Evaluation of the effectiveness of malaria control health education among overseas enterprise employees / 中国血吸虫病防治杂志

Objective To evaluate the effectiveness of health education on knowledge, attitude and practice (KAP) relating to malaria control among overseas enterprise employees. Methods In September 2019, on-site malaria control health education was conducted among all Chinese employees of a China-funded mining enterprise in the Democratic Republic of Congo. The KAP questionnaire for malaria control was generated on the Questionstar website, and the participants were subjected to two questionnaire surveys prior to and 14 months after health education. After the questionnaires were recovered, all valid questionnaires were divided into 4 groups, including the baseline group (the questionnaires filled out by respondents who received health education and participated in two questionnaire surveys before health education), the loss-to-follow-up group (the questionnaires filled out by respondents who received health education but only participated in the questionnaire survey after health education), the retest group (the questionnaires filled out by respondents who received health education and participated in two questionnaire surveys after health education) and the new group (questionnaires filled out by respondents who did not receive health education and only participated in the questionnaire survey after health education) according to subjects’ receiving health education and participation in two questionnaire surveys. The correct rate of malaria control knowledge, the proportion to good attitudes towards malaria control and the proportion of good practices towards malaria control were compared between the baseline group and the loss-to-follow-up group, between the baseline group and the retest group, and between the retest group and the new group. Results A total of 110 and 142 valid questionnaires were recovered during the two surveys, and the recovery rates were 90.9% and 70.3%, respectively. There were 77, 77, 33, and 65 valid questionnaires recovered from the baseline group, the loss-to-follow-up group, the retest group, and the new group, respectively. There were no significant differences in respondents’ gender, age and educational levels between the baseline group and the loss-to-follow-up group (all P values > 0.05), and there were no significant differences between the two groups in terms of the mean score of malaria control knowledge (Z = 2.011, P > 0.05), the mean score of attitudes towards malaria control (t = −0.787, P > 0.05) and the mean score of practices towards malaria control (t = −0.787, P > 0.05). There were significant differences between the retest group and the baseline group in terms of the mean score of malaria control knowledge (10.83 vs. 9.79; Z = −4.017, P < 0.05), the mean score of attitudes towards malaria control (29.48 vs. 28.61; Z = −1.981, P < 0.05) and the mean score of practices towards malaria control (6.43 vs. 5.91; Z = −2.499, P < 0.05). There were no significant differences between the retest group and the new group in terms of gender, age or education levels (all P values > 0.05), and a higher mean score of malaria control knowledge was found in the retest group than in the new group (10.83 vs. 9.81; Z = −2.962, P < 0.05), while no significant differences were seen in the mean score of attitudes towards malaria control (29.48 vs. 30.17; Z = −1.158, P > 0.05) and the mean score of practices towards malaria control (6.43 vs. 6.37; Z = −0.048, P > 0.05) between the two groups. Conclusion Malaria control health education may significantly improve the understanding of malaria control knowledge, positive attitudes towards malaria control and the compliance of practices towards malaria control among overseas enterprise employees.

Exploration on Effect of Yinhuotang on Depression-like Behavior in Mice with Bilateral Ovariectomy Induced by Chronic Stress Based on E2/ERβ Signaling Pathway / 中国实验方剂学杂志

Objective:To observe the effect of Yinhuotang （YHT） on the depression-like behavior of mice with bilateral ovariectomy （OVX） induced by chronic stress and explore its action mechanism based on estradiol （E₂）-estrogen receptor <italic>β </italic>（ER<italic>β</italic>） pathway. Method:The experiment was divided into two parts. In the first part， mice were randomly divided into the sham operation （Sham） group， model （OVX） group， positive drug （E₂， 0.13 mg·kg^-1） group， and YHT （23.4 g·kg^-1） group. The OVX model was reproduced by OVX combined with chronic unpredictable mild stress （CUMS）. On the 8th day after OVX， the mice in each group were exposed to CUMS and treated with drugs. The changes in immobility time， horizontal movement score， and vertical movement score of mice in each group were observed in forced swimming test （FST）， tail suspension test （TST） and open-field test （OFT）， respectively. Serum and brain E₂ levels were detected by enzyme-linked immunosorbent assay （ELISA）， the aromatizing enzyme （Cyp19） mRNA expression by real-time fluorescence polymerase chain reaction （Real-time PCR）， the expression of ER<italic>α</italic> and ER<italic>β</italic> in dentate gyrus of hippocampus by immunohistochemistry （IHC）， and the total ER<italic>α</italic> and ER<italic>β</italic> levels in the brain by Western blotting. In the second part， the mice were divided into the Sham group， OVX group， YHT group， and blocker （Y+B， 23.4 g·kg^-1+100 μg·kg^-1） group. Mice in the Y+B group were first treated with intragastric administration of YHT and then with intraperitoneal injection of ER<italic>β</italic> blocker （PHTPP） on the next day. The changes in immobility time， horizontal motor score， and vertical motor score were observed in the three behavioral tests. Result:Compared with the Sham group， the OVX group displayed significantly increased immobility time， decreased horizontal and vertical movement scores （<italic>P</italic><0.01）， down-regulated serum and brain E₂levels （<italic>P</italic><0.01） and Cyp19 mRNA expression in the brain （<italic>P</italic><0.01）， and up-regulated total ER<italic>β</italic> in dentate gyrus and brain （<italic>P</italic><0.01）. However， there was no significant change in total ER<italic>α</italic> expression in the dentate gyrus or brain. As revealed by comparison with the OVX group， the immobility time of the E₂ group was decreased significantly， while the horizontal and vertical movement scores were increased significantly （<italic>P</italic><0.01）. The E₂ levels in the serum was significantly elevated （<italic>P</italic><0.01）. The Cyp19 mRNA expression in the brain and the total ER<italic>α</italic> expression in the dentate gyrus and brain were not significantly changed， while the expression levels of total ER<italic>β</italic> in dentate gyrus and brain were significantly increased （<italic>P</italic><0.01）. In the YHT group， the immobility time declined significantly， and the horizontal and vertical movement scores rose significantly （<italic>P</italic><0.01）. The serum E₂ did not increase， whereas the brain E₂ increased significantly （<italic>P</italic><0.01）. The expression of Cyp19 gene in the brain was significantly increased （<italic>P</italic><0.05，<italic>P</italic><0.01）. There was no significant change in the total ER<italic>α</italic> of dentate gyrus and brain， but the expression levels of total ER<italic>β</italic> in dentate gyrus and brain were significantly increased （<italic>P</italic><0.05，<italic>P</italic><0.01）. PHTPP reversed the effects of YHT on OVX mice in FST， TST and OFT. Conclusion:YHT promotes the synthesis and release of endogenous estrogen in brain and improves the depression-like behavior of OVX mice induced by chronic stress， which is possibly related to the activation of E₂/ER<italic>β</italic> pathway.

Expression of forkhead transcription factor O4 in prostate cancer and its effect on prostate cancer cell invasion / 中南大学学报(医学版)

To examine the expression of forkhead transcription factor O4 (FOXO4) in prostate cancer and to explore its effect on prostate cancer cell invasion.
 Methods: Immunohistochemistry was used to detect the expression of FOXO4 in prostate hyperplasia tissues and prostate cancer tissues. Western blot was used to detect the expression of FOXO4 in prostate hyperplasia cell line BPH-1 and prostate cancer cell lines: PC-3 and DU145. PC-3 cells with high relative expression of FOXO4 were transfected with FOXO4 siRNA and scramble siRNA; DU145 cells with low expression of FOXO4 were transfected with FOXO4 plasmid and blank vector. Matrigel Transwell assay was used to detect the invasive ability of transfected cells. The expression of endothelial-mesenchymal transition (EMT)-related proteins E-cadherin, N-cadherin, and vimentin in the transfected cells was detected by Western blot.
 Results: The expression of FOXO4 in prostate cancer cells and tissues was significantly lower than that in the prostate hyperplasia cells and tissues (both P10 (all P<0.05). The expression of FOXO4 in cancer tissues with Gleason score <8 was significantly higher than that in the cancer tissues with Gleason ≥8 (P<0.05). The expression of FOXO4 in clinical stage T1-T2 prostate cancer tissues was higher than that in the clinical stage T3-T4 prostate cancer tissues (P<0.05). The expression of FOXO4 in prostate cancer tissues without lymph node metastasis was significantly higher than that in the prostate cancer tissues with lymph node metastasis (P<0.05). Down-regulation of FOXO4 in PC-3 cells could significantly promote the EMT and invasion, with the decreased expression of E-cadherin and the increased expression of N-cadherin and vimentin (all P<0.05); Up-regulation of FOXO4 in DU145 cells could inhibit the EMT and invasion of cells, with the increased expression of E-cadherin and the decreased expression of N-cadherin and vimentin (all P<0.05).
 Conclusion: FOXO4 is involved in prostate cancer progression, and it can inhibit prostate cancer cell invasion by regulating EMT of prostate cancer cells.

Effect of salvianolic acid B on nasal absorption in rats in situ / 中国中药杂志

This experiment focused on the effect of salvianolic acid B's nasal absorption characteristics in rats. In the study, HPLC determination of salvianolic acid B(SalB) in perfusion liquid was established to examine the SalB nasal irritation in different pH buffers and stability in nasal perfusion solution, and systematically study in vivo nasal absorption characteristics of SalB. Improved rats were adopted to establish the in situ nasal perfusion model to measure the release of total protein and lactate dehydrogenase in perfusion fluid, quantitatively evaluate the nasal irritation and the stability in perfusion liquid of pH 4.0, 5.0, 6.0 SalB phosphate buffer, compare the absorption of SalB in pH 5.0 buffer solution with low, medium and high concentrations (200, 400, 800 mg•L⁻¹). According to the results, nasal irritation: pH 4.0>pH 5.0>pH 6.0, RSD of pH 6.0 SalB buffer solution within 24 h was 3.1%, stability was poor. PH 5.0 SalB buffer solution had a smaller irritation and good stability. According to the nose perfusion test in rats, the nasal absorption of SalB fitted the first-order process and could be considered as passive absorption based on concentration gradient. SalB buffer solution of pH 5.0 had also a small nasal irritation and good stability, with a good absorption in rat nasal perfusion test, which therefore had a certain significance for the development of SalB nasal formulation.

UPLC-MS/MS determination of content of three iridoids of xingnaojing oral preparation in rat brains and study on their brain pharmacokinetics / 中国中药杂志

To establish a UPLC-MS/MS method for the simultaneous determination of geniposide, genipin 1-O-beta-D-gentiobioside and geniposidic acid in rat brains and study the brain pharmacokinetics of the three iridoid glycosides in stroke rat after the oral administration of Xingnaojing. In this experiment, brain samples were precipitated with protein for twice. Acquity BEH C18 column was adopted, with acetonitrile-0.1% formic acid-water as the mobile phase for gradient elution. ESI source was adopted for mass spectra; multiple reaction monitoring (MRM) was conducted to detect negative ions. The time for sample analysis was 3.5 min. the results showed good linear relations among the three iridoid glycosides, with the extraction recovery between 99.6% and 114.3%, good intra- and inter-day precisions and accuracies and stability in line with the requirements. The t1/2 and MRT in the three components were similar in brains of stroke rats. Geniposide and genipin 1-O-beta-D-gentiobioside showed double peaks; where as geniposidic acid showed a single peak. In conclusion, the method is so specific, sensitive, accurate and reliable that it can be used to study the brain pharmacokinetics of Xingnaojing oral preparation.

Optimization of Extraction Process of Volatile Oil from Wenyang Purgation Granules by Orthogonal Design / 中国中医药信息杂志

Objective To optimize the extraction conditions of volatile oil from Angelica Sinensis and Cassia Bark in Wenyang purgation granules.Methods The volatile oil was extracted from Angelica Sinensis and Cassia Bark by the method of steam distillation light oil device with diethyl ether extraction. The yield of the volatile oil was chosen as the evaluation index. The time of dip in water, the ratio of water to herbal medicine material and the time of distillation were used as the main factors. The optimum extraction conditions were investigated by the L9(34) orthogonal design. Results The optimal conditions for extraction process of volatile oil from Angelica Sinensis and Cassia Bark in Wenyang purgation granules were as follows:the time of dip in water was 3 h;the ratio of water to herbal medicine material was 10∶1;the time of distillation was 6 h. Conclusion The optimized conditions of extraction process are stable and feasible.

Study on in situ intestinal absorption of active ingredients in Shuanghuanglian oral liquid in rats / 中国中药杂志

<p><b>OBJECTIVE</b>To study the intestinal absorption kinetics characteristic of the main four active ingredients in Shuanghuanglian oral liquid (SHL) and to investigate the influence of herbal compatibility in SHL on absorption of main effective ingredients.</p><p><b>METHOD</b>The in situ rat circulation model was used to investigate the concentration change differences of the four active components in SHL during perfusion.</p><p><b>RESULT</b>The absorption quantity of different concentrations of baicalin, chlorogenic acid, phillyrin and forsythoside A ranging from 40-160, 6-24, 3-12, 2.6-10.4 mg x L(-1) respectively was linear with concentration and showed no saturation at high concentration. The absorption rate constant K(a) and the hourly absorption percentages A were essentially unchanged. The pH changing from 5.0-7.43 had little influence on the absorption of phillyrin except baicalin, chlorogenic acid and forsythoside A. The calculated K(a) and A of the four active ingredients had no significant differences from that obtained after perfusing via duodenum, jejunum, ileum and colon; The calculated K(a) and A of baicalin in Scutellariae Radix (SR), chlorogenic acid in Lonicerae Japonicae Flos (LJF) and phillyrin in Forsythiae Fructus (FF) had no significant differences compared with that in SHL, but the calculated K(a) and A of forsythoside A in FF were obviously superior to that in SHL.</p><p><b>CONCLUSION</b>The intestinal absorption of the four active ingredients in SHL was mainly passive diffusion and had no difference in different segments of rat intestine; the compatibility of SHL compounds changed the absorption of forsythoside A in FF obviously.</p>

Intestinal absorption of forsythoside A by rat circulation in situ / 药学学报

This study is to investigate the effects of concentration, intestinal section, pH, paracellular route, substrate/inhibitor of enzyme (CYP3A) and proteins (P-gp, MRP2, SGL1) on the absorption of forsythoside A. The absorption of three concentrations (2.6, 5.2, and 10.4 microg x mL(-1)) of forsythoside A in different intestinal segments was studied with phenol red as the marker by rat circulation in situ. The results showed that the residue of forsythoside A with different concentrations had little significant difference from that obtained after perfusing via duodenum, jejunum, ileum and colon, which indicated that the absorption of forsythoside A was passive diffusion and had no difference in different segments of rat intestine. The residue of forsythoside A increased to 466.160 and 463.429 microg respectively when cyclosporine (4 microg x mL(-1)) or midazolam (50 micromol x L(-1)) was added to the circulation fluid, which showed significant difference compared to the control group (P < 0.05). Moreover, the residue of forsythoside A showed a tendency of increase with the increase of cyclosporine or midazolam. When digoxin (50 micromol x L(-1)) or EDTA (10 microg x mL(-1)) was added to the circulation fluid, the residue of forsythoside A decreased to 325.110 and 369.888 microg respectively, which showed significant difference as compared to the control group (P < 0.05). Besides, the residue of forsythoside A showed a tendency of reduction with the increase of digoxin or EDTA. However, there is no significant change in the absorption of forsythoside A when the different concentrations of mannitol were added to the circulation fluid. The results above indicated that the absorption of forsythoside A was mainly passive diffusion and involved paracellular route at the same time. In addition, the substrates of P-gp or CYP3A had dose-dependent effect on the absorption of forsythoside A.

Important application of intestinal transporters and metabolism enzymes on gastrointestinal disposal of active ingredients of Chinese materia medica / 中国中药杂志

Oral drug bioavailability depends on gastrointestinal absorption, intestinal transporters and metabolism enzymes are the important factors in drug gastrointestinal absorption and they can also be induced or inhibited by the active ingredients of Chinese materia medica. This article presents important application of intestinal transporters and metabolism enzymes on gastrointestinal disposal of the active ingredients of Chinese materia medica, and points out the importance of research on transport and metabolism of the active ingredients of Chinese materia medica in Chinese extract and Chinese medicinal formulae.

Intestinal absorption of forsythoside A by rat circulation in situ / 药学学报

This study is to investigate the effects of concentration, intestinal section, pH, paracellular route, substrate/inhibitor of enzyme (CYP3A) and proteins (P-gp, MRP2, SGL1) on the absorption of forsythoside A. The absorption of three concentrations (2.6, 5.2, and 10.4 microg x mL(-1)) of forsythoside A in different intestinal segments was studied with phenol red as the marker by rat circulation in situ. The results showed that the residue of forsythoside A with different concentrations had little significant difference from that obtained after perfusing via duodenum, jejunum, ileum and colon, which indicated that the absorption of forsythoside A was passive diffusion and had no difference in different segments of rat intestine. The residue of forsythoside A increased to 466.160 and 463.429 microg respectively when cyclosporine (4 microg x mL(-1)) or midazolam (50 micromol x L(-1)) was added to the circulation fluid, which showed significant difference compared to the control group (P < 0.05). Moreover, the residue of forsythoside A showed a tendency of increase with the increase of cyclosporine or midazolam. When digoxin (50 micromol x L(-1)) or EDTA (10 microg x mL(-1)) was added to the circulation fluid, the residue of forsythoside A decreased to 325.110 and 369.888 microg respectively, which showed significant difference as compared to the control group (P < 0.05). Besides, the residue of forsythoside A showed a tendency of reduction with the increase of digoxin or EDTA. However, there is no significant change in the absorption of forsythoside A when the different concentrations of mannitol were added to the circulation fluid. The results above indicated that the absorption of forsythoside A was mainly passive diffusion and involved paracellular route at the same time. In addition, the substrates of P-gp or CYP3A had dose-dependent effect on the absorption of forsythoside A.

Intestinal absorption of daphnetin by rats single pass perfusion in situ / 药学学报

This study investigated the effects of concentration, intestinal section, pH and P-gp on the absorption of daphnetin. The absorptions of three concentrations (10, 20, 40 microg x mL(-1)) of daphnetin in different intestinal segments were studied with phenol red as the marker by in situ rats single pass perfusion model. The results showed that daphnetin was stable under pH 6.0 condition and little affected by metabolism enzyme. There was upgrade tendency between the Peff of duodenum, jejunum, ileum and colon in different concentration of daphnetin, and it has obvious difference between the high concentration and low concentration in jejunum and colon, which indicated that the absorption of daphnetin was passive diffusion and no difference in different segments of rat intestine. However, compared with colon, the absorption of small intestine was better significantly (P < 0.05). Daphnetin may be not a substrate of P-gp as verapamil had not significantly affected the absorption of daphnetin in different intestinal segments of rats.