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Buxrugulosides A-E, four lignan glycosides (1-4) and a protocatechuate derivative (5) featuring a rare (N, N-diethyl)methyl amino group at aromatic rings, were obtained from the aerial parts of Buxus rugulosa, which is famous for treating coronary heart disease. Their structures including absolute configurations were elucidated by HRMS, 1D and 2D NMR, and by comparing their CD data with previous reports. Compound 1 was a rare sesquilignan, and all of these compounds were the first example of lignans with (N, N-diethyl)methyl amino group.
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Objective: The aim of this study is to discover the possible working mechanisms of Ardisiae Japonicae Herba (AJH) on hepatoma carcinoma (HCC). Methods: In this study, ethanol extract of AJH was prepared and used to treat HCC cell in vitro. Furthermore, a genomic wide RNA sequencing (RNA-seq) was performed to screen deregulated genes in HCC cells after the treatment of AJH extract. The gene and protein expression related to lipid metabolism in HCC cells were also investigated to validate the results obtained from RNA-seq. Results: AJH extract could inhibit HCC cell proliferation in vitro. RNA-seq analysis has identified 1,601 differentially expressed genes (DEGs, fold change ≥ 2.0 or fold change ≤ 0.5, P < 0.05) in HCC after AJH extract treatment, which included 225 up-regulated genes and 1,376 down-regulated genes. KEGG pathway analysis of DEGs demonstrated that lipid metabolism was a potential pathway related to AJH treatment. In agreement with the RNA-seq data, qPCR and Western-blot analysis indicated that expression of genes and proteins related to lipid metabolism (SREBP1, ACC, ACLY and FASN) were significantly down-regulated in AJH treatment group as compared with the control group. Furthermore, AJH extract could also decrease lipid contents and cellular free fatty acid levels in HCC cells. Conclusion: Ethanol extract of AJH could inhibit HCC cell proliferation in vitro, the possible mechanism may be related to the inhibition of lipid metabolism.
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The aim of this study was to elucidate the mechanism of nuciferine on alleviating obesity based on modulating gut microbiota, ameliorating chronic inflammation, and improving gut permeability. In this study, the obese model mice were induced by high-fat diet and then randomly divided into model group, and nuciferine group; some other mice of the same week age were fed with normal diet as normal group. In the modeling process, the mice were administered intragastrically(ig) for 12 weeks. In the course of both modeling and treatment, the body weight and food intake of mice in each group were measured weekly. After modeling and treatment, the Lee's index, weight percentage of inguinal subcutaneous fat, and the level of blood lipid in each group were measured. The pathological changes of adipocytes were observed by HE staining to evaluate the efficacy of nuciferine treatment in obese model mice. 16 S rRNA sequencing analysis was conducted to study the changes in diversity and abundance of gut microbiota after nuciferine treatment. Enzyme-linked immunosorbent assay(ELISA) and quantitative Real-time polymerase chain reaction(qPCR) were used to detect the levels of inflammatory factors interleukin-6(IL-6), interleukin-1β(IL-1β), tumor necrosis factor-α(TNF-α) and the expression of related genes in adipose tissue of mice in each group, so as to evaluate the effect of nuciferine on chronic inflammation of mice in obese model group. qPCR was used to detect the expression of occludin and tight junction protein 1(ZO-1)gene in colon tissure, so as to evaluate the effect of nuciferine on intestinal permeability of mice in obese group. Nuciferine decreased the body weight of obese mice, Lee's index, weight percentage of inguinal subcutaneous fat(P<0.05), and reduced the volume of adipocytes, decreased the level of total cholesterol(TC), triglyceride(TG), and low density lipoprotein cholesterol(LDL-C)(P<0.05) in serum, improved dysbacteriosis, increased the relative abundance of Alloprevotella, Turicibacter, and Lactobacillus, lowered the relative abundance of Helicobac-ter, decreased the expression of inflammatory cytokines IL-6, IL-1β, and TNF-α genes in adipose tissue(P<0.01), decreased the levels of inflammatory cytokines IL-6, IL-1β, and TNF-α in serum(P<0.05), and increased the expression of occludin and ZO-1 genes related to tight junction in colon tissue(P<0.01). Nuciferine could treat obesity through modulating gut microbiota, decreasing gut permeability and ameliorating inflammation.
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Animals , Mice , Aporphines , Diet, High-Fat/adverse effects , Gastrointestinal Microbiome , Mice, Inbred C57BL , Mice, Obese , Obesity/geneticsABSTRACT
BCS Ⅱ drugs are characterized by low solubility and high permeability. Improving their solubility is considered an important approach to improve its oral absorption. Recent strategies to increase the solubility of poorly-soluble drugs may unexpectedly result in greatly depressed permeability, ultimately leading to failure in improving oral absorption. Based on the mathematics of membrane permeability coefficient of a drug, the membrane/aqueous partition coefficient is dependent on the drug's solubility in the gastrointestinal milieu, suggesting a unique interplay between the solubility and permeability of the drug, and treating the one irrespectively of the other may be insufficient. When we focus on the increase of drug solubility and overlook the efficacy of drug permeability, the positive effect of increased solubility to drug oral absorption might be traded off by depressed permeability. To provide rational formulary designs, by optimizing excipients and evaluation, this review summarizes solubility- permeability interplay for different types of solubilizing techniques, such as cyclodextrin, surfactants-based vehicle, cosolvent, amorphous solid dispersions, other infectors such as P-gp transporters and new techniques for simultaneous evaluation of drug solubility and permeability.
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Objective To research the difference of medicines prices in the new round of centralized purchasing from 10 provinces,and provide references for further perfecting centralized medicines procurement of provinces in China.Methods Based on the 2015 national sample hospital medicines procurement ranking list and the new round centralized procurement of every province,15 kinds of medicines are selected.By comparative studying,the difference of 15 medicines price among 10 provinces is analyzed.And the difference of prices between the domestic medicines and imported medicines in reference to WHO/HAl drug price standard survey method,the prices of medicines in each province and the international reference prices are analyzed.Results The medicine prices are different in different provinces.The medicines prices of Fujian Province are obviously lower than other provinces.The prices of a few imported medicines are obviously higher than those of domestic ones.Median prices ratios of some medicines exceed the reasonable range.Conclusion It is suggested that every province should refer to the useful experience of Fujian Province in medicines centralized procurement,to improve their centralized procurement plans.Every province should grant equal bids for imported patents,domestic generic drugs and original medicines,to make them have consistency bidding.The international reference price is incorporated into the price limit reference system,to make more reasonable price limit standard.
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Objective:To study the new round provincial medicines centralized bidding procurement policies,and to provide reference for the improvement of provincial centralized bidding procurement work.Methods:It collected the latest provincial centralized procurement documents after the publication of Guidance on Implementing Drug Centralized Purchasing in Public Hopitols and Announcement on the Guidance on Implementing Drug Centralized Purchasing in Public Hospitals.By using literature review,comparative analysis and experts consulting,it analyzed the content of centralized bidding procurement,summaried the differences of provincial medicines centralized bidding procurement work.Results:Progress of provincial centralized bidding procurement work was not the same.There were differences in quantity purchasing,price fixing regulations,the double envelope evaluation,and other aspects.Conclusion:It needed to implement layering price fixing regulation to reflect the quality difference of medicines.The price fixing range was determined based on the average of reference prices.It needed to set reasonable economic and technical indexes,determine winning medicines by cross-referencing the economic and technical score and price,increase the number of winning medicines to ensure supply of medicines.
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Objective To explore the effect of remind-to-move treatment on upper limb motor function,activities of daily living and participation in patients with subacute stroke. Methods From February,2016 to October,2017,45 patients with mild to medium upper limbs dysfunction after stroke were randomly assigned to control group(n=23)and experimental group(n=22).The control group accepted rou-tine occupational therapy,while the experimental group wore a wristwatch on the hemiplegic forearm to encour-age the predetermined training programs,for three weeks.They were measured with Fugl-Meyer Assessment-Up-per Extremity(FMA-UE),Function Independence Measurement(FIM),Motor Activity Log(MAL),and Stroke Impact Scale(SIS)before and after treatment. Results Both groups improved in part of the scores of three scales after treatment(P<0.05),and improved more in the experimental group than in the control group in scores of FMA-UE and FIM,and some sub-scores of MAL and SIS(t>1.183,P<0.05),with no significant difference in other indexes(P>0.05). Conclusion Remind-to-move treatment can promote the recovery of upper limb motor function,activities of daily living and participation in the patients with subacute stroke.
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BACKGROUND: Intestinal and lymphoid tissues constitute an important part of intestinal immunity, which plays an important regulatory role in spleen deficiency and hydronephrosis. OBJECTIVE: To observe the effect of acupuncture on T lymphocyte subsets in lymph nodes of rats with spleen deficiency, and to investigate the correlation of spleen deficiency with intestinal immunity and the mechanism of acupuncture for spleen deficiency syndrome. METHODS: Thirty-six female Sprague-Dawley rats were randomly divided into three groups: model, acupuncture and blank control groups. The rat model of spleen deficiency was established by fatigue-induced spleen injury plus abnormal diet for 31 days. Afterwards, the rats in the acupuncture group received acupuncture at Zusanli(ST 36).Urine D-xylose excretion rate was detected during modeling and treatment.Then, the mesenteric lymph nodes were removed, and the changes in T lymphocyte subsets in the mesentericlymph nodes were observed by immunohistochemistry. RESULTS AND CONCLUSION: Urine D-xylose excretion rate under spleen deficiency in the modeling and acupuncture groups was significantly lower than that in the blank control group (P < 0.05 or P < 0.01); after acupuncture, the urine D-xylose excretion rate was significantly increased compared with the modeling group (P < 0.01), but still lower than that in the blank control group (P < 0.05). The count of CD4+T lymphocytes, count of CD8+T lymphocytes and ratio of CD4+/CD8+T lymphocytes were ranked as follows: blank control group >acupuncture group>modeling group(P<0.01 or P<0.05).These results suggest that acupuncture at Zusanli can improve the urine D-xylose excretion rate, regulate the balance of T lymphocyte subsets in mesenteric lymph node of rats with spleen deficiency, thus improving the intestinal immune function, spleen deficiency systems, disorder of intestinal digestive function, intestinal digestion and absorption, as well as anorexia, loose stool, diarrhea and other symptoms of the digestive system.
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Objective: Kangxian Pills, containing Angelicae Sinensis, Chuanxiong Rhizoma, radix paeoniae rubra, and 12 other kinds of Chinese materia medica, have the functions of softening and dispersing blood stasis. It has been used for liver injury and liver fibrosis. The current study was designed to evaluate the anti-hepatic injury activity and the mechanism of Kangxian Pills on a CCl4-induced animal model. Methods: To induce chronic liver injury, mice were treated with CCl4 twice a week for four weeks. Kangxian Pills (6 or 12 g/kg) and Compound Biejia Ruangan Tablet (0.901 g/kg) were ig given to mice once daily for four weeks after CCl4 was withdrawal. The anti-hepatic injury activities and mechanisms of Kangxian Pills were assessed by hepatic histology and by measuring the levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), albumin (ALB), and total protein (TP) of serum as well as superoxide dismutase (SOD) and glycogen (Gn) of the liver. Results: Kangxian Pills significantly decreased the levels of liver index, ALT, and AST in mice liver injury models in treatment group. Moreover, Kangxian Pills and Compound Biejia Ruangan Tablet inhibited the CCl4-induced reduction of SOD and Gn levels in the liver. The histological study showed that Kangxian Pills could reduce cellular swelling and infiltration of inflammatory cells in liver injury. Conclusion: Kangxian Pills possess the potent abilities to alleviate chronic liver injury, suggesting that Kangxian Pills exert this effect by enhancing the anti-oxidant ability and metabolism of the liver.
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In this study, 120 patients with rheumatic heart disease undergoing valve replacement were randomly divided into the control group and the Qishen group, with 60 cases in each group. Before the operation, the control group was given routine heart and diuretic treatments and placebo of Qishen Yiqi dropping pills for seven days (0.5 g each time, three times a day); While the Qishen group was given Qishen Yiqi dropping pills for seven days (0.5 g each time after meal, three times a day) on the basis of the routine treatments. The right ventricular end-diastolic volume (RVEDV), end-systolic volume (RVESV), stroke volume (SV) and right ventricular ejection fraction (RVEF) were detected after the operation. The results showed that patients in the two groups showed significantly lower right ventricular end diastolic volume (RVEDV), right ventricular end systolic volume (RVESV) and stroke volume (SV) decreased than that before the operation, but with significantly higher Ejection fraction (RVEF) significantly than that before the operation. However, the Qishen group showed a significantly lower right heart function reduction than the control group, with the statistical significance in the differences (P < 0.05). This indicated that the pretreatment with Qishenyiqi Drop Pills showed a remarkable efficacy in the improvement of right ventricular function after valve replacement.
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Aged , Female , Humans , Male , Middle Aged , Cardiac Valve Annuloplasty , Drugs, Chinese Herbal , Heart Valve Diseases , Drug Therapy , General Surgery , Perioperative Care , Ventricular Function, RightABSTRACT
<p><b>OBJECTIVE</b>To report the experience of the surgical treatment of congenital heart diseases (CHD) in pediatric patients with body weight less than 10 kg.</p><p><b>METHODS</b>Between January 2000 and December 2007, 105 children with CHD, aged 2 months to 3 years and weighing between 3.5 to 10 kg, underwent surgical treatment. Of the 105 patients, 56 were concomitant with moderate to severe pulmonary hypertension or repeated pulmonary infections, and 35 with complex cardiac abnormalities. Operations were performed through median sternotomy with moderate hypothermic cardiopulmonary bypass in 88 cases, with normothermic extracorporeal circulation on beating heart in 14 cases, and with deep hypothermic circulatory arrest in 3 cases.</p><p><b>RESULTS</b>There were 5 early deaths (4.8%). During a follow-up of 2 month to 3 year, 97 survivors with corrective procedure had no late mortality or complications with NYHA class I of cardiac function, excepting 2 cases with little residual shunt. Three survivors with palliative procedure enjoyed higher quality of life.</p><p><b>CONCLUSIONS</b>The surgical treatment of CHD in pediatric patients with body weight less than 10 kg seems to be feasible and safe, with satisfactory early and long-term results.</p>