bluuebunny/crossref_metadata_2025_split huggingface dataset:
Dimedone Derivative {2-[(4-Hydroxy-phenylamino)- methylene]-5,5-dimethyl-cyclohexane-1,3-dione} Plays an Important Role in Breast Cancer Treatment
Authors: Song L , Kang H , Liu D , Dai Z , He J , Wang B , Zhao Y , Wang X , Xi W 
Published: March 2021

Purpose: To investigate the effect of 2-[(4-hydroxy-phenylamino)-methylene]-5,5-dimethyl-cyclohex (HPDH) on mammary carcinogenesis induced by 7,12-dimethylbenz(a)anthracene in female Sprague Dawley rats.Methods: Among three groups of rats (50 each) used in the study, the control group was fed standard diet alone, ibuprofen group received standard diet containing 1200 mg/kg ibuprofen while HPDH group was administered standard diet containing 1200 mg/kg HPDH. The treatment was for 10 days for all the groups. All the animals received 20 mg of DMBA intragastrically by gavage. Clinical parameters for the rats were recorded weekly. Micrometer caliper was used to measure the diameter of all the tumors at the end of the experiment and tumor volume calculated. Histological evaluation was performed using hematoxylin and eosin (H&E) staining. High performance liquid chromatography (HPLC) was used to determine the level of HPDH and ibuprofen in the serum of the animals.Results: The data revealed a significant decrease in the number of rats with mammary tumor, number of tumors/rat and tumor volume by 54, 72 and 75 %, respectively, in HPDH group compared to control group. The ibuprofen- treated rats also showed significant decrease in the number of rats with tumor, number of tumors/rat and tumor volume by 43, 55, and 59 %, respectively. Treatment of rats with HPDH increased the latency period of tumor induction significantly (p < 0.005). Median detection period (50 % of tumors) was 92, 83 and 56 days, respectively, in HPDH, ibuprofen and control groups, respectively, after DMBA induction.Conclusion: These results demonstrate that HPDH possesses strong chemopreventive activity against mammary carcinogenesis.Keywords: Carcinogenesis, Mammary tumor, Median detection period, Tumor, Latency period, Chemopreventive activity, Ibuprofen
Development and in-vitro Evaluation of Once Daily Tablet Dosage Form of Loxoprofen Sodium
Authors: Zaman M , Sarfraz RM , Adnan S , Mahmood A , Hanif M , Qureshi J , Chaudhary MT , Akram MA , Bashir I 
Published: March 2021

Purpose: To formulate and characterize once daily controlled release tablet of loxoprofen sodium.Methods: Eudragit RS-100, hydroxylpropyl methylcellulose (HPMC) and pectin were used as release retarding polymers. All the formulations were prepared by direct compression method. Various precompression studies were carried out to determine Hausner’s ratio, Carr’s index, angle of repose, bulk density and tapped density Differential scanning calorimetry (DSC) studies and also post-compression studies to evaluate hardness, friability, weight variation, drug content, in-vitro drug release were conducted on the tablets. The drug release data were subjected to kinetic models, including zero order, first order, Hixon Crowell, Higuchi and Korsmeyer-Peppas.Results: Compressibility index (7.6 ± 1.32 - 12.5 ± 1.43%), Hausner’s ratio (1.08 ± 0.04 - 1.14 ± 0.03), angle of repose (27.78 ± 0.47 - 30.49 ± 0.46°), hardness (6.25 ± 0.27 - 7.21±0.21 kg/cm2), friability (0.14 ± 0.06 - 0.28 ± 0.0 %), weight variation (249.5 ± 2.09 - 251.35 ± 2.41 mg) and drug content (97.30 ± 0.28 - 103.70 ± 0.31 %) were within generally accepted limits for the pre-and post-compression formulations, respectively. The tablets having the maximum amount of among the three polymers tested as matrix materials, HPMC, represented by F3 tablets, exerted better sustained release properties after 12 h. Release pattern was more of Fickian diffusion followed by Higuchi mechanism.Conclusion: The release of the loxoprofen sodium was optimized up to 12 h.Keywords: Loxoprofen, Sustained release, hydroxypropyl methylcelluose, Pectin, Eudragit, Matrix tablets
Bergenin suppresses the growth of colorectal cancer cells by inhibiting PI3K/AKT/mTOR signaling pathway
Authors: Gao Xucan , Wang Yazhu , Zhang Jianzhuo , Lin Lifen , Yao Qi , Xiang Guoan 
Published: March 2021

Purpose: To investigate anticancer effects of bergenin on human colorectal cancer cell lines.Methods: Human colorectal adenocarcinoma cell line HCT116 was treated with various concentrations of bergenin for 24 and 48 h. Cell viability, apoptosis, cell cycle arrest and reactive oxygen species (ROS) level were analyzed by MTT, flow cytometry and fluorescent dye assays, respectively. DNA damage-associated protein expressions were analyzed by Western blotting.Results: Bergenin significantly suppressed the viability of HCT116 cells. Moreover, bergenin induced cells to accumulate in G1 phase and resulted in DNA breaks in HCT116 cells. It also led to marked accumulation of intracellular reactive oxygen species (ROS), a breaker of DNA strand in HCT116 cells. Interestingly, bergenin inhibited PI3K/AKT/mTOR pathway.Conclusion: Bergenin effectively suppresses the growth of colorectal adenocarcinoma by inducing generation of intracellular ROS, DNA damage and consequent G1 phase arrest via inhibition of PI3K/AKT/mTOR pathway.Keywords: Bergenin, Colorectal cancer, DNA damage, Cell cycle arrest, PI3K/AKT/mTOR
In vivo anti-inflammatory activity of Liquidambar formosana Hance infructescence extract
Authors: Ma Haoran , Wang Fuqian , Jiang Jie , Cheng Lu , Zhang Hong , Zhang Geng 
Published: March 2021

Purpose: To evaluate the anti-inflammatory activity of Liquidambar formosana Hance infructescence (Liquidambaris fructus, ELF) in vivo, and clarify its underlying mechanisms. Methods: The in vivo anti-inflammatory activity of ELF was examined by xylene-induced ear swelling test in mice as well as carrageenan-induced paw edema method in rats. The levels of inflammatory cytokines (TNF-α, IL-1β, IL-6 and IL-10) in serum were measured by enzyme-linked immunosorbent assay (ELISA), while the expressions of COX-2, iNOS and NF-κB p65 in paw tissue of rats were evaluated by western blot.Results: After ELF treatment, the levels of TNF-α (p < 0.001), IL-1β (p < 0.001) and IL-6 (p < 0.001) in serum decreased and the levels of anti-inflammatory cytokine IL-10 increased (p < 0.01). In addition, ELF treatment resulted in decrease of COX-2 (p < 0.01), iNOS (p < 0.01) and NF-κB p65 (p < 0.01) expressions in Wistar rats.Conclusion: The results reveal that ELF possesses significant anti-inflammatory effect in vivo. The anti-inflammatory activity is associated with the levels of TNF-α, IL-1β, IL-6 and IL-10 in serum. Furthermore, the suppression of NF-κB p65, iNOS and COX-2 is linked to its anti-inflammatory effect. These results provide a rationale for the use of Liquidambaris fructus in inflammatory disease in traditional medicine.Keywords: Anti-inflammatory activity, Liquidambaris fructus, Cytokines, Ear swelling test, Paw edema
Anti-hyperlipidemic effects of Caralluma edulis (Asclepiadaceae) and Verbena officinalis (Verbenaceae) whole plants against high-fat diet-induced hyperlipidemia in mice
Authors: Ashfaq Aqsa , Khan Arif-ullah , Minhas Amber Mahmood , Aqeel Tahir , Assiri Asaad M. , Bukhari Ishfaq A. 
Published: March 2021

Purpose: To investigate the anti-hyperlipidemic effect of Caralluma edulis and Verbena officinalis.Methods: Phytochemical analysis of crude extracts of Caralluma edulis (Ce.Cr) and Verbena officinalis (Vo.Cr) were carried out. Hyperlipidemia was induced in mice with high-fat diet (HFD, 1.25 % w/w cholesterol, 0.5 % w/w cholic acid and 10 % v/w coconut oil). All the groups, except the saline-treated group, were fed on HFD for 4 weeks (lead-in period) to induce hyperlipidemia. Thereafter, the groups were treated with varying doses of the plant extract for 2 weeks (treatment period) as well as atorvastatin (10 mg/kg) reference standard. Body weight was measured fortnightly for all groups. Total cholesterol (TC), triglyceride (TGs) and low density lipoprotein (LDL) were assayed using Merck diagnostic kits. For histopathological analysis, liver slices were fixed in 10 % formalin and embedded in paraffin wax and was examined with the aid of hematoxylin and eosin staining (H & E).Results: Caralluma edulis (Ce.Cr) contains saponins, alkaloids, tannins, phenol, glycosides, terpenoids and flavonoids while Verbena officinalis (Vo.Cr) tested positive for the presence of alkaloids, carbohydrates, flavonoids, saponins and tannins. HFD increased total cholesterol (TC), triglyceride (TGs), low density lipoprotein (LDL) and very low density lipoprotein (VLDL) compared to regulator diet (p < 0.001). Treatment of the animals with Ce.Cr and Vo.Cr dose-dependently (500 - 1000 mg/kg) reduced serum TC, TGs, LDL and VLDL (p < 0.05, p < 0.01, p < 0.001, vs. HFD group) and raised high density lipoprotein (HDL) (p < 0.01, vs. HFD group), similar to that observed with atorvastatin (10 mg/kg). The anti-hyperlipidemic effects of Ce.Cr and Vo.Cr were also confirmed via liver histopathology results, showing improved structure with no hepatocellular necrosis and fat accumulation.Conclusion: These results indicate that Caralluma edulis and Verbena officinalis exhibit antihyperlipidemic effect; thus, the plants have therapeutic potentials for the management of lipid disorders.Keywords: Caralluma edulis, Verbena officinalis, Anti-hyperlipidemia, Hepatocellular necrosis
Anti-arthritic effect of total anthraquinone from Polygonum cuspidatum on type II collagen-induced arthritis in rats
Authors: Wang Feng , Qiao Yan-hong , Niu Hui-min , Zhao Hong 
Published: March 2021

Purpose: To study the anti-arthritic effect of total anthraquinone from Polygonum cuspidatum (TAPC) on type II collagen-induced arthritis (CIA) in rats, and to investigate the underlying mechanism(s).Methods: CIA rats were prepared and treated orally with TAPC at doses of 50, 100 and 200 mg/kg/day, for 24 days. Paw volume and arthritis score were measured prior to TAPC treatment, and subsequently at 3-day intervals on days 3, 6, 9, 12, 15, 18, 21 and 24. Serum levels of TNF-α, IL-6 and IL-17 were determined by enzyme-linked immunosorbent assay (ELISA), while synovial tissue TNF-α, IL-6 and IL-17mRNA expressions were assayed by real time-polymerase chain reaction (RT-PCR). Thymus and spleen indices were also determined.Results: TAPC (50, 100 and 200 mg/kg) significantly alleviated paw swelling (p < 0.05), arthritis scores (p < 0.05) and thymus and spleen indices (p < 0.05) of CIA rats, when compared with the control rats. In addition, TAPC significantly decreased serum levels of the pro-inflammatory cytokines TNF-α, IL-6 and IL-17 (p < 0.01); and down-regulated their mRNA expressions in synovial tissues (p < 0.01).Conclusion: These results suggest that TAPC exerts good anti-arthritic activity in rats, most probably via suppression of inflammatory responses.Keywords: Polygonum cuspidatum, Anthraquinone, Type II collagen-induced arthritis, Pro-inflammatory cytokines
Construction and evaluation of a novel triple cell epitopebased polypeptide vaccine against cow mastitis induced by Staphylococcus aureus, Escherichia coli and Streptococcus
Authors: Liu Xiang , Chen Chunlin , Chen Chen , Marslin Gregory , Ding Rui , Wu Sanqiao 
Published: March 2021

Purpose: To construct a novel triple cell epitope-based polypeptide vaccine against cow mastitis induced by Staphylococcus aureus, Escherichia coli and Streptococcus and to reduce the use of antibiotics.Methods: Based on bioinformatics approach, a novel triple epitope-based polypeptide (CM-TEP) was designed and subjected to Ni-NTA flow resin purification. Purified CM-TEP was immunized into mice to prepare a polyclonal antibody. Pull-down assays and enzyme-linked immunosorbent assay (ELISA) were used to detect the interaction between CM-TEP antibodies and S. aureus, E. coli and Streptococcus. Active immunity mice and challenge of bacterial pathogens were used to detect immune protection of CM-TEP. Additionally, the optimal expressing conditions of CM-TEP strain were analyzed using orthogonal test design.Results: A novel cow mastitis triple cell epitope-based polypeptide (CM-TEP) with a MW of 36 kDa was designed, purified and used to immunize mice to prepare a polyclonal antibody. Pull-down assays and ELISA data showed that CM-TEP antibodies directly interacted with S. aureus, E. coli and Streptococcus. CM-TEP displayed a significant immune protective effect against infection by S. aureus (50 %, p < 0.05) and E. coli (54.54 %, p < 0.05) and provided some immune protective effect (30.78 %, p > 0.05) against Streptococcus. The optimum expressing conditions of CM-TEP were as follows: IPTG concentration of 0.3 mmol/L, strain OD600 value of 1, inducing temperature of 37 oC, and inducing time of 8 h.Conclusion: The findings suggest that epitope-based vaccine of CM-TEP may be a useful strategy for treating cow mastitis induced by S. aureus, E. coli and Streptococcus.Keywords: Cow mastitis, Epitope vaccine, Immunogenicity, Immune protective
Recent novel tumor gatekeepers and potential therapeutic approaches (2017)
Authors: Zahid Kashif Rafiq , Zada Hira Khan , Wassan Ghulam Mustafa , Hassan Waseem , Liu Ke , Liu Yanli , Liu Jinlin , Zhao Haobin , Qi Chao 
Published: March 2021

Tumor remains a challenging task for oncology community. Drug resistance due to chemotherapy remain principal impediments toward potential therapeutic strategies. Development of novel anti-cancer drugs or new targeted strategies to conquer drug resistance is a key goal of cancer research. In this respect, novel tumor gatekeepers and innovative targeted strategies can be helpful in overcoming drug resistance as well as improve currently used targeted therapies. In this review, efforts have been made to present some of the latest knowledge about novel tumor gatekeepers and new therapeutic strategies to improve the efficacy of chemotherapy and give new hope to cancer patients to fight against cancer.Keywords: Cancer, Potent inhibitors, Gatekeepers, Therapeutic approaches, Oncogenic pathways
Preparation and characterization of N-benzyl-N,O-succinyl chitosan polymeric micelles for solubilization of poorly soluble non-steroidal anti-inflammatory drugs
Authors: Woraphatphadung Thisirak , Sajomsang Warayuth , Rojanarata Theerasak , Akkaramongkolporn Prasert , Ngawhirunpat Tanasait , Opanasopit Praneet 
Published: March 2021

Purpose: To investigate the solubilization of poorly water-soluble non-steroidal anti-inflammatory drugs (NSAIDs) in N-benzyl-N,O-succinyl chitosan (BSCS) polymeric micellesMethods: BSCS was synthesized by reductive amination and succinylation, respectively. NSAIDs; meloxicam (MX), piroxicam (PRX), ketoprofen (KP) and indomethacin (IND) were entrapped in the hydrophobic inner cores by evaporation method. The effects of drug structure on loading efficiency, particle size and surface charge of micelles were investigated.Results: The critical micelle concentration of BSCS micelles was 0.0385 mg/mL and cytotoxicity on Caco-2 cells depends on the polymer concentration (IC50 = 3.23 ± 0.08 mg/mL). BSCS micelles were able to entrap MX, PRX, KP and IND and also improve the solubility of drugs. Drug loading efficiency was highly dependent on the drug molecules. The drug loading capacity of these BSCS micelles was in the following rank order: KP (282.9 μg/mg) > PRX (200.8 μg/mg) > MX (73.7 μg/mg) > IND (41.2 μg/mg). The highest loading efficiency was observed in KP-loaded BSCS micelles due to the attractive force between phenyl groups of KP and benzyl groups of the polymer. Particle size and surface charge were in the range of 312 - 433 nm and -38 to -41 mV, respectively.Conclusion: BSCS copolymer presents desirable attributes for enhancing the solubility of hydrophobic drugs. Moreover, BSCS polymeric micelles might be beneficial carrier in a drug delivery system.Keywords: BSCS, polymeric micelles, solubilization, non-steroidal anti-inflammatory drugs
HIPK2 reduces the resistance of gastric cancer cells to cisplatin via p53 pathway
Authors: Mi Jiali , Zhang Xing , Jia Yingdong 
Published: March 2021

Purpose: To uncover the functional effect of homologous domain-associated protein kinase 2 (HIPK2) on the viability of cisplatin (DDP)-resistant gastric cancer (GC) cells and elucidate the possible mechanism of action.Methods: The effect of DDP on GC viability and apoptotic rate was evaluated using MTT and flow cytometry (FCM) assays. The potential effect of HIPK2 on DDP sensitivity and cell apoptosis was investigated in the presence of cisplatin while the effect of HIPK2 on p53 activation was determined by immunoblot assay.Results: HIPK2 expression was decreased in DDP-resistant GC cell while upregulation of HIPK2 reduced growth, but promoted apoptosis in DDP-resistant GC cells. Further investigations showed that HIPK2 promoted p53 activation, while suppression of p53 weakened the inhibitory effect of HIPK2 on DDP-resistance in GC cells.Conclusion: The results suggest that HIPK2 is a promising and important therapeutic factor for the regulation of the resistance of GC cells to DDP. Thus, may have a role to play in the management of gastric cancer
Keywords: Gastric cancer, Cisplatin, HIPK2, Homologous domain-associated protein kinase 2, p53 pathway, Therapeutic target
LncRNA gas5 regulates granulosa cell apoptosis and viability following radiation by X-ray through sponging miR-205-5p and Wnt/β-catenin signaling pathway ingranulosa cell tumor of ovary
Authors: Li Yan , Ma Xing , Li Jun , He Saifei , Zhuang Juhua , Wang Guoyu , Ye Ying , Xia Wei 
Published: March 2021

Purpose: The study explored the role of lncRNA gas5 in ovarian granulosa cells exposed to X-ray in granulosa cell tumor of ovary(GCTO).
Methods:Exposed the KGN cell line (KALANG, Beijing, China) to X-ray to mimic the radiotherapy for GCSO patients in vitro, cell viability was checked by CCK8 assays. RT-qPCR detected the RNA expression of apoptosis-related genes while Western Blot for biomarkers in wnt/β-catenin signaling. Differential expressions of lncRNA gas5 were examined after cells exposed to X ray for 0,24,48hs. We over expressed gas5 and assessed resultant cell viabilities, apoptosis and signaling. The sponging between gas5 and miR-205-5p was verified through Luciferase Assay. CCK8, RT-qPCR and Western Blot were applied for investigations into the correlation between miR-205-5p and cell viability and apoptosis after miR-205-5p augmentation. Similarly, the interactions between the gas5 and miR-205-5p were assessed after co-transfection of miR-205-5p mimics and oe-gas5. Last, wnt inhibitor was used to study the role of signaling pathway in KGN cells.
Results: Exposure of KGN toX-ray reduced cell viabilities and increased apoptosis. Gas5 had reduced expression in cells while miR-205-5p increased. Gas5 upregulation could protect the cells from apoptosis and add to the cell viability and activation of wnt//β-catenin signaling. lncRNA gas5 targeted miR-205-5p and miR-205-5p mimics could counteract functions of up-regulated lncRNA gas5, regulating Wnt/β-catenin signaling pathway. Inactivation in Wnt/β-catenin could suppress cell viability.
Conclusions: lncRNA gas5 regulated the cell apoptosis and viability after cellular radiation, which might be a potential therapeutic target to combine into radiotherapy for GCTO patients in clinical stage.
Keywords: Ovary, proliferation, apoptosis, lncRNA gas5, x-ray
Effect of vitamin D on Becker muscular dystrophy: A review
Authors: Alasady Shaymaa H. 
Published: March 2021

The correlation between Becker muscular dystrophy (BMD) and vitamin D has long been known, since vitamin D controls bone turnover which occurs in this disease. Thus, vitamin D is beneficial to some extent to BMD patients due to the fact that it has long been known to play an important part in bone metabolism. According to recent studies which suggest association between vitamin D and multiple diseases involving multiple organs, vitamin D may alleviate the pathophysiology of BMD. This review focuses on the benefits of vitamin D to BMD patients through alleviation of the pathophysiology and complications of the disease.
Keywords: Becker muscular dystrophy, Cardiomyopathy, Vitamin D
MiR-384-3p aggravates propofol induced apoptosis in developing neurons by targeting Wnt3a
Authors: Shi Xiaoling , Jia Wei 
Published: March 2021

Purpose: To evaluate the cytotoxicity of miR-384-3p toward propofol-treated neonatal rat hippocampal neurons and investigate its related molecular mechanism(s).Methods: Quantitative real-time polymerase chain reaction (qRT-PCR) was employed to determine miR-384-3p expression levels in propofol-treated neonatal rat hippocampal neurons. Cell apoptosis and cell viability were evaluated by flow cytometry analysis and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, respectively. Bioinformatics and dual-luciferase reporterassay were applied together to forecast and verify the interaction between miR-384-3p and Wnt3a. Wnt3a expression in transfected neonatal rat hippocampal neurons was assessed by Western blot assay.Results: Propofol induced apoptosis in developing neurons by upregulating miR-384-3p expression levels. Knockdown of miR-384-3p reduced propofol-induced apoptosis in developing neurons. Subsequent experiments indicated that miR-384-3p directly regulated Wnt3a expression via coupling with the 3′-untranslated region of Wnt3a. Furthermore, upregulation of Wnt3a expression levels alleviated propofol-induced cytotoxicity promoted by miR-384-3p (p < 0.01).Conclusion: MiR-384-3p aggravates propofol-induced apoptosis in developing neurons by targeting Wnt3a.
Keywords: MiR-384-3p, Wnt3a, Propofol, Apoptosis, Developing neurons
KOMPETENSI MANAJERIAL KEPALA MADRASAH DALAM MEMBANGUN MOTIVASI KERJA GURU DI SEKOLAH MENENGAH PERTAMA NEGERI 2 BILAH HULU KABUPATEN LABUHANBATU
Authors: Siti Amrina Hasibuan Candra Wijaya, Syamsu Nahar, 
Published: March 2021

<p><strong>Abstrak</strong>: Penelitian ini bertujuan untuk menganalisis: 1) Kompetensi manajemen kepala sekolah di SMP Negeri 2 Bila Hulu Kabupaten Labuhanbatu, 2) Upaya kepala sekolah dalam membangun motivasi kerja guru di SMP Negeri 2 Bila Hulu Kabupaten Labuhanbatu, 3) Kompetensi manajerial kepala sekolah dalam membangun motivasi kerja guru di SMP Negeri 2 Bila Hulu Kabupaten Labuhanbatu. Penelitian menggunakan pendekatan kualitatif. Teknik pengumpulan data penelitian berupa observasi, wawancara dan dokumentasi. Hasil penelitian mengungkapkan tiga temuan, yaitu: 1) Kompetensi Manajerial Kepala SMP Negeri 2 Bilah Hulu Kabupaten Labuhanbatu bahwa kepala sekolah dalam hal ini sudah begitu berusaha keras untuk menerapkan kompetensi manajerial yang dimilikinya, 2) Upaya kepala sekolah dalam membangun motivasi kerja guru di SMP Negeri 2 Bila Hulu Kabupaten Labuhanbatu, yaitu: dengan pendekatan terhadap guru; membangun keakraban; memberikan hadiah; mendengar masukan dari guru, 3) Kompetensi Manajerial Kepala sekolah dalam Membangun Motivasi Kerja Guru di SMP Negeri 2 Bilah Hulu Kabupaten Labuhanbatu, diantaranya sebagai berikut: Kepala sekolah telah berupaya keras mengelola budaya dan iklim sekolah yang baik sehingga terciptanya suasana kerja yang harmonis, terjalinnya komunikasi yang baik antara kepala sekolah dengan personel sekolah lainnya serta dapat dilihat pula dari tingkat kehadiran guru dalam memberikan pengajaran di dalam kelas</p><p><strong>Kata Kunci: </strong>Kompetensi Manajerial dan Motivasi</p>