bluuebunny/crossref_metadata_2025_split huggingface dataset:
Formulation, characterization and wound-healing potential of emulgel and in-situ gel containing root extract of <i>Saussurea lappa Clarke</i> (Asteraceae)
Authors: Ahsan Aitazaz , Miana Ghulam A. , Naureen Humaira , Rehman Masood U. , Anum Kamil , Malik Imran 
Published: June 2020

Purpose: To investigate the wound-healing potential of herbal formulations (emulgels and in situ gels) containing Saussurea lappa root extract (SLRE) via excision wound induction in albino rats.
Methods: Preliminary phytochemical analysis of the methanol extract of roots of Saussurea lappa (SLRE) was performed using standard procedures. In vitro anti-inflammatory assay of SLRE was conducted using heat-induced hemolysis method at a concentration of 100 μg/mL. Acute toxicity of SLRE was also evaluated in mice at a single dose of 1000 mg/kg for 24 h. Emulgels and in situ gels were prepared using different concentrations of SLRE and assessed for their organoleptic and physical properties. In vitro drug release studies of the prepared formulations were carried out by Franz diffusion cell and the data fitted into various pharmacokinetic models. Wound healing was assessed using excision wound induction (380 mm2) on dorsal surface of male albino rats. Each formulation (F4, F5, F6, G1, G2 and G3) and pyodine gel (standard) were applied topically (0.5 g) for 20 days. Wound contraction was measured every fourth day.
Results: SLRE showed 42.8 % inhibition in heat-induced hemolysis on erythrocyte membrane model, compared to aspirin (positive control). Moreover, SLRE did not cause mortality in mice at the given doses. All the formulations were stable after one month stability check at 40 °C for emulgels and at 25 °C for in situ gels. All the formulations followed first order drug release pattern. In situ gel (G3) exhibited better wound healing (100 ± 0.0028) than emulgel (F6, 99 ± 0.004) containing 5 g extract and standard pyodine gel (91 ± 0.014, p <0.05).
Conclusion: The results indicate that in situ gel of SLRE exhibits significant wound healing in rats. Thus, the findings present a strategy for the formulation of gel products with better wound healing potentials.
Keywords: Saussurea lappa, Wound healing, Emulgel, In situ gel, Herbal formulation
Farrerol ameliorates diabetic hepatopathy in rat model of type 2 diabetes mellitus via modulation of oxidativeinflammatory stress
Authors: Dong Li , Yang Lixia , Liu Fengsui , Zhan Haitao , Chen Xinwei 
Published: June 2020

Purpose: To investigate the effect of farrerol on diabetic hepatopathy in a rat model of type 2 diabetes mellitus (T2DM).Methods: Adult male Wistar rats (n = 40) were randomly assigned to four groups of ten rats each: normal control, diabetic control, farrerol control and treatment groups. With the exception of normal control and farrerol control groups, the rats were fed high-fat diet (HFD) for four weeks, and thereafter injected streptozotocin (STZ) at a dose of 30 mg/kg body weight intraperitoneally (i.p.) for induction of T2DM. Rats in farrerol control and treatment groups received 50 mg/kg farrerol orally/day. Serum levels of triacylglycerol (TG), total cholesterol (TC), high-density lipoprotein cholesterol (HDL-C) and lowdensity lipoprotein cholesterol (LDL-C) were determined. Superoxide dismutase (SOD) activity and malondialdehyde (MDA) levels were assessed in liver homogenate while mRNA and protein expressions of glucose transporter 2 (GLUT2) were assayed in liver using real-time quantitative polymerase chain reaction (qRT-PCR) and Western blotting, respectively. Expression levels of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) were also determined using qRT-PCR.Results: Diabetes mellitus (DM) led to significant reductions in rat body weight and SOD activity, while increasing fasting blood glucose (FBG) and MDA levels (p < 0.05). However, treatment with farrerol significantly reversed the effect of DM on these parameters (p < 0.05). The mRNA expressions of TNF-α and IL-1β were significantly higher in diabetic control group than in normal control group, but were significantly reduced after farrerol treatment (p < 0.05). Treatment with farrerol also significantly reversed the effect of DM on rat lipid profile (p < 0.05). The expression of GLUT2 protein was significantly downregulated in the liver of diabetic control rats, when compared with normal control rats, but was significantly upregulated after treatment with farrerol (p < 0.05).Conclusion: The results of this study show that farrerol alleviates STZ-induced hyperglycemia and dyslipidemia via reduction in oxidative stress and inflammation, and upregulation of GLUT2 protein expression. Thus, farrerol has antidiabetic and hepatoprotective potentials for clinical use in humans.
Keywords: Diabetes mellitus, Dyslipidemia, Farrerol, Hepatopathy, High-fat diet
Effects of mTOR inhibitor, everolimus, on proliferation, autophagy and temozolomide sensitivity of glioma cells
Authors: Dong Wei , Wang Jialiang , Liu Haipeng , Sun Shuo , Wang Yanbin 
Published: June 2020

Purpose: To study the effect of the mTOR inhibitor, everolimus, on glioma cell proliferation, autophagy, and drug sensitivity to temozolomide (TMZ).Methods: Human glioma cell lines were cultured in vitro, and the effects of different concentrations of everolimus on the proliferation of brain glial cells were determined using CCK-8 method. The effect of different concentrations of everolimus on brain glial cell levels of autophagy protein were assayed by western blot method.Results: The results of CCK-8 analysis showed that everolimus inhibited the proliferation of glial cells in a time- and concentration-dependent manner. Western blot results showed that the expression levels of autophagy proteins, LC3-II and LC3-II/I, were gradually and concentration-dependently up-regulated, while p62 protein level was gradually decreased concentration-dependently, when compared with blank control (p < 0.05). Treatment with different concentrations of TMZ alone, and in combination with everolimus for 48 h inhibited the proliferation of brain glial cells in a concentration-dependent manner, but the inhibition due to TMZ-everolimus combination was significantly higher than that of TMZ singletreatment (p < 0.05). After 48 h, the expression level of Beclin-1 increased with the ratio of LC3-II/LC-I in TMZ-everolimus group, while the expression level of p62 decreased, when compared with TMZ alone, or control (p < 0.05).Conclusion: Everolimus significantly inhibits the proliferation of glioma cells and promotes the occurrence of autophagy. Combined use of TMZ and everolimus significantly enhances the sensitivity of TMZ to glioma cells, inhibits cell proliferation, and promotes autophagy better than TMZ alone.
Keywords: mTOR inhibitor, Everolimus, Glioma cells, Proliferation, Autophagy
Compound xiebai capsule alleviates pulmonary vascular remodeling in monocrotaline-induced pulmonary arterial hypertension in rats
Authors: Wu Zhouye , Xi Zhaoqing 
Published: June 2020

Purpose: To investigate the effect of compound xiebai capsule (CXC) on pulmonary arterial vascular remodeling in a rat model of monocrotaline-mediated pulmonary arterial hypertension (PAH).Methods: PAH model was established through intraperitoneal injection of MCT (60 mg/kg) to male Sprague-Dawley rats. Thereafter, the rats were grouped and treated with saline (control), nifedipine at a dose of 0.02 g/kg/day (positive control), or different doses of CXC (0.67, 1.00 and 1.32 g/kg/day). The effect of treatments on PAH were determined by measurement of hemodynamic indices and right ventricular hypertrophy index (RVHI). Pathological features and ultrastructure of the lung tissue were examined by H & E staining and transmission electron microscopy (TEM). Immunohistochemistry was employed to determine the expressions of proliferation-associated protein and proliferating cell nuclear antigen (PCNA). Western blotting was applied to assay the expressions of apoptotic pathway proteins.Results: CXC treatment decreased the levels of hemodynamic parameters in PAH rats, alleviated RVHI, improved pulmonary vascular remodeling, decreased vascular wall thickness and area (WT and WA), downregulated the expression of PCNA, and enhanced the expressions of apoptosis-related proteins (cytochrome C, caspase-3, and caspase-9).Conclusion: This is the first study to investigate the effect of CXC on vascular remodeling in PAH. The results indicate that CXC markedly reversed the deleterious changes in PAH-induced rat model.
Keywords: Pulmonary arterial hypertension, Pulmonary vascular remodeling, Caspase, Cytochrome C, Apoptosis, Compound xiebai capsule
Radioprotective and anti-diabetic effects of <I>Costus speciosus</I> and carnosine
Authors: Marzook Ebtisam A. , Marzook Fawzy A. , Abd El Moneim Ahmed E. 
Published: June 2020

Purpose: To evaluate the possible radioprotective effect of Costus speciosus and carnosine as natural antioxidants in order to control the hyperglycemia developed in male albino rats exposed to acute oxidative stress induced by gamma radiation.
Methods: Twenty-eight adult male albino rats were divided into four groups. The first group was taken as a control group, while the three other groups were exposed to Ɣ irradiation at a single 7.5 Gy dose. Furthermore, the rats in the second and third groups were i.p. injected with Costus speciosus root powder and carnosine, respectively. On the 3rd day, after irradiation, the serum levels of glucose, insulin, C peptide, copper, iron, calcium, total antioxidant capacity (TAC) and malondialdehyde (MDA) were measureded.
Results: The results revealed that exposure to Ɣ irradiation induced significant increases in serum glucose, iron, and malondialdehyde. However, the levels of serum calcium, copper, total antioxidant capacity and insulin significantly decreased (p < 0.05). A significant decrease was observed in Cpeptide in the exposed group, compared to control group. All the test parameters indicate improvement after treatment with Costus speciosus and carnosine (p < 0.05).
Conclusion: Costus speciosus and carnosine ameliorate the effect of gamma radiation, indicating their role as antidiabetic agents and radioprotectors; however, Costus speciosus was critically more efficient than carnosine.
Keywords: Costus speciosus, Carnosine, Diabetes, Insulin, Gamma radiation protection
Potentiation of raloxifene cytotoxicity against MCF-7 breast cancer cell lines via transdermal delivery and loading on self-emulsifying nanoemulsions
Authors: Aldawsari Hibah M. , Negm Aya A. 
Published: June 2020

Purpose: To enhance raloxifene (RLX) delivery and cytotoxicity against breast cancer (MCF-7) cell lines.
Methods: This was a solubility study of RLX in different oils, surfactants, and co-surfactants. Twelve formulae were tested to reach the smallest globular size, and hydroxypropyl methylcellulose, (HPMC), and Carbopol 947 polymers were tested for formation of transdermal films. The formula with the lowest size was compared with raw RLX in diffusion studies using a Franz diffusion cell. Finally, a cytotoxicity study against MCF-7 breast cancer cell lines was conducted.
Results: The maximum solubility of RLX was in Tween 80, peppermint oil, and PEG 200; therefore, these were the main components of the 12 formulations. The release of RLX loaded on the selfnanoemulsion drug delivery system (SNEDDS) was increased 3-fold compared with raw RLX.Cytotoxicity results revealed that RLX SNEDDs decreased MCF-7 cell survival by approximately 40 %, compared with raw RLX (control), which augmented the RLX suppression of breast cancer cell lines.
Conclusion: Improvement in RLX cytotoxicity is a novel strategy to suppress breast cancer.
Keywords: Raloxifene, Osteoporosis, Bioavailability, Nanoemulsion, Nanoparticles
Synthesis, characterization and evaluation of antiinflammatory properties of novel α, β-unsaturated ketones
Authors: Alrubaie Leaqaa A. , Muhasin Raheem J. , Mousa Mazin N. 
Published: June 2020

Purpose: To prepare and characterize alicyclic aromatic chalcone derivatives, and study their antibiotic and anti-inflammatory properties.Methods: Claisen-Schmidt (aldol condensation) base-catalyzed condensation was used for preparation of chalcone derivatives (compounds I - IV), and the products were characterized using ultraviolet-visible spectroscopy (UV), FT-IR spectroscopy, proton nuclear magnetic resonance (1H-NMR), carbone 13CNMR and mass spectroscopy (MS). The antibacterial effect of the compounds was determined against Baci. cereus, Staph. Aureus, E. coli, and Pseudomonas Aeruginosa. In addition, their anti-inflammatory effects were assayed using cotton granule-induced granuloma in mice. The results were compared with those for diclofenac, a standard drug. The synthesized derivatives were subjected to theoretical studies on their stabilities, and some chemical parameters were calculated using density function theory [DFT].Results: Using Claisen-Schmidt reaction, it was possible to prepare stable chalcone derivatives, such as derivatives of 2-(3-phenyl acryloyl)cyclopentan-1-one, with good results. Depending on the substituted group, it was also shown that the derivatives had effective biological effects. Compound IV displayed a noticeable antibacterial effect against Staph. aureus and E. coli. The prepared chalcone derivatives exerted markedly variable anti-inflammatory effects.Conclusion: These results indicate that Claisen-Schmidt reaction is not limited to the preparation of chalcone derivatives from diphenyl structures only. Stable alicyclic aromatic structures can also be used. This results in derivatives with good biological effects.
Keywords: Chalcones, Claisen-Schmidt, Anti-inflammatory effects, Granuloma, Aldol Condensation
Immunoprotective evaluation of <I>Escherichia coli</I> outer membrane protein A against the main pathogens of animal mastitis
Authors: Chen Chen , Wu Nana , Rong Na , Kang Chao , Chen Chunlin , Wu Sanqiao , Liu Xiang , Zhang Xiaoying 
Published: June 2020

Purpose: To evaluate prokaryotic expression of the Escherichia coli (E. coli) outer membrane protein A (OmpA) and its immunoprotective function against the main pathogens of animal mastitis.Methods: A molecular cloning method was used to develop a prokaryotic strain expressing OmpA protein, which was purified by Ni-affinity chromatography. Polyclonal antiserum was generated in mice immunized with OmpA protein. Enzyme-linked immunosorbent assay (ELISA) and western blotting were used to determine the titer and verify anti-OmpA serum specificity, respectively. Interaction between OmpA antiserum and main pathogens of animal mastitis was verified by ELISA and a pull-down method. The immune protective function of OmpA protein was evaluated in mice challenged with pathogens of animal mastitis. Optimal fermentation conditions to produce OmpA protein were determined by the L9(34) orthogonal test.Results: A prokaryotic strain expressing OmpA protein was developed, and purified OmpA was used to develop a mouse polyclonal antibody. The anti-OmpA serum exhibited high specificity and a titer of 1:1600. Anti-OmpA serum directly interacted with E. coli and Staphylococcus aureus (S. aureus). OmpA demonstrated a significant immune protective function of 58.33 % against E. coli and 46.15 % against S. aureus. The optimal conditions for expressing fermentation OmpA were a strain absorbance of 0.5 at a wavelength of 600 nm, IPTG final concentration of 0.3 mmol/L, induction time of 12 h, and induction temperature of 28 °C.Conclusion: OmpA possesses selective immunogenicity and a significant immune protective effect against the main pathogens of animal mastitis. The results suggest that OmpA may potentially be used as a vaccine for animal mastitis.
Keywords: E. coli, OmpA protein, Immunoprotection, Animal mastitis, Protein fermentation
Comparison of efficacy and safety of teriparatide and hyaluronic acid - calcitonin combination treatments in Chinese osteoporotic patients with risk of bone fracture: A preliminary investigation
Authors: Hou Changju 
Published: June 2020

Purpose: To evaluate the efficacy and safety of teriparatide and hyaluronic-calcitonin combination treatment in Chinese osteoporotic patients with risk of bone fracture.Methods: Osteoporotic patients aged 30 to 80 years, with at least one vertebral fracture and immediate risk of new vertebral fractures, were recruited from Hangzhou First People's Hospital. They were randomly assigned to two groups (50/group) treated with either teriparatide (20 μg/day) or hyaluronic acid + calcitonin (1:1 ratio, 200 IU daily) for 12 months. The patients were followed up every 3 months. Bone mineral density (BMD) was evaluated using x-ray absorptiometry. The proportion of patients with new fractures was recorded. Changes in serum osteocalcin and serum bone alkaline phosphatase (BSAP) from baseline to endpoint were also measured.Results: Treatment with teriparatide at a dose of 20 μg/day resulted in a significant reduction in the proportion of patients with new fractures (p < 0.05), when compared to patients treated with a combination of hyaluronic acid + calcitonin (200 IU daily). Teriparatide treatment for 12 months resulted in significant increase in lumbar BMD. Significant increases in spine BMD were evident after 3 months of treatment. There were significantly greater increases in serum osteocalcin and BSAP levels in teriparatide-treated patients than in those given hyaluronic acid + calcitonin. The most common treatment adverse event reported by both sexes was dizziness.Conclusion: These results demonstrate that teriparatide is efficacious and well tolerated in Chinese men and post-menopausal women with osteoporosis, when compared to the combination of hyaluronic acid and calcitonin. The efficacy of teriparatide is not associated with gender differences.
Keyword: Teriparatide, Calcitonin, Hyaluronic acid, Bone-specific alkaline phosphatase, Postmenopausal, Bone mineral density
Methylenetetrahydrofolate reductase polymorphism and capecitabine-induced toxicity in patients with gastric cancer
Authors: Xie Xiong-wei , Wang Mao-ren , Zhang Yong-lian 
Published: June 2020

Purpose: To evaluate the effect of methylenetetrahydrofolate reductase (MTHFR) polymorphism on toxicity in gastric cancer (GC) patients treated with capecitabine.
Methods: One hundred and twenty-six GC patients were treated with capecitabine in the study. DNA from GC patients was genotyped for MTHFR A1298C using direct sequencing. Toxicity evaluations were graded. Clinical response was assessed.
Results: In 87.3 % of the patients, capecitabine toxicity was observed. As for MTHFR A1298C polymorphism, 55.6 % patients who exhibited it were associated with reduced MTHFR activity. MTHFR A1298C was associated with capecitabine-related toxicity (p = 0.008); in addition, MTHFR A1298C was significantly associated with gastrointestinal toxicity (p = 0.026), but not with other types of toxicity.
Conclusion: The findings suggest that MTHFR A1298C may be useful for predicting toxicity in GC patients receiving capecitabine treatment, especially gastrointestinal toxicity.
Keywords: MTHFR, Polymorphism, Gastric cancer, Toxicity
Imidazole-thiazolidinone inhibits oesophageal cancer cell proliferation via induction of apoptosis and cell cycle arrest at S phase
Authors: Wang Qian , Yuan Yuan , Jiang Mi , Huang Lihua , Huang Jie , Shen Hongyuan 
Published: June 2020

Purpose: To investigate the effect of imidazole-thiazolidinone on oesophageal cancer (OC) cell proliferation, and the mechanism of action involved.Methods: Human OC cells (HCE-6 and KYSE-1170) were cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10 % fetal bovine serum (FBS) and 1 % penicillin/streptomycin solution at 37 ˚C for 24 h in a humidified atmosphere of 5 % CO2 and 95 % air. After attaining 60 - 70 % confluency, the cells were treated with serum-free medium and graded concentrations of imidazolethiazolidinone (up to 160 μM) for 24 h. Normal cell culture without imidazole-thiazolidinone served as control. Cells in logarithmic growth phase were selected and used in this study. Cell proliferation and apoptosis were assessed using 3 (4,5 dimethyl thiazol 2 yl) 2,5 diphenyl 2H tetrazolium bromide (MTT), and flow cytometric assays, respectively. The levels of expression of apoptosis-related proteins were determined using Western blotting.Results: Treatment of HCE-6 and KYSE-1170 cells with imidazole-thiazolidinone for 48 h led to significant and dose-dependent reduction in their proliferation, as well as significant and dosedependent increase in the number of apoptotic cells (p < 0.05). Light microscopy revealed significantreduction in HCE-6 cell count, detached cells, reduced cell size and irregular cytoplasmic vacuoles. Imidazole-thiazolidinone treatment significantly and dose-dependently decreased HCE-6 and KYSE-1170 cell migration, and arrested HCE-6 cell cycle at S phase (p < 0.05). In HCE-6 cells, imidazolethiazolidinone treatment significantly and dose-dependently upregulated the expressions of cleaved caspase-3/8/9 and bax, but down-regulated bcl-2 expression significantly and dose-dependently (p < 0.05). However, metalloproteinases 2 and 9 (MMP-2 and MMP-9) expressions in HCE-6 and KYSE-1170 cells were significantly and dose-dependently down-regulated by imidazole-thiazolidinone treatment (p < 0.05).Conclusion: The results obtained in this study suggest that imidazole-thiazolidinone suppresses OC cell proliferation via induction of apoptosis and arrest of cell cycle at S phase.
Keywords: Imidazole-thiazolidinone, Oesophageal cancer, Metastasis, Cell cycle arrest, Apoptosis
Knowledge, attitude and perception on PharmD program among penultimate and final-year undergraduate pharmacy students in a Nigerian university – An intervention study
Authors: Aje Akinniyi A. , Okhamafe Augustine O. 
Published: June 2020

Purpose: To carry out an interventional study on the knowledge, attitude and perception of penultimate and final year undergraduate pharmacy students of the University of Ibadan on Doctor of Pharmacy (PharmD) program.
Methods: A cross-sectional study was carried out among penultimate and final-year undergraduate students of the Faculty of Pharmacy, University of Ibadan using semi-structured questionnaire. A seminar was organized for the intervention group. The data were summarized using descriptive and inferential statistics.
Results: Pre-intervention PharmD knowledge assessment of majority, 63 (94.0 %) control group and 63 (87.5 %) intervention group participants was below average. Post-intervention, 38 (52.8 %) intervention group participants had satisfactory scores, while 54 (80.6 %) of control group had below average scores. Generally, the participants had good PharmD attitude and perception. There was a significant difference (p < 0.001) between pre- and post-intervention PharmD knowledge assessment among the intervention group. A significant difference (p < 0.001) was observed between the post-intervention PharmD knowledge of the control group and the intervention group.
Conclusion: Baseline below average PharmD knowledge of study participants improved significantly in the intervention group post-intervention. Generally, the participants had a good attitude and perception towards the PharmD program.
Keywords: PharmD, Pre-post intervention, Undergraduate pharmacy students, Knowledge, Attitude, Perception, University of Ibadan