the effect of the extract from gardenia on influenza viral pneumonia in mice and virus-induced cytopathic effect.</p><p><b>METHOD</b>The mice were infected by influenza virus in nasal, the lung inflammation, mortality rate and life elongation rate were observed respectively. The anti-viral activity of the extract from gardenia was accessed by cytopathic effect (CPE) in vitro and 0% toxicity concentration (TC0), 50% toxicity concentration (TC50), 50% inhibitor concentration (IC50), therapeutic index (TI) were determined by Reed-Muench method.</p><p><b>RESULT</b>The pneumonia induced by influenza virus in mice was inhibited significantly by the extract from gardenia, as the mortality rate decreased and the life elongation rate increased remarkably. Meanwhile the NO content in serum decreased significantly; The cytopathic effect induced by six kinds of viruses was inhibited remarkably.</p><p><b>CONCLUSION</b>The six kinds of viruses were inhibited significantly by the extract from gardenia which inhibitory effect on mice influenza viral pneumonia was related to the NO content decreased.</p>

Determination of quercetin-3-O-beta-D-glucopyranosyl-7-O-beta-D-gentiobioside in semen descurainiae by HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To establish a method for the determination of quercetin-3-O-beta-D-glucopyranosyl-7-O-beta-D-gentiobioside in Semen Descurainiae.</p><p><b>METHOD</b>HPLC was used with self-made quercetin-3-O-beta-D-glucopyranosyl-7-O-beta-D-gentiobioside as reference substances.</p><p><b>RESULT</b>The average collection was 99.78%, RSD 2.4%.</p><p><b>CONCLUSION</b>The method is appropriate for quality control of Semen Descurainiae.</p>

Isolation and structure identification of chemical constituents from the seeds of Descurainia sophia (L.) Webb ex Prantl / 药学学报

<p><b>AIM</b>To isolate and determine the structures of chemical constituents from the seeds of Descurainia sophia (L.) Webb ex Prantl.</p><p><b>METHODS</b>The chemical constituents were extracted from the seeds of Descurainia sophia (L.) Webb ex Prantl with 75% ethanol and purified by polyamide, silica gel, RP-C18 and Sephadex LH-20 on column chromatography. Chemical methods and spectroscopic methods, such as 1H and 13CNMR, HSQC, HMBC and TOCSY spectra were used for the structural identification.</p><p><b>RESULTS</b>Fifteen compounds were obtained. Twelve of them were identified as quercetin-3-O-beta-D-glucopyranosyl-7-O-beta-gentiobioside (I), kaempferol-3-O-beta-D-glucopyranosyl-7-O-beta-gentiobioside (II), isorhamnetin-3-O-beta-D-glucopyranosyl-7-O-beta-gentiobioside (III), quercetin-7-O-beta-gentiobioside (IV), kaempferol-7-O-beta-gentiobioside (V), isorhamnetin-7-O-beta-gentiobioside (VI), quercetin-3,7-di-O-beta-D-glucopyranoside (VII), kaempferol-3, 7-di-O-beta-D-glucopyranoside (VIII), isorhamnetin-3, 7-di-O-beta-D-glucopyranoside (IX), kaempferol-3-O-beta-D-glucopyranosyl-7-O-[(2-O-trans-sinnapoyl)-beta-D- glucopyranosyl(1-->6)]-beta-D-glucopyranoside) (X), sinapic acid ethyl ester (XI) and 3, 4, 5-trimethoxyl-cinnamic acid (XII).</p><p><b>CONCLUSION</b>Compounds X and VI are new compounds. IV, V, VII, VIII and IX were isolated from Cruciferae family for the first time. I, II, III were obtained from Descurania genus and XI, XII from D. sophia for the first time.</p>