Lin, Guan-Yu; He, Ling-Juan; Yan, Yan; Wang, Duo-Duo; Zhuang, Kai-Zan; Zhu, Hong; Yang, Bo
Bendamustine is a multifunctional alkylating agent for the treatment of multiple myeloma, with the G2/M arrest-induction ability in human multiple myeloma RPMI-8226 cells, but the mechanism remains ambiguous. In this study, we found bendamustine caused the G2 arrest in 24 h, regulated the phosphorylation status of Cdc2, and blocked the nuclear import of Cdc2-CyclinB1 complex. Pretreatment with ATM/ATR inhibitor caffeine or p38 MAPK inhibitor SB203580 suppressed the phosphorylation of Cdc2 at Thr14/Tyr15 or attenuate the blockade of nuclear import, respectively; however, neither of these two inhibitors nor the combination imposed significant effects on Bendamustine-triggered G2 arrest. Bendamustine-induced blockade of the...
Yao, Qian; Gan, Liangchun; Hou, Shixiang; Guo, Xiaoqiang; Yan, Jun; Song, Qin; Gou, Xiaojun
The conventional method for preparing chitosan nanoparticles (CS-NPs) leads to the surface amino groups protonated and unable to link other useful moieties. In this study, we optimized the method of sodium chloride precipitation our lab established before to produce CS-NPs with surface free amino groups. The effects of preparation conditions on the size and encapsulation efficiency were examined. As surface amino groups may exert special effect on the NPs biodistribution, in vivo distribution was investigated after intravenous administration to the mice. The optimized CS-NPs were round with the mean diameter of 257 ± 21 nm. Compared with trans-resveratrol solution, the...
Yilmaz, Mehmet; Ozgeris, Fatma B.; Isaoglu, Unal; Cetin, Nihal; Turan, Mehmet I.; Suleyman, Bahadir; Gocer, Fatma; Suleyman, Halis
In this study, the impacts of adrenalin on ovarian injury caused by ischemia reperfusion were investigated in rats. In addition, it’s been investigated whether there is a correlation between adrenergic receptors and oxidant/anti-oxidant and COX1/COX-2 levels. It’s been observed that the COX-2 level that is responsible for MDA and inflammatory reaction (which are the indicators of oxidative stress in ovarian tissue to which ischemia reperfusion was applied) increased and the COX-1 levels that are responsible for GSH (an endogenic anti-oxidant with protective impact) were depressed. Adrenalin has prevented an increase in MDA and COX-2 activity in the ovarian tissue, to...
Liu, Yi; Ling, Xin; Gou, Lingshang; Fu, Xiaobin; Li, Sai; Lan, Nuo
The present study was designed to investigate the protective effects of luteolin, a flavonoid, against acute immobilization-induced liver damage in mice. Mice were immobilized for a period of 6 h daily for three consecutive weeks. Luteolin (25 or 100 mg/kg, i.g.) was administered 30 min before subjecting the animals to restraint stress (RS). Our experiment showed that RS could induce liver damage, with an increase in glutamic-pyruvic transaminase (GPT) and glutamic-oxaloacetic transaminase (GOT) in the liver tissue. Furthermore, the changes of anti-oxidative capacity in liver tissue were also measured. The changes of malondialdehyde (MDA), glutathione (GSH), superoxide dismutase (SOD) and...
Hao, Juan; Wu, Shanshan; Gao, Wenyuan; Man, Shuli; Huang, Luqi
The classical Chinese herbal formula Zha Chong Shi San Wei pill (ZCSSW) has been commonly used in traditional Chinese herbal medicine for hundreds of years to alleviate pain and inflammation. The anti-inflammatory effects of the ethanol extract were examined by using albumin egg-induce paw edema in mice assay and xylene-induced ear edema in mice method. Analgesic activity was evaluated by three models of acetic acid-induced writhing, formalin test and hot-plate test in mice. In addition, the total flavonoids (TF), total polysaccharide (TP) and total alkaloids (TA) in ZCSSWE were determined.
The result suggested that ZCSSWE possesses excellent anti-inflammatory activity as well...
Sellamuthu, Periyar S.; Arulselvan, Palanisamy; Muniappan, Balu P.; Fakurazi, Sharida; Kandasamy, Murugesan
The activities of membrane-bound ATPases and lysosomal hydrolases are altered in tissues of streptozotocin (STZ)-induced diabetic rats. Diabetes is stimulating the deterioration of membrane function and weakens the intracellular metabolism. The objective of the present study was to determine the effect of mangiferin, isolated from Salacia chinensis on membrane bound phosphatases and lysosomal hydrolases in the liver and kidney of STZ-induced diabetic rats. In our investigation, the levels of blood glucose and glycosylated haemoglobin were significantly increased in the diabetic rats. Moreover, membrane bound phosphatases and lysosomal hydrolases activities were ominously altered in the liver and kidney of STZ-induced diabetic...
Rajabalaya, Rajan; David, Sheba R.N.; Xian, Tan W.
The objectives of this study were to develop and characterize the matrix type transdermal drug delivery system (TDDS) of ondansetron hydrochloride (ODH). The matrix patch contains different ratios of Eudragit RS 100 and polyvinyl pyrrolidone (PVP) with different concentrations of plasticizer like triethyl citrate (TEC) and dibutyl sebacate (DBS) as well as vegetable oils such as linseed oil, castor oil and eugenol were added and prepared by solvent casting method. Thickness, tensile strength, drug content, moisture content and water absorption studies of the matrix patches were measured. The in vitro drug release and permeation studies were carried out in Franz...
Qiu, Xiangjun; Fei, Ai-li; Xu, Zhisheng; Du, Xiaoxiang; Xu, Ren-ai; Zhu, Haiyan
A sensitive and selective liquid chromatography–tandem mass spectrometry method (LC–MS/MS) for the determination of tolbutamide (TB) and its metabolite hydroxytolbutamide (HTB) in rat plasma was developed using carbamazepine as an internal standard. Chromatographic separation was performed by an Agilent Zorbax SB-C18 column (150 mmx2.1 mm, 3.5 μm), using the gradient elution of 0.1 % formic acid in water and acetonitrile. Calibration plots were linear over range of 5–1000 ng/mL for TB and 10–2000 ng/mL for HTB in rat plasma. The intra- and inter-day relative standard deviations of the assay were less than 10 % for both TB and HTB. The...
Chen, Jun; Hu, Rongrong; Yang, Xixiong; Tian, Rong; Gu, Wei; Chen, Zhipeng; Cai, Baochang
The aim of this study was to evaluate the effect of lactone ratios on the lactone/carboxylate equilibria of 9-nitrocamptothecin (9-NC) in vitro and in vivo. The interconversion of lactone and carboxylate forms of 9-NC was studied. Then the lactone ratio vs time profiles of these 9-NC solutions were further investigated in pH 7.4 PBS, rat plasma and blood. 9-NC solutions with different lactone ratios (lactone ratios=100 %, 75 %, 50 %, 25 % and 0 %, respectively) were obtained by modifying the pH of solution and it was found that the effects on lactone/carboxylate equilibrium were in the order: blood...
Zheng, Meiqin; Liu, Chunming; Fan, Yajun; Shi, Dongfang
The present study investigated the antidepressant-like effect of hyperoside extracted from Apocynum venetum leaves in mice using the tail suspension test (TST) and forced swimming test (FST).
Hyperoside administration at 10, 20 and 30 mg/kg (p.o.) for 10 days reduced immobility time in both tests.
This effect is dose-dependent without influencing the animals’ locomotor activity. Additionally, the monoaminergic mechanisms involved in the antidepressant-like effect of hyperoside in the mouse forced swimming test (FST) were evaluated. The results showed that hyperoside produced an antidepressant-like effect in the FST (10-30 mg/kg, i.g.) and in the TST (10–30 mg/kg, i.g.), without accompanying changes in ambulation...
Franco, Luis A.; Macareno, José L.; Ocampo, Yanet C.; Pájaro, Indira B.; Gaitán, Ricardo
The present study aimed to investigate the anti-inflammatory effect of marine sponges of the genus Neopetrosia which are abundant in the Colombian Caribbean. We obtained three fractions from a total methanolic extract of Neopetrosia rosariensis and proxima. In vivo activity was measured using λ-carrageenan-induced paw edema assay. The in vitro inhibitory effects were evaluated on myeloperoxidase activity (MPO) and nitric oxide (NO), prostaglandin E2 (PGE2), and tumor necrosis factor alpha (TNF- α) production. Total extracts of N. rosariensis and N. proxima (100 mg/Kg) significantly inhibited the paw edema of rats (71.74% and 60.06%, respectively). Dichloromethane and methanol fractions of Neopetrosia...
Castanheira, Liliana; Castro, Maria de Lurdes; Calheiros, José
The majority of patients submitted to surgical procedures are on chronic medication. Unfortunately, there are few outcome data about the majority of medications taken in the perioperative period and how clinicians manage chronic medication in this setting. All adult patients consecutively admitted for elective surgery at “Cova da Beira” Hospital Center were selected for the study. The study consisted of 929 patients submitted to elective surgery between September 2008 and July 2010. A total of 71.3 % were on chronic medication. The mean number of drugs taken was 2.4 ± 2.5(1-14). In logistic regression analysis both taking chronic medication and...
Chen, Zhibin; Zhu, Lihe; Zhen, Yangming; Li, Dan; Tang, Busheng; Chen, Wenhai; Hu, Lufeng
This study investigated the anti-proteinuric effect of sulodexide in rats with adriamycin (ADR) nephropathy. A total of 40 healthy male Sprague-Dawley (SD) rats were randomly assigned to four groups: normal control group (Control-group), ADR control group (ADR-group), sulodexide treatment group (SUL-group), and losartan treatment group (LOS-group). The ADR-induced rat models were established by injecting two different doses of ADR (4 and 3.5 mg/kg) into the caudal vein of rat for two consecutive weeks. After that, SUL-group and LOS-group were respectively treated with sulodexide (10 mg/kg/day) and losartan (10 mg/kg/day) for an additional 4 weeks period. Samples of 24-hour urine were...
Murtaza, Ghulam; Rehman, Nisar-ur; Khan, Shujaat A.; Noor, Tahira; Karim, Sabiha; Bashir, Deeba; Bibi, Shumaila; Kaleem, Saman
This study set sights at the issue of predominance of the attitude and behavior of self medication, medication storage and self treatment among female students of a Pakistani university. Random sampling and cross sectional surveys were conducted after collecting the data with the help of a questionnaire
that was circulated amongst students. Of the 450 participants, 78.74 % of students admitted that they
store medicines with them while other 50.95 % of students replied that they stop taking medicine prescribed by their doctors with the doctor’s intimation. The 78.74 % females were involved in self-medication. The 21.98 % were of the opinion...
Rorig, Ketily D. V.; Oliveira, Cibeli L. de
This study aims to evaluate the implementation and operation of a pharmacovigilance program in the pharmaceutical industry in Brazil, taking as a tool a questionnaire with closed questions. The survey was carried out between the second quarter of 2009 and the first quarter of 2010. From 181 pharmaceutical companies that received the questionnaire, 7.18 % did not answer, but reported that they did not have a pharmacovigilance program or said that it was confidential company information, 27.62 % have contributed to the survey by answering the questions. Of these, 82 % said they already have a program of pharmacovigilance and...
Manchini, Martha T.; Boiati, Raphael F.; Sousa, Dannylo W.N.; Batista, Jorge G.; Malaguti, Carla; Silva Junior, José A.; Nascimento, Jorge W.L.
This study evaluated the effect of prednisolone on acute lung inflammatory response, tissue damage and nitric oxide in elastase-induced emphysema in rats. A total of 32 male rats were divided into four groups: control and prednisolone groups received intratracheal instillation of saline; emphysema and emphysema + prednisolone groups received elastase. Prednisolone was administered in prednisolone and emphysema + prednisolone groups for 25 days by gavage. The results showed a significant increase in the alveolar airspace enlargement in the emphysema group. However, comparing control and emphysema + prednisolone groups, the treatment did not show significant reduction in the alveolar airspace enlargement....
Barik, B. B.; Dewani, Sunil P.
In order to reduce the recrystallinity of poorly insoluble drug nelfinavir, PEG 6000 blends
were prepared by spray drying with HPMC. The maximal reduction of recrystallinity in PEG 6000 was
obtained by co-spray drying with HPMC as revealed by in vitro dissolution studies. The resulting ternary
solid dispersions containing nelfinavir were characterized. The results of this study show that addition of
PEG 6000 to nelfinavir/HPMC system leads to extended release of nelfinavir that in most cases recrystallizes indicated by reduction in solubility. For all ternary dispersions containing 20 % of nelfinavir, the
drug was highly amorphous and dissolution was improved compared to binary 20/80 w/w
Silveira, Alessandro C.O.; Claudino, Vanessa D.; Yunes, Rosendo Augusto; Cechinel Filho, Valdir; Malheiro, Angela; Cordova, Caio M.M.; Bella Cruz, Alexandre
Men have used medicinal plant properties to treat infectious diseases. Both the rise of emerging infectious diseases as the microbial resistance problem has stimulated the searching for new antimicrobial agents. This study evaluated the antibacterial activity and toxicity of crude extracts, fractions and pure compounds from Drimys brasiliensis. The antibacterial activity of five extracts, twelve fractions and five isolated compounds were tested against six Gram-positive and seven Gram-negative bacteria. The methodology used was agar dilution. The extract potential toxicities were evaluated using Artemia salina assay. Antibacterial activity tests showed some promising results, such as bark chloroform extract with minimum inhibitory...