bluuebunny/crossref_metadata_2025 huggingface dataset:
Framing violence in presidential discourse
Authors: Plemenitaš Katja
Published: June 2020

The paper discusses the characteristics of modern American presidential political rhetoric with special reference to Barack Obama’s speeches in which he addressed the highly publicized killings of black Americans. Three of the analysed speeches contain Obama’s rhetorical reaction to the judicial decisions not to indict the police officers responsible for the killings, while one speech gives his immediate reaction to the mass murder of black parishioners by a white supremacist. The study is based on the discourse-linguistic analysis of attitudinal meanings and their functions, which are conceptualized as evaluative frames. Evaluative frames are used to highlight different kinds of discourse participants through judgments of behaviour, attributions of emotions and evaluations of semiotic phenomena and objects. The theoretical framework for the different categories of evaluative frames is based on the theory of news framing and theory of evaluative language within systemic-functional linguistics. The findings of the analysis show that Obama uses an interplay of positive and negative evaluations of different kinds to transcend racial categorizations and avoid a direct attribution of blame. When he acknowledges the continuing relevance of the racial divide in US society, he often applies evaluative frames in such a way that they unify rather than divide the discourse participants on both sides of the divide.
Nietzsche in Cankar
Authors: Zupan Sosič Alojzija
Published: June 2020

Roman Gospa Judit (1904) Ivana Cankarja še ni bil obravnavan kot izhodišče za primerjavo s filozofsko in umetniško mislijo Friedricha Nietzscheja, zato sem s primerjalno analizo, različnimi metodami teorije pripovedi ter primerjalno-interpretativnim pristopom stičnosti tega romana dokazovala s fragmenti Nietzschejeve misli oziroma naslednjimi miselnimi jedri: morala, čustva, smrt Boga in nadčlovek. Če se morala v romanu Gospa Judit kaže kot Nietzschejev moralni perspektivizem ali, preprosteje, celo kot predsodek, jo Cankar literarno ošvrkne kot okostenel seznam pravil, ki jih mora pravi umetnik preseči. Pripovedovalka Judit v enačenju naroda z moralo ter umetnika z nemoralo ne ironizira samo strogosti morale do umetnika, ampak tudi do ženske, torej do nje same, v patriarhalni družbi. Juditin položaj poudarja posebnost umetnika, predvsem specifičnost njegovega pogleda na svet, v katerem osrednje mesto zavzema srce. Srce kot sinonim za čustva je pomembno sidrišče Nietzschejeve filozofije in Cankarjeve literarno-publicistične misli: v slovenski književnosti je prav Cankar tisti umetnik, ki se je najbolj sistematično ukvarjal s čustvi in se v različnih besedilih ni sramoval poudarjati njihove življenjske pomembnosti. Tudi kategorijo nadčloveka (delno jo zastopa Judit) Cankar predstavlja podobno kot Nietzsche – ta naj bi imel vse tiste lastnosti, ki jih ne more več imeti odsotni ali mrtvi Bog, zato naj bi bil človek nove vrste dionizični človek, vitalen in močan. Tudi inovativnost na pripovedni ravni lahko primerjamo s provokativnostjo nekaterih Nietzschejevih tekstov, na primer filozofskega romana Tako je govoril Zaratustra; tu mislim predvsem na zvrstni sinkretizem v smislu prepleta esejizacije, lirizacije in inovativnosti avtobiografskega izhodišča ter na večperspektivičnost satire in polisemičnost ironije.
Political communication in post-truth society
Authors: Gorenc Nina
Published: June 2020

The research behind this paper is set in the context of the 2016 US presidential election that has come to symbolize the post-truth era. We conducted a literature review on the 2016 election, with the aim to better understand the impact of computational propaganda on the election outcome and on the behaviour of voters. The paper opens with a definition of post-truth society and related concepts such as fake news and computational propaganda. It explores the changes of political communication in a digital environment and analyses the role of social media in the 2016 election. It probes into phenomena such as the trivialization of politics and the loss of credibility of political actors, which are both common in post-truth societies. The reviewed literature seems to indicate that social media have become strong actors on the political stage, but so far not the predominant source of political information and influence on the behaviour of voters. The paper makes two important contributions. Firstly, drawing on the concept of post-truth society, it analyses the role of computational propaganda in the 2016 presidential election, and secondly, it attempts to explain the paradox of general political apathy on one hand, and increased political activism on the other. These are some of the challenges we are now facing, and in order to be able to cope with them it is important to acknowledge and understand them.
Identity Crisis and Inter-Ethnic Conflicts in Northern and Upper East Regions of Ghana
Authors: Gasu John
Published: June 2020

The paper examines conflicts in Northern and Upper East regions of Ghana from the perspective of identity crisis in an ethnically heterogeneous section of the country. Notwithstanding the long periods of co-existence among the heterogeneous ethnic groups the melting pot effect has not emerged as attachment to primordial identity lines still prevail. This is most manifested between the traditionally acephalous societies and the chiefly societies. The relationship between these two societies has been antagonistic, especially as the acephalous societies seem to be besieged with identity crisis. The rejection of the chiefly hegemony is at the root of the identity conflicts. The cases examined in this paper illustrate two of such ‘wars of emancipation’ but with differential results. Whereas the Kusasi had been ‘successful’ in wrestling out of the chiefly hegemonic control of the Mamprusi, the Konkomba have not been all that successful against their antagonists. In both situations, however, the acephalous societies tend to slough off their past ‘anarchic’, systems to adopt and/or adapt the chiefly political culture. This adaptation has become the mode of assertion to redress the low social categorisation of the acephalous societies. It is concluded that observance of peace in two areas continue to be tedious as primordial cleavages are still alive. It is thus recommended, among others that the National Peace Council should work with stakeholders to sustain peace.

Keywords: Identity, Conflict, Kusasi, Mamprusi, Konkomba
Anti-glioma effect of 7-H-pyrrolo [2,3-di]pyrimidine derivative via induction of cell death
Authors: Wang Jie , Peng Xiang , Cao Chengan , Zhao Yan , Xia Xing
Published: June 2020

Purpose: To investigate the effect of 7-H-pyrrolo[2,3-di]pyrimidine derivative (7-HPPD) on glioma cell growth.Methods: Cell viability was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay, while apoptosis was assessed in Hoechst 33342 stained cells using flow cytometry. Changes in cell morphology were assessed by scanning electron microscopy (SEM).Results: Glioma cell viability showed a concentration-dependent decrease on exposure to 7-HPPD for 72 h (p < 0.05). The viabilities of C6, U251 and U87 cells were reduced by 24, 28 and 31 %, respectively, following treatment with 20 μM 7-HPPD. Exposure to various concentrations of 7-HPPDresulted in a marked decrease in BrdU LI and cAMP levels in C6, U251 and U87 glioma cells (p < 0.05). Moreover, 7-HPPD induced apoptosis in U251 and U87 cell cultures, as was evident in the condensation of chromatin material, presence of apoptotic bodies and intense blue fluorescence.Treatment of U251 cells with 7-HPPD for 72 h led to a significant increase in the proportion of cells in G0/G1 phase, and significant decrease in percentage of cells in G2/M and S phases. The population of rounded cells showed a significant rise with increase in 7-HPPD concentration from 10 to 20 μM (p < 0.05).Conclusion: 7-HPPD inhibits growth and proliferation of glioma cells by inducing apoptosis. Therefore, it has a potential for application in glioma chemotherapy.

Keywords: Glioma, Fluorescence, Metastasis, Apoptosis, Infiltration
In vivo antimalarial effect of Ananas comosus (L) Merr (Bromeliaceae) fruit peel, and gas chromatography-mass spectroscopy profiling: A possible role for polyunsaturated fatty acid
Authors: Uzor Philip F. , Ishiwu Blessing U , Nwodo Ngozi J.
Published: June 2020

Purpose: To evaluate the antimalarial effect of Ananas comosus extract and fractions and also to identify the likely bioactive compounds.Method: The fruit peel of the plant was extracted with methanol, and the extract successively fractionated with n-hexane, dichloromethane, ethyl acetate, methanol and water. The n-hexane fraction was further subjected to vacuum liquid chromatography to afford four sub-fractions, one of which was also analyzed using gas chromatography-mass spectroscopy (GC-MS). Plasmodium berghei-infected mice were treated orally with three doses (100, 200 and 400 mg/kg) of the plant extract and a single dose (200 mg/kg) of each of the fractions and sub-fractions in a curative antimalarial model using artemisinin combination therapy (ACT) as the reference drug.Results: The extract exhibited significant (p < 0.001) non-dose dependent parasitemia inhibitory activity in the range of 44.84 to 76.09 %. All fractions displayed inhibitory effect (p < 0.001) in the range of 46.44 to 87.58 % with the dichloromethane fraction displaying the highest effect (87.58 %). The subfractions exhibited significant inhibitory effect (p < 0.001) in the range of 84.14 to 92.54 %. The ACT produced significant (p < 0.001) inhibitory effect of 83.92 %. GC-MS analysis revealed the presence of 17 bioactive compounds, the most abundant of which were linoleic acid and palmitic acid.Conclusion: A. comosus displays strong antimalarial activity which supports the folkloric use of the plant for malarial treatment. A polyunsaturated fatty acid (linoleic acid) was the most abundant phytoconstituent identified.

Keywords: Ananas comosus, Antimalarial, Malaria, Pineapple, Plasmodium beighei
In vitro evaluation of the inhibitory effect of 3, 5-dichloro-2- pyridone on Mycobacterium tuberculosis H37Rv
Authors: Ling Lin , Ling Chen , Wu Hua
Published: June 2020

Purpose: To investigate the anti-tuberculosis potential of twelve commercially available pyridone analogues against Mycobacterium tuberculosis H37Rv strain.Methods: Twelve commercially available pyridone-based compounds were screened against M. tuberculosis H37Rv using different susceptibility tests. The most active or lead compound was further evaluated in detail for its anti-tuberculosis (anti-TB) potential. Kill kinetics was used to determine the dynamics of its anti-TB activity in vitro.Results: Compounds d, j and k were potent against M. tuberculosis H37Rv, with minimum inhibitory concentrations (MICs) of 10, 5 and 10 μg/mL, respectively. The standard anti-TB drugs used in this study (positive control drugs) demonstrated MIC of 2.5 μg/mL. The anti-TB effect of compound j was comparable with those of the standard drugs (RIF, LVX, AMK, EMB and INH). The minimum bactericidal concentration (MBC) of compound j was 10 μg/mL. It produced an MIC of 5 μg/mL in agar proportion method (APM). However, its MIC in Middlebrook 7H9 broth supplemented with 10 % fetal bovine serum (FBS) and 4 % bovine serum albumin (BSA) increased 4- and 8-fold, respectively. The bactericidal effect of compound j was time- and concentration-dependent at dilutions above 2x MIC. Combination of compound j with RIF, LVX or AMK exhibited fractional inhibitory concentration index (ΣFIC) of 1, indicative of additive drug-drug interactions. However, combination with INH or EMB produced a ΣFIC of 2. None of the tested drug combinations was antagonistic.Conclusion: Compound j exhibits potent time- and concentration-dependent antimicrobial effect against M. tuberculosis H37Rv. Thus, it may be suitable as an adjunct to current treatment of drug sensitive and drug-resistant TB.

Keywords: Tuberculosis, Mycobacterium tuberculosis, Pyridone analogs, Antimicrobial activity, Antibiotics
In-silico design of novel 4-aminoquinolinyl analogs as potential anti-malaria agents using quantitative structure– activity relationships and ADMET approach
Authors: Wu Bo , Wang Jiao-Long , Li Liang , Wu Chun-Jie , Zhao Chong-Bo
Published: June 2020

Purpose: To design and screen for potential anti-malaria agents based on a series of 4-aminoquinolinyl analogues.Methods: Molecular fingerprint analysis was used for molecular partitioning of training and test sets. Acquired training sets were used for CoMFA and CoMSIA model construction after good alignment was achieved. Partial least squares analysis combined with external validation were used for  model evaluation. Deep analysis of acquired contour maps was performed to summarize the substituent property requirements for further rational molecular design. Using the chosen models, activity prediction and subsequent ADMET investigation were performed to discover novel designed  compounds with the desired properties.Results: Three different set partitions for model establishment were obtained using fingerprint-based selection. Partition 02 offered an optimal CoMFA model (r2 = 0.964, q2 = 0.605 and r2pred = 0.6362) and the best CoMSIA model (r2 = 0.955, q2 = 0.585 and r2 pred = 0.6403). Based on contour map analysis, a series of compounds were designed for activity prediction. Two of the compounds (wmx09, wmx25) were chosen for their ideal predicted biological activities. Subsequent ADMET investigation indicated that these compoundss have acceptable drug-like characteristics.Conclusion: The screening reveals that compounds wmx09 and wmx25 have strong potential as antimalaria agents.

Keywords: Malaria, 4-Aminoquinolinyl, Molecular fingerprint, QSAR, ADMET
Efficacy and safety of VEGFR inhibitors versus standard chemotherapy in Chinese patients with metastatic liver cancer: Results of a preliminary clinical trial
Authors: Qian Dong , Wang Shuai , Zhao Hongzhi , Zhang Chen
Published: June 2020

Purpose: To evaluate efficacy and safety of vandetanib with and without standard chemotherapy in Chinese patients with metastatic liver cancer.

Methods: Patients with confirmed diagnosis of metastatic liver cancer were randomized to receive vandetanib (300 mg per day in 28 days cycle) intravenously or standard chemotherapy (FOLFOX4) plus best supportive care. Efficacy measures such as overall survival (OS), objective response rate (ORR), and progression-free survival (PFS) were assessed after study drug treatment. Safety of vandetanib and FOLFOX4 was also assessed. Survival time with respect to disease progression was also assessed.

Results: Vandetanib + standard chemotherapy-based regimens showed significantly higher OS benefit when compared to vandetanib and chemotherapy alone. Objective response rate (ORR) was also favorable among the patients treated with combination therapy when compared with monotherapy. A similar trend was noted for PFS; treatment with vandetanib + chemotherapy showed significantly longer PFS when compared to vandetanib and chemotherapy alone, respectively. Trial results demonstrated that vandetanib as a monotherapy or in combination with standard chemotherapy appears to be safe.

Conclusion: The results of this trial may aid clinicians to select appropriate therapeutic intervention for patients with metastatic liver cancer.

Keywords: Vandetanib, Metastatic liver cancer, Chemotherapy, FOLFOX4, VEGFR inhibitors
A clinical study of drugs associated with acute kidney injury in the Chinese population
Authors: Xu Xiaoting , Yu Haiping
Published: June 2020

Purpose: To carry out a study aimed at comprehensive identificat6ion of classes of drugs which cause acute kidney injury (AKI).Methods: A total of 110,508 patients enrolled in Weihai Central Hospital, Weihai, Shandong, China between March 2014 to April 2018 were asked to provide information on comprehensive prescription drug coverage including antivirals, antibiotics, NSAIDs, diuretics and anti-cancer drugs. Only the active user  of these classes of drugs were included in the study. Daily prescription dose, duration, date and time of each drug were recorded. Furthermore, the characteristics and other conditions of the patients such as hypertension, congestive heart failure, diabetes, liver disease,  angiotensin receptor blockers (ARBs), alpha-receptor blockers, beta-receptor blockers, and calcium channel-blockers were included.Results: A total of 1230 patients presented with AKI during the first 60 days of follow-up, while 1546 (58 %) patients were diagnosed with AKI in the secondary endpoint. Indomethacin, valacyclovir, fluorouracil, levofloxacin, ibuprofen and rofecoxib produced higher frequencies of AKI than the control drug, celecoxib. Indomethacin (OR = 2.97 ; 95 % CI= 1.94 - 3.89) and valacyclovir (OR = 2.85 ; 95 % CI = 1.56 - 3.42) were mostly responsible for AKI, followed by rofecoxib (OR = 2.48 ; 95 % CI = 2.32 - 2.71), fluorouracil (OR = 2.58 ; 95 % CI = 1.94 - 3.11), ibuprofen (OR = 1.68 ; 95 % CI = 1.28 - 2.21) and levofloxacin (OR = 1.58 ; 95 % CI = 1.48 - 2.73), in that orderConclusion: This study has identified various classes of drugs which frequently induced AKI. Therefore, physicians should exercise caution in prescribing these drugs, and should consider other medicines to minimize the risk of AKI.

Keywords: Acute kidney injury, Antiviral, NSAID, Toxicity
Cytotoxic, colony formation and anti-migratory effects of Spilanthes acmella (Asteraceae) aerial extract on MCF-7 cells and its cream formulation
Authors: Boontha Supavadee , Thoedyotin Thatcha , Saengtabtim Thanaphon , Im-erb Pathitta , Chaniad Natthamon , Buranrat Benjaporn , Pitaksuteepong Tasana
Published: June 2020

Purpose: To determine anti-breast cancer activities of Spilanthes acmella (S. acmella) extract.Methods: S. acmella was macerated with 95% ethanol. Phenolic, flavonoid content and antioxidant activity of the extract were assessed using Folin  Ciocalteu method, aluminum chloride (AlCl3) colorimetric method and 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay, respectively. Cytotoxicity, colony formation and cell migration suppression on MCF-7 cells, representing anti-breast cancer effects, were also evaluated by sulforhodamine B (SRB), clonogenic and wound healing assays, respectively. Creams containing the extract were formulated and then characterized in terms of their physical appearance, viscosity and pH, before and after stability testing.Results: The crude extract contained phenolic content of 62.8 ± 5.2 mg gallic acid equivalent/g and flavonoid content of 375.6 ± 20.1 mg rutin equivalent/g. The results showed that the extract exhibits antioxidant effect with half-maximal inhibitory concentration (IC50) of 1.2 ± 0.1 mg/mL. It showed cytotoxicity on MCF-7 cells with IC50 of 37.1 ± 1.1 μg/mL in 48 h and inhibited colony formation of cells with IC50 of 44.9 ± 1.3 μM. In addition, it demonstrated an anti-migration effect at a concentration of 50 μg/mL. The developed creams displayed good physical appearance and maintained stable physical properties overt a two-month period.

Conclusion: S. acmella extract exhibits potential anti-breast cancer activity. The cream containing the extract is promising for the topical treatment of breast cancer.

Keywords: Spilanthes acmella, Antioxidant, Anti-breast cancer, Flavonoids, Phenolics, Topical cream
In vitro alteration of artemisinin biosynthesis in Artemisia annua L during treatment with methyl jasmonate
Authors: Alam Pravej , Albalawi Thamer H.
Published: June 2020

Purpose: To investigate the in vitro effect of methyl jasmonate (MeJA) on artemisinin biosynthesis in Artemisia annua.Method: The effect of two concentrations of MeJA i.e. 2 μm (T2) and 5 μm (T5) on biomass, plant height and artemisinin content of Artemisia annua L. was investigated in vitro in MS medium.Results: Plant height (6.5 ± 1.8 cm), biomass (0.18 ± 0.02 g/plant) and artemisinin content (0.035 ± 0.002 % dry weight) were higher in T5 and T2 treatment groups than in non-treated control plants (C). Artemisinin content, biomass and plant height were positively correlated after 2 - 8 days of treatment, but remained unchanged on the 12th day of treatment.Conclusion: The observed effects of exogenous MeJA on the biosynthesis of artemisinin and other secondary metabolites may lead to elucidation of promising targets for further studies on metabolic engineering of Artemisia annua L.

Keywords: Artemisia annua L. Methyl jasmonate, HPLC, Artemisinin
Hypotensive, vaso-relaxant, cardio-depressant and diuretic effect of crude extract of Crotalaria burhia (Fabaceae)
Authors: Raza Muhammad Ali , Imran
Published: June 2020

Purpose: To examine 70 % aqueous-methanol crude extract of Crotalaria burhia (Cb.Cr) for its hypotensive and diuretic effects.

Methods: The effect of intravenous administration of Cb.Cr on blood pressure (BP) of normotensive anesthetized rats was studied. In vitro experiments on rabbit isolated aortic and atrial preparations were performed to elucidate the mechanism of action. The diuretic effect was assessed following oral administration of Cb.Cr in rats.

Results: Intravenous administration of Cb.Cr produced 14.70 ± 1.21, 22.00 ± 2.24 and 36.21 ± 2.65 % reduction in mean arterial blood pressure of the rats at doses of 1, 3 and 10 mg/kg, respectively. It was more potent in relaxing potassium (80 mM)- than phenylephrine (1 μM)-induced contractions in isolated aorta of rabbit with half-maximal effective concentration (EC50) values of 0.58 ± 0.03 and 1.58 ± 0.16 mg/mL, respectively, which are similar to verapamil. The extract showed depressant effects on spontaneously beating atrial preparations of rabbit in a dose-dependent manner. Moreover, Cb.Cr also increased urine volume and urinary electrolyte excretion in rats.

Conclusion: Crotalaria burhia crude extract exhibits hypotensive and diuretic effects in rats. The hypotensive activity of the extract possibly involves vasodilator, cardio-depressant, calcium channel blocking and diuretic actions.

Keywords: Khip, Crotalaria burhia, Calcium channel blocker, Antihypertensive, Diuretic
In vitro cytotoxic and antimicrobial effects of a novel peroxysesquiterpene glucoside from the rhizomes of Cyperus rotundus L (Cyperaceae)
Authors: Sabir Mohammed N. , Saour Kawkab Y. , Rachid Shwan
Published: June 2020

Purpose: To study the antimicrobial and cytotoxic potential of a novel 3,9-peroxsesquiterpene-15-Oglucoside from Cyperus rotundus rhizomes, against HeLa cell line and selected strains of microorganisms.

Methods: The rhizomes were macerated with methanol and fractionated with n-hexane, chloroform, ethyl acetate and butanol. High-performance liquid chromatography (HPLC) was performed together with chemical analysis of the fractions. The 3,9-peroxysesquiterpene-15-O-glucoside was purified through column chromatography of the ethyl acetate fraction, and its purity was determined via reversephase HPLC. Structural elucidation was done with Infrared (IR), proton-nuclear magnetic resonance (HNMR), carbon-13 nuclear magnetic resonance (13C NMR), and mass spectrometry (MS) spectroscopic analyses.

Results: The isolated compound exhibited bactericidal and fungicidal activities against S. aureus and C. albicans at concentration, respectively, in the range of 32 – 100 μg/mL, while MTT assay results showed the cytotoxicity of the compound against eukaryotic (HeLa) cell line (IC50, 88.32 μg/mL).

Conclusion: The isolated metabolite from the methanol extract of C. rotundus rhizome exhibits bactericidal, fungicidal, and cytotoxic potential. However, further studies are required to ascertain its suitability for use as a therapeutic agent.

Keywords: Terpenoids, Column chromatography, Spectroscopy, Antimicrobial, Cytotoxicity, Cyperus rotundus
Epigallocatechin gallate activates miR-193a-3p and protects mice against glucocorticoid-induced osteoporosis by targeting NFATC1 expression
Authors: Dou Ben , Wu Xiaohui , Xie Yisong , Ruan Hongliang , Liu Xiaolan
Published: June 2020

Purpose: To investigate the effect of epigallocatechin gallate (EGCG) on microRNAs in a mouse model of glucocorticoid-induced osteoporosis (GIOP), and the mechanism involved.

Methods: Osteoclast-specific marker mRNA expressions, receptor activator of nuclear factor kappa-B ligand (RANKL), receptor activator of nuclear factor κ B (RANK), and miRNA expressions were determined using reverse transcription polymerase chain reaction (RT-qPCR) analysis. Western blotting was used to assay protein expressions, while miRNA and 3’UTR interaction studies were carried out with reporter assay.

Results: Treatment with EGCG resulted in downregulation of glucocorticoid-induced expressions of RANKL, RANK and osteoclast-specific markers i.e. tumor necrosis factor receptor-associated factor 6, (TRAF6), nuclear factor of activated T cells 1 (NFATc1), cathepsin K, matrix metallopeptidase 9 (MMP9) and tartrate-resistant acid phosphatase (TRAP). Furthermore, EGCG treatment significantly reduced reactive oxygen species (ROS) levels and inflammatory cytokine expressions in GIOP mice. The expression of miRNA-targeting osteoclast marker mmu-mir-193-3p was significantly down-regulated in GIOP mice. However, EGCG treatment increased mmu-mir-193-3p expression and had specific interaction with NFATc1 3’UTR (3’-untranslated region). In vitro results showed that mmu-mir-193-3p mimics downregulated dexamethasone (DXM)-induced osteoclast-specific marker expressions.

Conclusion: These results show that EGCG exerts a protective role against GIOP by upregulating miR- 193a-3p expressions.

Keywords: Epigallocatechin gallate, Glucocorticoids, RANKL, Osteoporosis
Synthesis and evaluation of antimicrobial properties of some azole derivatives
Authors: Imran Mohd , Bawadekji Abdulhakim , Alotaibi Nawaf
Published: June 2020

Purpose: To synthesize new azole derivatives and determine their antimicrobial properties.

Methods: The reaction of the intermediates (2a-2c) with 3a-3c in acetone/potassium carbonate solution yielded 4a-4i, which were characterized using Fourier-transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H-NMR), carbon-13 nuclear magnetic resonance (13C-NMR)) and mass spectrometry (MS). Compounds 4a-4i were assessed for their antibacterial and antifungal effects using the sequential dilution technique, relative to ofloxacin and ketoconazole.

Results: The spectral data for 4a-4i were consistent with the assigned structures. The MIC of compound 4h (10 μg/ml) was similar to that of ketoconazole against Aspergillus flavus, Penicillium citrinum, and Aspergillus niger. The MIC value of compound 4b (10 μg/ml) for Penicillium citrinum was comparable to that of ketoconazole while the MIC value of compound 4d against Staphylococcus aureus and Escherichia coli (20 μg/ml) was equivalent to the corresponding MIC value for ofloxacin.

Conclusion: The synthesized compounds bearing boronic acid moiety are good antimicrobial agents. Accordingly, further investigation into the thiazole-imidazole or thiazole-triazole derivatives bearing boronic acid moiety is suggested.

Keywords: Synthesis, Imidazole, Thiazole, Triazole, Antimicrobials
Perception and satisfaction of stakeholders regarding the patient care area pharmacist initiative in a military hospital in Saudi Arabia
Authors: Almzeiny Mohammed , Khurshid Fowad M. , Alaneazi Nadeen L. , Alotaibi Suhoud S. , Alharbi Sara N. , Almitwazi Ali A. , Alkhodair Ali M. , AlKharji Fahad , Alomar Hussain A. , Alsultan Mohammed S.
Published: June 2020

Purpose: To explore the perceptions and satisfaction of stakeholders (physicians, nurses, and pharmacists) regarding services provided by the patient care area pharmacist (PCAP) initiative.

Methods: This was a cross-sectional study conducted at Prince Sultan Military Medical City (PSMMC). The questionnaire was hand-delivered to a random sample of stakeholder groups (including physicians, nurses, and pharmacists) in three different areas of the hospital: the neonatal intensive care unit (NICU), high dependency unit (HDU), and pediatric nephrology. The questionnaire consisted of three sections. The first section collected demographic information of the participants, and the other sections collected anonymous opinions regarding services provided by the PCAP.

Results: Ninety-nine participants, comprising physicians (n = 27; 27.27 %), nurses (n = 55; 55.55%), inpatient pharmacists (n = 13; 13.13%), and PCAPs (n = 4; 4.04%), participated in the survey. A majority of the respondents (92.3 %) were satisfied with the PCAP services, and all respondents recommended expansion of the PCAP service to cover all wards.

Conclusion: The findings show that all participants have a positive perception of the PCAP service; PCAPs were seen by the participants as drug experts, and their recommendations were perceived as clinically relevant. All stakeholders sought to continue working with the PCAP.

Keywords: Patient care, PCAP, Attitude, Satisfaction, Pharmacy
Comparison of the effects of Tripterygii totorum and sulfasalazine on rheumatoid arthritis: A retrospective cohort study
Authors: Huang Renchun , Tang Yongliang , Zeng Jiali
Published: June 2020

Purpose: To compare, in a retrospective study, the effects and safety profiles of Tripterygii totorum and sulfasalazine in patients with rheumatoid arthritis (RA) following 24 weeks of treatment.

Methods: RA patients (n = 164) who were treated with Tripterygii totorum or sulfasalazine from August 2012 to February 2016 were included in this study. The major end-point was ≥ 20 % improvement as per American College of Rheumatology (ACR) criterion (ACR 20 response) after 24 weeks. Moreover, ACR 50 and ACR 70 responses were studied. The safety parameters investigated comprised of adverse events, vital signs, as well as hematological and biochemical indices (blood counts, electrolyte levels, and kidney and liver function).

Results: At 24 weeks, ACR 20 response was 57.32 % in patients on Tripterygii totorum, while the corresponding value in patients on sulfasalazine was 39.02 % (p = 0.02). In the Tripterygii totorum group, ACR 50 response was 41.46 %, while ACR 70 response was 29.27 %. In sulfasalazine group, ACR 50 response was identified in 26.83 % of the patients, while ACR 70 response was seen in 21.95 % of patients. Adverse events were greater in the Tripterygii totorum group than in sulfasalazine group.

Conclusion: These results suggest that Tripterygii Totorum significantly mitigates RA, with a tolerable safety profile. However, there is need for long-term or controlled trials to ascertain the therapeutic potential of Tripterygii totorum in RA.

Keywords: Traditional Chinese medicine, Tripterygii totorum, Sulfasalazine, Rheumatoid arthritis
Efficacy of Pluronic F-127 gel containing green tea catechin extract on chronic periodontitis – A clinical study
Authors: Nagate Raghavendra Reddy , Yuvaraja M , AlQahtani Saad M. , AlQahtani Nabeeh A. , Tikare Shreyas , Gokhale Shankar T. , Ravi K.S. , Elagib Mohammed Fadul A.
Published: June 2020

Purpose: To evaluate the efficacy of pluronic F-127 gel containing green tea catechin extract as a local drug delivery system in the treatment of chronic periodontitis.

Methods: A total of 20 chronic periodontitis patients participated as per the set inclusion and exclusion criteria. Complete scaling and root planing (SRP) was done for all subjects and pluronic F-127 gel containing green tea catechin was applied on one site. The contralateral site received SRP alone. The plaque index (PI), gingival index (GI), and probing pocket depth (PPD) were recorded at baseline and on the 28th day.

Results: At the 28th-day follow-up, green tea catechin tooth sites showed significantly lower mean scores (GI = 0.55, p = 0.30 and PPD = 3.35 mm) than the corresponding SRP tooth sites (GI = 1.25, PI = 1.15, and PPD = 4.40 mm) (p < 0.05).

Conclusion: When compared to scaling and root planing alone, the local drug delivery gel containing green tea catechin as an adjuvant was more effective in reducing the clinical parameters of periodontitis.

Keywords: Adjuvant therapy, Camellia sinensis, Local drug delivery, Periodontal pocket
Bisleuconothine A potentiates the effect of hyperbaric oxygen therapy against traumatic brain injury by enhancing P2X4 protein expressions
Authors: Meng Xiangen , Zhang Chunyang , Li Na , Zhang Yu , Fan Danfeng , Yang Chen , Li Hang , Guo Dazhi , Pan Shuyi
Published: June 2020

Purpose: To investigate the effect of bisleuconothine A (BA), alone and in combination with hyperbaric oxygen (HO), on traumatic brain injury (TBI) in rats.

Methods: Traumatic brain injury (TBI) was induced by dropping a 200-g weight of steel on the left anterior frontal areas of Sprague-Dawley rats. The synergistic effect of BA and HO was determined by assessing neurological score, as well as parameters of oxidative stress and inflammation, expressions of P2X4 protein and other proteins, and levels of reactive oxygen species (ROS) in the brain tissues of TBI rats.

Results: Neurological function score, levels of inflammatory mediators and oxidative stress parameters were significantly reduced in rats treated with BA alone, and in those treated with a combination of BA and HO, when compared with untreated TBI rats (p < 0.01). Moreover, treatment with BA alone, and BA-HO combination attenuated the altered protein expressions of P2X4, Akt, PI3K and TLR-4 in the TBI rats, and also upregulated the mRNA expression of P2X4 in the brain tissue, when compared with untreated TBI rats (p < 0.01).

Conclusion: These results suggest that BA, when used alone or in combination with HO, reduces neuronal injury through upregulation of the protein expression of P2X4 in rats with traumatic brain injury. Thus, BA may be used clinically with HO therapy for the management of traumatic injury.

Keywords: Bisleuconothine A, Hyperbaric oxygen, Neuronal injury, Oxidative stress, Inflammatory mediators
Geraniin inhibits bladder cancer cell growth via regulation of PI3K/AKT signaling pathways
Authors: Xu Junwei , Qin Ning , Yao Yebin , Chen Tao , Jiang Wenbo
Published: June 2020

Purpose: The effect of geraniin on human bladder transitional carcinoma was not clear, this study was thus intended to reveal it and reveal the mechanism.

Methods: T24 cells were treated with 5, 10, and 20 μM of geraniin and the viability and apoptosis of T24 cells were determined using thiazolyl blue tetrazolium bromide (MTT) assay and flow cytometry. The protein expression levels of Cyclin D1, p21, BAL-2, BAX, cleaved caspase-3 and PI3K/AKT pathway were evaluated using western blot.

Results: Geraniin decreased T24 cell viability and induced T24 cell cycle arrest. The proportion of T24 cells in S phase was decreased by geraniin. Besides, geraniin promoted T24 cell apoptosis and regulated PI3K/AKT pathway.

Conclusion: Geraniin appears to regulate bladder cancer cell growth by decreasing the levels of PI3K and AKT phosphorylation. Thus, this agent may be useful in the management of bladder cancer

Keywords: Geraniin, T24 cells, Apoptosis, PI3K/AKT signaling
Effect of quercetin on bone metabolism and serum osteocalcin in osteoporotic rats
Authors: Yang Hai , Liu Juntao , Wang Man , Wang Lu , Zhang Lixiong , Zhang Fan
Published: June 2020

Purpose: To determine the effect of quercetin on bone metabolism and serum osteocalcin in osteoporotic rats.

Methods: Sixty specific pathogen-free rats were randomly divided into control group, model group; high, medium and low dose quercetin groups, and diethylstilbestrol group, with 10 rats in each group. The high, middle and low dose quercetin groups were given quercetin suspension at doses of 200, 100, 50 mg/kg/day, respectively; the ethylene estradiol group was given ethylene estradiol (1.0 mg/kg/week), while control rats received ethylene estradiol at doses of 200, 100, 50 mg/kg/day. Rats in the model group were given saline. Samples were taken after 6 weeks of administration. The levels of serum bone-derived alkaline phosphatase (BALP), estradiol (E2) and serum osteocalcin (BGP) in femur tissue were measured using ELISA kits. Bone mineral density (BMD) was determined using BMD tester.

Results: Relative to normal rats, BALP and BGP levels in the model rats were markedly increased, while E2 was significantly lower (p < 0.5). Quercetin treatment led to significant increases in BALP and E2 levels in the middle and high dose groups, relative to the model group, while BGP levels in all quercetin treatment groups decreased significantly, when compared to model rats (p < 0.05). There were higher BMD values in quercetin and diethylstilbestrol groups than in model (p < 0.05).

Conclusion: Quercetin enhances bone formation and BMD, but decreases osteocalcin levels and maintains bone biomechanics in ovariectomized rats. Thus, it may find therapeutic application in maintaining bone health.

Keywords: Quercetin, Osteoporosis, Bone metabolism, Osteocalcin
Involvement of YAP and LATS1 in lung development in a rat model of nitrofen-induced congenital diaphragmatic hernia
Authors: Liao Junzuo , Liu Wenying , Zhang Libin , Li Qin , Hou Fang
Published: June 2020

Purpose: To investigate the role of Hippo pathway in lung development in congenital diaphragmatic hernia (CDH).

Methods: One oral dose of nitrofen was maternally administered for induction of CDH on embryonic day 9.5 (E 9.5). Sildenafil was administered intragastrically at a dose of 100 mg/kg on E 11.5. Three rat groups were used: control, CDH, and CDH + sildenafil. Cesarean section was used for fetal delivery on E 21.5. Fetuses with left diaphragmatic hernia (except in control rats) were chosen for investigations. Fetal body weight and weight of lung tissue were recorded, and lung histological evaluation, western blot and PCR were carried out after lung processing.

Results: There was markedly higher expression of YAP in CDH rats than in control rats was unaffected by antenatal sildenafil administration (p < 0.05). However, prenatal sildenafil intervention significantly increased LATS1 expression in the lung of CDH fetuses (p < 0.05).

Conclusion: These results indicate that increased pulmonary YAP expression in CDH rat model might contribute to pulmonary vascular remodeling and suppression of lung development. Thus, antenatal sildenafil administration not only mitigates abnormal vascular remodeling but also promotes lung development, most likely via increased expression of LATS1.

Keywords: Congenital diaphragmatic hernia (CDH), Hippo pathway, Lung development, Sildenafil
Dark Purple Luem Pua rice extract reduces disease severity in rat models of inflammatory bowel disease
Authors: Thipart Kornsuda , Phunikhom Kutcharin , Noenplab Acharaporn Na Lampang , Sattayasai Jintana
Published: June 2020

Purpose: To investigate the effects of an aqueous extract of unpolished dark purple glutinous Thai rice, variety Luem pua (LP), in two rat models of inflammatory bowel disease (IBD).

Methods: Polyphenolic compounds content were determined by HPLC methods and antioxidant activities by DPPH and FRAP assays of the LP extract. The effect of the LP extract at 5 g/kg/day were evaluated in two rat models of IBD that included acetic acid and indomethacin induced IBD. On each day of treatment, changes of body weight, stool consistency and stool blood were scored and expressed as disease activity index (DAI). At the end of the experiments, the animals were euthanized. Colon length and spleen weight were determined, and the degree of inflammation of the colon was scored.

Results: Rats in both models of IBD (acetic acid- and indomethacin-induced IBD), exhibited significant increases in DAI, macroscopic inflammation scores and spleen weights, while the lengths of colon were decreased. Pretreatment with LP extract attenuated the disease severity in both models as seen by the reverse of all observed altered parameters.

Conclusion: These data suggest that LP extract might be beneficial in preventing and/or treating IBD.

Keywords: Inflammatory bowel disease (IBD), Dark purple glutinous rice Var. Luem Pua, Acetic acid, Indomethacin
Chemical composition and anti-arthritic activity of the essential oil from Litsea cubeba against Type II collagen rheumatoid arthritis in rat collagen
Authors: Zhao Jiancun , Wang Qianqian , Ma Jie
Published: June 2020

Purpose: To study the curative effect of the volatile oil from Litsea cubeba (EOL) on type II collagen (CII) induced arthritic (CIA) rat.

Methods: The chemical constituents of EOL were analyzed by gas chromatography-mass spectrometry (GC-MS). The analgesic effect of the oil was assessed by acetic acid-stimulated torsion and hot plate methods, while antiinflammatory potential was further assessed by in an ear oedema model induced by dimethylbenzene in mice. The anti-rheumatoid arthritis (RA) activity of EOL in mice was evaluated in terms of paw volume, arthritis index, thymus and spleen index, and serum inflammatory factor levels.

Results: GC-MS showed that α-citral (26.42 %), β-citral (21.94 %), and limonene (12.79 %) were the main components of EOL. Different doses of EOL (50, 100, 200 mg/kg) exerted varying inhibitory effects on torsion in mice induced by acetic acid (p < 0.01) but had no significant effect on thermal stimulation-induced pain. EOL reduced ear oedema in mice (p < 0.01). In addition, EOL (50, 100, 200 mg/kg) reduced the mouse paw volume, arthritis index, and thymus and spleen index (p < 0.01). Furthermore, EOL reduced proinflammatory cytokines in serum but increased antiinflammatory cytokines (p < 0.01).

Conclusion: EOL ameliorates symptoms of inflammation in CIA rats by inhibiting inflammatory reactions, suggesting it could be further developed as an anti-arthritic drug.

Keywords: Litsea cubeba, Essential oil, Rrheumatoid arthritis, Pro-inflammatory cytokines
JNK pathway promotes hepatocyte apoptosis by inhibiting Bcl-2 and upregulating expressions of Bim, caspase-3 and caspase-9 after cardiopulmonary bypass
Authors: Yu Haibin , Zhang Haojie , Cheng Yan , Fa Xian’en , Zhu Fangtao , Lin Yachao , Huang Weihua
Published: June 2020

Purpose: To study the effect of Jun N-terminal kinase (JNK) signaling pathway on hepatocyte apoptosis in vivo and in vitro, and to elucidate the mechanism of action.

Methods: TdT-mediated dUTP Nick-End Labeling (TUNEL) method was used to determine apoptosis in control and cardiopulmonary bypass (CPB) groups at 0, 3 and 6 hours after rat surgery. The expressions of JNK and p-c-Jun in liver tissues at 0, 3 and 6 h after surgery, and the levels of p-c-Jun, Bcl-2 and Bim following overexpression of JNK, were determined using Western blot assay. Human liver cell line HL-7702 was cultured and transfected with over-expressed JNK plasmid and empty plasmid. Proliferation of HL-7702 cells after JNK over-expression was assessed by Cell Counting Kit-8 (CCK-8), while quantitative real-time polymerase chain reaction (RT-qPCR) was employed to evaluate mRNA expression levels of caspase-3 and caspase-9 mRNA after JNK over-expression. Apoptosis of the cells was determined by flow cytometry (FC) after JNK over-expression.

Results: FC results showed that the number of apoptotic hepatocytes increased after JNK overexpression in hepatocytes while TUNEL assay results demonstrated that hepatocyte apoptosis increased in CPB group, when compared to control group; furthermore, the number of apoptotic cells gradually increased within 6 h after surgery. The expressions of JNK and p-c-Jun were higher in CPB group than in control group, and increased gradually in both groups within 6 h after surgery. Overexpression of JNK decreased the proliferation of hepatocytes, and also lowered protein expression levels of p-c-Jun and Bim; on the other hand, the protein expression levels of Bcl-2 fell, while mRNA expression levels of caspase-3 and caspase-9 mRNA increased.

Conclusion: JNK pathway promotes hepatocyte apoptosis after cardiopulmonary bypass by inhibiting Bcl-2 pathway and promoting the expressions of Bim caspase-3 and caspase-9.

Keywords: Cardiopulmonary bypass, Apoptosis, JNK pathway, Bim, caspase-3 and caspase-9
Anti-endometriotic effect of Angelica sinensis (Oliv.) Diels extract in human endometriotic cells and rats
Authors: Xiong Qi-Xiang , Ruan Xiao-Yun , Deng Al-Ping , Liu Jue , Zhou Qing
Published: June 2020

Purpose: To study the anti-endometriotic effect of Angelica sinensis (Oliv.) Diels extract (ASDE) in human endometriotic cells and rats.Method: Forty female rats were randomly divided into four groups (10 rats/group): control, endometriosis+danazol, endometriosis+high dose of ASDE and low dose of ASDE. The rats were orally administered either vehicle (200 μL of PBS) alone or ASDE (140, 280 and 560 mg/kg/day) for 5 weeks. Danazol was used as the control drug. After induction of endometriosis for 4 weeks, the rats were sacrificed by cervical dislocation and the peritoneum and visceral organs examined visually to measure the number of endometriotic lesions. Serum levels of cancer antigen 125 (CA-125) and interleukin 13 (IL-13), interleukin 18 (IL-18) and tumor necrosis factor-alpha (TNF-α) of peritoneal fluids of rats were measured using ELISA kits. Western blot assay was performed to measure the levels of matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9)  expressions after 24 h of treatment with ASDE (30, 60, and 120 μg/mL).Results: ASDE-treated rats displayed reduced numbers of total endometriotic lesions when compared with vehicle-treated controls (p < 0.01). When the rats were treated with high dose of ASDE, serum CA-125 level, as well as IL-18 and TNF-α levels in peritoneal fluids were significantly lower than that of the control group (p < 0.01); however, IL-13 level in peritoneal fluids was significantly higher than that of the control group (p < 0.01). ASDE treatment significantly suppressed the levels of MMP-2 and MMP-9 protein in 11Z cell (p < 0.01).Conclusion: The results reveal that ASDE exhibits significant anti-endometriotic effect by inhibiting inflammatory factors in rats. Thus, the plant extract can potentially be developed for the clinical management of endometriosis.

Keywords: Angelica sinensis, Endometriosis, Cancer antigen, Endometriotic lesions, Matrix metalloproteinase
Bronchodilatory effect of Zingiber officinale Roscoe (ginger) in guinea pigs
Authors: Vaghela Jitendra H. , Vadgama Vishalkumar K. , Purohit Bhargav M.
Published: June 2020

Purpose: To determine the bronchodilatory effect of ginger on histamine-induced bronchospasm in guinea pigs.

Methods: Thirty-six guinea pigs weighing 400 - 700 g were randomly divided into six groups. Group 1 received distilled water, while group 2 was given formoterol (1.55 μg/kg) + budesonide (0.02 mg/kg). Guinea pigs in groups 3 and 4 were given ginger (350 and 700 mg/kg, respectively), while those in groups 5 and 6 received ginger (350 and 700 mg/kg, respectively) in addition to formoterol (1.55 μg/kg) and budesonide (0.02 mg/kg). Pre-convulsion time and percent protection in each group was calculated.

Results: There was statistically significant improvement in pre-convulsion times, with values of 156.64 ± 32.93, 299.33 ± 44.20, and 235.99 ± 34.55 s for groups 2, 5 and 6, respectively (p < 0.01). Moreover, statistically significant protection values of 73 and 68 % were obtained for groups 5 and 6, respectively, relative to normal control (p < 0.01).

Conclusion: These results indicate that ginger has promising potential for use as an add-on treatment for bronchospasm.

Keywords: Zingiber officinale, Histamine, Asthma, Pre-convulsion time