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Sulfated polysaccharides are with hydroxyl group containing sulfate radicals, which can be obtained by natural extraction or chemical modification of sulfation. Recent studies have shown that sulfated polysaccharides exhibit different levels of antitumor activ-ity, especially in comparison with those before chemical modification; therefore, they have attracted wide attention. This article briefly reviewed the domestic and foreign researches on the antitumor effects of natural sulfated polysaccharides and chemical synthesized sul-fated polysaccharides in recent years.
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Objective:To investigate the transport mechanism of punicalagin in MDCK monolayer model .Methods:The safe con-centration of punicalagin in MDCK cells was determined by CCK8 assay.Millicell -ERS was used to measure cell monolayer TEER value to determine the integrity of the cell monolayer .The effects of direction , drug concentration , time, P-gp inhibitor and EDTA-Na2 on the absorption and transport of punicalagin were studied systematically .And then the drug concentration was analyzed by HPLC to calculate the apparent permeability coefficient (Papp) and efflux ratio(ER).Results: Punicalagin transport in MDCK cells was time and concentration dependent .Punicalagin showed poor absorption in MDCK cells .Papp from apical to basolateral side ( AP-BL) within the concentration range of 100-300μg· ml-1 was (6.13 ±0.12) ×10 -7 cm· s-1 , (6.96 ±0.26) ×10 -7 cm· s-1 and (5.94 ±0.10) ×10 -7 cm· s-1 , respectively .P-gp inhibitor and EDTA-Na2 could significantly increase the transport of punicalagin in AP-BL direc-tion, while the transport decreased at 4℃.Conclusion:The transport mechanism of punicalagin might be passive diffusion as the dom-inating process involving active transportation .Punicalagin is one of P-gp substrates with exocytosis and absorbed via the paracellular route.
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Objective To observe the clinical effect of ropivacaine erector spinae plane block assisting general anesthesia in lumbar spine surgery. Methods A total of 60 cases of male patients with selective lumbar spine surgery under general anesthesia were chosen and randomly divided into control group(group C) and erector spinae plane block group(group E) (n= 30).Group C was directly treated with total intravenous anesthesia.In group E,the erector spinae were blocked with 0.375%ropivacaine before skin incision.The patient's vital signs during operative period were recorded,as well as the operation time, anesthesia time,drug dosage and satisfaction of muscle relaxation.Postoperative VAS scores at 4,8,24 and 48 h were recorded. Remedied analgesic drug use,the number of PCIA press,complications such as nausea and vomiting,patients' satisfaction degree within 48 h of postoperative were all recorded. Results There were no statistical difference in the vital signs,operation section, operation time,anesthesia time and postoperative complications(all P>0.05) in two groups. Compared with group C,the dosage of propofol,rifentanyl and benzene sulfonate in group E were significantly reduced.In group C and group E,dosage of propofol was(1 526.2±134.5) mg and(1 305.8±212.8) mg;dosage of remifentanil was(2 452.2±232.5) μg and(2 076.8±311.6) μg; dosage of benzene sulfonate was(31.8±4.2) mg and (22.3±5.1) mg]( P<0.05 or P<0.01).Satisfaction of muscle relaxation in the operation area of group E was significantly increased(P<0.05).The VAS scores at 4 h and 8 h after operation in group E were all significantly reduced(P<0.01).In group E,the frequency(or total) of remediation analgesic drugs usage and PCIA compressions times were significantly reduced in 48 h after surgery(P<0.01).The satisfaction degree of the patients in group E was significantly increased(P<0.01). Conclusion Ropivacaine erector spinae plane block assisting general anesthesia in lumbar spine surgery can reduce perioperative general anesthesia drug dosage,the number of postoperative remediation of analgesic drugs,PCIA compressions times,and can improve satisfaction of operative doctors and patients with anesthesia.
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Objective: To confirm the structure and preferential conformation of the Schiff base of gossypol with 1, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine and explore its anti-HIV-1 activity.Methods: The Schiff base of gossypol with 11, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine was synthesized and identified by FT-IR, NMR spectroscopy and the PM6 semi-classical calculation.The inhibitory activity of the novel compound against the laboratory-adapted HIV-1IIIB strain was examined using the HIV-1IIIB/TZM-bl indicator cell culture system.Results: The 1H and 13C-NMR signals of the new Schiff base were assigned.The PM6 semi-classical calculation indicated that enamine-enamine tautomeric form of the new Schiff base was more stable,which was stabilized by the intramolecular hydrogen bonds.The anti-HIV-1 test showed that the compound could block the entry of HIV-1IIIB into the target cells.Conclusion: The Schiff base of gossypol with 1, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine exhibits enamine-enamine tautomeric form in solution, which shows potential anti-HIV-1 activity.
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Objective:To study the effect of tannins from Pericarpium Granati on hepatic microsomal enzyme in rats. Methods:Thirty Wistar rats were randomly divided into five groups:the blank control group, high, medium and low dose groups of tannins from Pericarpium Granati, the positive control group of phenobarbital sodium. The blank control group was given physiological saline. The three different doses groups were respectively given tannins from Pericarpium Granati orally at the dose of 150,100 and 75 mg·kg-1 · d-1 for 7 days. The positive control group was given phenobarbital sodium 80 mg·kg-1 ·d-1 with intramuscular injection for 5 days. At the end of the experiment, the activity ofⅠandⅡphase metabolic enzymes in liver microsomes of each group was determined by UV. Results:Compared with the blank control group, the high, medium and low dose groups of tannins from Pericarpium Granati could sig-nificantly decrease the content of CYP 450 and CYPb5, and inhabit the activity of ADM (P<0. 01);the high and medium dose group could significantly inhibit ERD enzyme activity (P<0. 01);the high dose group could significantly reduce GST enzyme activity (P<0. 01). Conclusion:Tannins from Pericarpium Granati has notably inhibitory effect on hepatic microsomal enzyme in rats, which can reduce the expression of CYP3A and CYP2E1 in a dose-dependent manner.
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Objective:To study the in vitro transdermal permeability of nifedipine nanoemulsion ( NFNE) containing different per-meation enhancers to lay foundation for the development of transdermal nifedipine preparation. Methods: Franz diffusion cells were used to study the transdermal enhancement of NFNE with different transdermal enhancers ( Azone, oleic acid, TMC20, TMC40, TMC60). Results:The in vitro transdermal effect of NFNE was better than that of nifedipine (NF). The order of in vitro transdermal permeation enhancement was as follows: azone > oleic acid > TMC60 > TMC40 > TMC20, while the water-soluble transdermal permeation enhancers had faster effect. Conclusion:For NFNE, fat-soluble transdermal permeation enhancers have better effect.
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Objective:To compare the effect of lightwand guided tracheal intubation in difficult airway between waking state and intravenous anesthesia induced state. Methods:According to the random number table, 78 cases of difficult airway patients were di-vided equally into waking group and intravenous anesthesia induction group . The changes of vital signs, the time of tracheal intubation and the extubation complications after 1 h were compared between the groups. Results:Compared with the corresponding values of the waking group, the blood pressure and heart rate before and after the tracheal intubation significantly increased in the intravenous anes-thesia induction group (P<0. 05 or P<0. 01). In the same group, the blood pressure and heart rate increased significantly after the tracheal intubation when compared with those before the treatment (P<0. 05 or P<0. 01). Compared with that in the intravenous an-esthesia induction group, the time of tracheal intubation was significantly shorter in the waking group (P<0. 01), and the 24h postop-erative anesthesia satisfaction was improved significantly (P<0. 05). Conclusion: Compared with intravenous anesthesia induction, waking lightwand guided tracheal intubation in the patients with difficult airway has more advantages.
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ABSTRACT Ellagitannin is a complex compound of plant polyphenols, and it is an effective substance in many commonly used natu-ral drugs. Ellagitannin has been widely used in medicine, cosmetics, food, health care products and the other fields. The article re-viewed the structure source, biological activity and metabolic outcomes of ellagitannin in order to provide basis for the in-depth resear-ches and the resource development of natural medicines rich in tannins.
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ABSTRACT Ellagitannin is a complex compound of plant polyphenols, and it is an effective substance in many commonly used natu-ral drugs. Ellagitannin has been widely used in medicine, cosmetics, food, health care products and the other fields. The article re-viewed the structure source, biological activity and metabolic outcomes of ellagitannin in order to provide basis for the in-depth resear-ches and the resource development of natural medicines rich in tannins.
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Objective:To investigate the clinical application of fibrinogen (FIB) in a certain hospital to enhance the rational use in clinics.Methods:A retrospective investigation was adopted to analyze the clinical application of FIB in a certain hospital in 2016. Results:Totally 489 inpatients were treated with FIB in 2016,and among them,243 cases were surgery patients and another 246 ones were non-surgery patients. The main involved departments were cardiovascular surgery,cardiovascular medicine,emergency,intensive medicine,gynaecology and obstetrics, gastroenterology and neurosurgery. The rationality of indication was 80.0% (391/489), and the non-indication use mainly existed in cardiovascular surgery and cardiovascular medicine departments. Among the 391 cases with in-dication,3 cases were with improper compatibility,17 cases with low dosage, and the irrationality of usage and dosage was 17.9% (20/391). Conclusion:The clinical application of FIB is basically rational in the hospital,while non-indication use still exists during the perioperative period in cardiovascular and cerebrovascular surgery,and nonstandard usage and dosage appear in clinics from time to time. The prescription comment on blood products such as FIB should be enhanced in order to improve the rational use in clinics.
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Objective To investigate the diagnostic value of ultrasonography and CT in the diagnosis of adrenal tumors,and to provide reference for clinical diagnosis of tumors in the future.Methods 86 cases of adrenal tumor in our hospital from July 2013 to February 2016 were retrospectively reviewed.All the patients were examined by ultrasonography and CT.The characteristics of different types of adrenal tumors were observed and analyzed,and the diagnostic accuracy was compared between the two methods.Results The coincidence rate of CT diagnosis (93.02%)was higher than that of ultrasonic imaging(84.88%),but the difference was not statistically significant (χ2 =2.899 2,P >0.05).Conclusion The coincidence rate of ultrasound imaging and CT are higher in adrenal tumors,and has significant value in clinical application,should be based on the imaging of a gradient,into the imaging system,the formation of a simple,practical and economical examination method to achieve the best diagnosis effect.
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Objective:To study the pharmacokinetic parameters of gastrodin nasal in situ gel ( ISG) with the base of TMC-P407-P188-carbomer, and evaluate its brain-targeting ability preliminarily. Methods:Rats were used as the model animals. The experiment group was treated with gastrodin nasal in situ gel, and the control group was treated with gastrodin solution with intravenous administra-tion. The plasma sample and brain tissue ( cerebrum and cerebellum) were taken out at the predetermined time points, and the concen-tration of gastrodin in plasma and gastrodigenin in brain tissues were determined by HPLC to draw the curve of concentration vs time. The pharmacokinetic parameters such as MRT and AUC were calculated by 3P97 software. The bioavailability F (%) and the brain-targeting index BTI were compared between the groups. Results:The concentration of gastrodigenin in the brain tissues of grastrodin in situ gel was higher than that of gastrodin solution with intravenous administration (P<0. 05). AUC of cerebrum and cerebellum both increased significantly with BTI of 2. 38 and 1. 93, respectively. MRT increased by nearly two-fold in the gel group when compared with that in the control group, and F(%) increased significantly in cerebrum and cerebellum as well. Conclusion:Gastrodin nasal in situ gel with the base of TMC-P407-P188-carbomer has promising effectiveness. Meanwhile, it can improve the brain-targeting ability of gastrodin with sustained release.
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Objective:To study the in vitro and in vivo transdermal penetration of testosterone undecanoate ( TU) binary ethosomes gel. Methods:TU binary ethosomes were prepared by an ethanol injection method, and using carbopol 941 as the gel base, TU binary ethosomes gel was prepared. Using mouse skin as the barrier, Franz cells were applied to explore the in vitro transdermal penetration of TU binary ethosomes and the gel. Rats were used as the animals, and TU binary ethosomes and the gel was respectively administrated on the back skin. At the predetermined time points, plasma samples were withdrawn to detect the concentration of TU, and the main pharmacokinetics parameters were calculated. Results: The in vitro transdermal penetration of TU binary ethosomes and the gel was both fitted first-order equation:Q=8. 68t+6. 78(r=0. 998 2) and Q=6. 09t+3. 09(r=0. 999 3), and the stable penetration rate was 8. 68 μg·cm-2 ·h-1 and 6. 09μg·cm-2 ·h-1 , respectively. After the 24-hour penetration, the residual amount in skin of TU binary ethosomes and the gel was (208. 80 ± 55. 26)μg·g-1 and (225. 60 ± 38. 90)μg·g-1 , respectively. The main pharmacokinet-ics parameters of TU binary ethosomes and the gel were Cmax of(18.50 ±2.75)mg·L-1 and(20.80 ±2.42)mg·L-1, tmax of(6.20 ± 0. 14)h and(9. 54 ± 0. 52)h, and AUC0-48h of(336. 74 ± 2. 05)h and(486. 30 ± 1. 68)h. Conclusion:TU binary ethosomes and the gel both exhibit promising in vitro transdermal penetration, and the gel shows better sustained release property.
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Objective:To investigate the application of Xingnaojing injection ( XNJI) in the patients of neurosurgery department to provide reference for the rational drug use. Methods:The retrospective investigation was applied to survey 200 hospitalization records with XNJI from a certain hospital between January 2014 and June 2015. The usage, dosage, medication purpose, course of treatment, compatibility and adverse effects of XNJI were analyzed. Results:The unlabeled use of XNJI was found in neurosurgery department, and 34. 50% of the surveyed patients were found that their diagnoses didn’t conform to the indications in the medicine specification of XNJI. Moreover, 92. 50% of the inpatients were treated with overdose and almost 90. 00% were treated with single drug dose of 40 ml. It was also found that XNJI was often combined with potassium chloride or with potassium chloride plus insulin in clinical use. Conclu-sion:There is some irrational use of XNJI in clinics, thus the use and management of traditional Chinese medicine injections should be strengthened and regulated.
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Objective:To screen the best base for gastrodin nasal in situ gel ( ISG) to lay foundation for the development of gastrodin new preparation .Methods:Two bases were chosen , one was the combination of N-trimethyl chitosan ( TMC) , polyethylene glycol 4000 (PEG4000) and glycerophosphate (GP), and another was the combination of TMC, poloxamer 407 (P407), poloxamer 188 (P188) and carbomer.With the nasal cavity temperature of 35℃as the test temperature, the gelling time of the two bases was determined to screen the optimal ratio.Furthermore, gastrodin was added into the two bases , and the gelling time was determined to choose the suitable base for the drug.Results:The base of TMC-PEG4000-GP couldn’t gel in the nasal cavity temperature when combined with gastrodin , while the base of TMC-P407-P188-carbomer could gel quickly when combined with gastrodin .Conclusion:TMC-P407-P188-carbomer can be used as the base for gastrodin nasal in situ gel .
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Objective:To investigate the anti-tumor effect of different extracts of Tricholoma matsutake Sing. in vitro. Methods:MTT method was employed to study the inhibitory effect of ethanol extracts from different parts of Tricholoma matsutake Sing. and the polysaccharides extracts on HepG-2 cells, MCF-7 cells and Hela cells. FCM assay was used to detect HepG-2 and Hela cell apoptosis induced by the polysaccharides extracts. Results:The polysaccharides extracts of Tricholoma matsutake Sing. could inhibit the prolif-eration of the three tumor cells with IC50 of 53. 77 μg·mL-1(HepG-2), 40. 04 μg·mL-1(Hela) and 100. 65 μg·mL-1(MCF-7), respectively. The inhibitory effect of the polysaccharides extracts showed a time-and dose-dependent manner. The tumor cell apoptosis could be induced by the polysaccharides extracts. Conclusion:The maln anti-tumor effective extracts of Tricholoma matsutake Sing. in vitro is the polysaccharides extracts, which show significant anti-tumor activities in vitro and can induce tumor cell apoptosis.
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Objective:To explore the interaction between gossypol and human serum albumin ( HSA) . Methods:The interaction of gossypol and HSA under physiological conditions was studied by fluorescence spectroscopy, and the molecular docking software was used to simulate the interaction. Results:The binding constant of gossypol and HSA at 293K and 303K was 2. 390 6 × 105 L·mol-1 and 3. 576 8 × 103 L·mol-1 , respectively. There was one binding site on HSA for gossypol. Hydrogen bond and Van Der Waals inter-actions were involved in the binding process. The binding of gossypol and HAS was closer to tyrosine residue in HSA. The molecular simulation analysis verified the above results. Conclusion: The gossypol-induced fluorescence quenching of HSA belongs to a static quenching procedure.
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Objective:To investigate the entry point of clinic pharmaceutical care performed by clinical pharmacists in diabetic ne-phropathy patients with chronic renal insufficiency. Methods: Clinical pharmacists played an important role in the service of clinical pharmacy by doing pharmaceutical care in main treatment agents such as hypoglycemic agents, hypotensive drugs and symptomatic treatment agents including diuretics, lipid-lowering drugs and microcirculation improving drugs, and in the healthy diet education for the patients. Results:Clinical pharmacists improved the compliance of the patients and the trust in clinical pharmacists, which en-sured the safety and efficacy of clinical drugs. Conclusion:Clinical pharmacists can guarantee the safety of medication and delay the development of diabetic nephropathy with chronic renal insufficiency.
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Objective: To provide some experience and help for the pharmaceutical care for drug-induced acute kidney injury through analysis and pharmaceutical care performed by clinical pharmacist for two cases of drug-induced acute kidney injury. Meth-ods:Clinical pharmacist analyzed the mechanism of drug-induced acute kidney injury, provided some suggestions for the medication, helped doctors select hormone drugs reasonably and performed medical education in the patients. Results:The kidney function of the two patients was recovered during the hospitalization after the reasonable treatment and care by doctors and pharmacists. Conclusion:The drug-induced acute kidney injury should be paid high attention, and the medical education should be strengthened in the patients.
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Objective:To explore novel compounds with anti-EV71 activity. Methods: A series of oligopeptides were designed based on the active groove of the EV71 3C protease using molecular simulation technology. Furthermore, some oligopeptides were syn-thesized and tested for the inhibition ability against EV71 in vitro. Results:Pentapeptides had higher binding affinity to the EV71 3C protease than the other oligopeptides, such as compounds 25 and 16. Therefore, compounds 25 and 16 were synthesized and tested in vitro for the anti-EV71 activity, and compound 25 exhibited potent anti-EV71 activity(EC50 =1. 36 μmol·L-1, CC50 =211. 94 μmol ·L-1, SI=155. 84), while compound 16 had no evident effect on EV71. Conclusion: It is worthy of further investigation on com-pound 25 as a novel scaffold of anti-EV71inhibitor.