Drug Discoveries & Therapeutics
Online ISSN : 1881-784X
Print ISSN : 1881-7831
ISSN-L : 1881-7831
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Showing 1-10 articles out of 10 articles from the selected issue
Review
  • Elijah Kolawole Oladipo, Ayodeji Folorunsho Ajayi, Aduragbemi Noah Ode ...
    Type: review-article
    2020 Volume 14 Issue 4 Pages 153-160
    Published: August 31, 2020
    Released: September 08, 2020
    JOURNALS FREE ACCESS

    The COVID-19 infection has been a matter of urgency to tackle around the world today, there exist 200 countries around the world and 54 countries in Africa that the COVID-19 infection cases have been confirmed. This situation prompted us to look into the challenges African laboratories are facing in the diagnosis of novel COVID-19 infection. A limited supply of essential laboratory equipment and test kits are some of the challenges faced in combatting the novel virus in Africa. Also, there is inadequate skilled personnel, which might pose a significant danger in case there is a surge in COVID-19 infection cases. The choice of diagnostic method in Africa is limited as there are only two available diagnostic methods being used out of the six methods used globally, thereby reducing the opportunity of supplementary diagnosis, which will further lead to inappropriate diagnosis and affect the accuracy of diagnostic reports. Furthermore, challenges like inadequate power supply, the method used in sample collection, storage and transportation of specimens are also significant as they also pose their respective implication. From the observations, there is an urgent need for more investment into the laboratories for proper, timely, and accurate diagnosis of COVID-19.

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  • Shweta Sinha, Alka Sehgal, Rakesh Sehgal
    Type: review-article
    2020 Volume 14 Issue 4 Pages 161-170
    Published: August 31, 2020
    Released: September 08, 2020
    JOURNALS FREE ACCESS

    Coronavirus disease 2019 (COVID-19) is found to be associated with various comorbidities which include cardiovascular diseases, hypertension, and diabetes. The impaired regulation of renin-angiotensin-aldosterone system (RAAS) has been seen in COVID-19 patients, but whether RAAS inhibitors, such as angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin II type 1 receptor blockers (ARBs), are responsible for worsening of clinical conditions remains unknown. Herein, we review the role of angiotensin-converting enzyme 2 (ACE2) expression in disease progression, its association with comorbidities and COVID-19, and summarize the clinical evidence for several potential directions for future research work on ACEIs/ARBs in COVID-19 patients.

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  • Rohit Kumar, Kutty Sharada Vinod, Ankit Mittal, Shreya Das Adhikari, N ...
    Type: review-article
    2020 Volume 14 Issue 4 Pages 171-176
    Published: August 31, 2020
    Released: September 08, 2020
    JOURNALS FREE ACCESS

    The healthcare sector has been overwhelmed by the global rise in the number of COVID-19 cases. The primary care physicians at the forefront of this pandemic are being provided with multiple guidelines (state, national, international). The aim of this review was to examine the existing guidelines for congruence and critically analyze them in light of current evidence. A discordance was noted between the national and state guidelines with respect to indication, duration and dosage of antivirals, steroids/immunomodulators, anticoagulation and convalescent plasma. The lack of concordance between various guidelines mandates the need for a unified national guideline that is regularly updated.

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Original Article
  • Atmika Paudel, Suresh Panthee, Hiroshi Hamamoto, Kazuhisa Sekimizu
    Type: research-article
    2020 Volume 14 Issue 4 Pages 177-180
    Published: August 31, 2020
    Released: September 08, 2020
    [Advance publication] Released: August 24, 2020
    JOURNALS FREE ACCESS

    This study was performed with the aim of making a very simple recipe of silkworm diet for research purposes, especially screening of drug candidates. We prepared a diet containing mulberry leaves powder and soybean flour at different ratios, fed them to fifth instar silkworm larvae, and observed their growth. We selected the diet with 1:1 ratio of mulberry powder and soybean flour, named MS-11, and used for further experiments. MS-11 diet was available for oral administration of drugs in silkworm hyperglycemic model and infection model. The availability of a simple artificial diet for experiments that require feeding silkworms will enhance the use of silkworms for biological, biotechnological, and pharmacological researches.

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  • Xiaohui Luo, Pengdan Luo, Yushun Zhang
    Type: research-article
    2020 Volume 14 Issue 4 Pages 181-186
    Published: August 31, 2020
    Released: September 08, 2020
    [Advance publication] Released: July 29, 2020
    JOURNALS FREE ACCESS

    The aim of this study was to identify novel long non-coding RNA (lncRNA) biomarkers associated with dilated cardiomyopathy (DCM) and reveal the potential molecular mechanisms of DCM development using bioinformatics approaches. The array data of GSE5406, including 108 DCM samples and 16 non-failing control samples, were obtained from the Gene Expression Omnibus database. The differentially expressed lncRNAs were identified using limma package in R. Pearson's correlation analyses were performed between the differentially expressed lncRNAs and protein-coding genes based on their expression levels. Pathway enrichment of these lncRNAs was conducted based on the significantly co-expressed genes. From the receiver operating characteristic (ROC) curve, the area under the ROC curve (AUC) value was obtained and used for evaluating discriminatory ability. IDI2-AS1 and XIST were differentially expressed in DCM patients. A total of 510 co-expressed genes were identified. The enriched functions and pathways of the co-expressed genes mainly included NADH dehydrogenase activity, cardiac muscle contraction, and oxidative phosphorylation. The ROC curve analysis indicated that the two lncRNAs have favorable diagnostic values in DCM. The AUC values of XIST, IDI2-AS1, and the combination of XIST and IDI2-AS1 were 0.733 (95% CI: 0.646-0.809), 0.796 (95% CI: 0.715-0.863), and 0.823 (95% CI: 0.745-0.886), respectively. This study identified IDI2-AS1 and XIST lncRNAs and related pathways involved in the pathogenesis of DCM, thus providing potential diagnostic and therapeutic targets for DCM.

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  • Tiantian Wang, Zhigang Sun, Yong Wang, Feifei Li, Xiaoming Zhou, Xings ...
    Type: research-article
    2020 Volume 14 Issue 4 Pages 187-196
    Published: August 31, 2020
    Released: September 08, 2020
    [Advance publication] Released: August 27, 2020
    JOURNALS FREE ACCESS

    The incidence rate of thyroid carcinoma, especially papillary thyroid carcinoma (PTC), has increased significantly over time. As a primary pathway for metastasis, the lymphatic system is an important prognostic factor for PTC patients. Although the metabolic changes in PTC patients have been investigated in extensive studies, few studies focused on the whole blood metabolic profiling of PTC patients. In this study, we investigated the 1H NMR-based metabolic profiles of whole blood samples that were obtained from healthy individuals and PTC patients, with or without lymph node metastasis. The estimation of the predictive potential of metabolites was evaluated using multivariate statistical analyses, which revealed that the whole blood carries information that is sufficient for distinguishing between PTC patients and healthy individuals. However, PTC patients were not well classified as positive or negative according to the lymph nodes. We did not find a metabolite that could discriminate the presence of lymph node metastasis. Further studies with larger sample sizes are needed to elucidate significant metabolites to indicate the presence of lymph node metastasis in patients with PTC.

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Brief Report
  • Zhiyuan Lv, Shuo Wang, Wandong Zhao, Ningning He
    Type: brief-report
    2020 Volume 14 Issue 4 Pages 197-203
    Published: August 31, 2020
    Released: September 08, 2020
    [Advance publication] Released: August 29, 2020
    JOURNALS FREE ACCESS

    MicroRNAs (miRNAs) play a vital role in many biological processes, including cell growth, differentiation, apoptosis, development, differentiation, and carcinogenesis. Since miRNAs might play a part in cancer initiation and progression, they comprise an original class of promising diagnostic and prognostic molecular markers. In order to systematically understand the regulation of miRNA expression in cancers, the current study analyzed the miRNA expression profile in NCI-60 human cancer cell lines. Over 300 miRNAs exhibited unique expression profiles in cell lines derived from the same lineage. This study identified 9 lineage-specific miRNA expression patterns. Moreover, results indicated that miR-720 and miR-887 are expressed at relatively high levels in breast cancer cell lines compared to other types of cancer. Ultimately, matching NCI-60 drug response data to miR-720 and miR-887 expression profiles revealed that several FDA-approved drugs were inversely related to miR-720 and miR-887. Furthermore, the anti-cancer effect of perifosine was significantly enhanced by inhibiting miR-720 and decreased by miR-720 precursor treatment in breast cancer cell lines. 5-Fu treatment was enhanced by inhibiting miR-887 and decreased by miR-887 precursor treatment. The current results offer insight into the relationship between miRNA expression and their lineage types, and the approach used here represents a potential cancer therapy with the help of miRNAs.

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  • Yuki Kitamura, Ken-ichi Saeki
    Type: brief-report
    2020 Volume 14 Issue 4 Pages 204-208
    Published: August 31, 2020
    Released: September 08, 2020
    [Advance publication] Released: August 29, 2020
    JOURNALS FREE ACCESS

    To investigate the effect of fluorine substitution on tolbutamide (TB) hydroxylation catalyzed by CYP2C9, the hydroxylation of TB and its fluorinated derivative 3'-fluoro-tolbutamide (3'-F-TB) by recombinant human CYP2C9*1, CYP2C9*2, and CYP2C9*3 was analyzed. In general, fluorine substitution near the metabolic site may decrease enzymatic oxidation owing to its electron-withdrawing nature. Fluorine substitution reduced the Michaelis–Menten-derived Km of 4'-hydroxylation of TB catalyzed by CYP2C9*1 from 115 (TB) to 77 (3'-F-TB) µM. In the case of TB hydroxylation catalyzed by CYP2C9*2, the Km value of TB was also reduced by fluorine substitution from 129 to 88 µM. The greatest effect of fluorine substitution on the Km in TB hydroxylation was observed in the catalysis by CYP2C9*3, in which the Km value decreased from 287 to 117 µM. When a mixture containing TB and 3′-F-TB was hydroxylated by CYP2C9, the hydroxylated metabolite ratio in CYP2C9*3 was significantly increased compared with that in CYP2C9*1 and CYP2C9*2 (p < 0.01, Tukey–Kramer test). These results suggest that obtaining the metabolite profiles of fluorine-substituted analogs of the key substrate molecule may be useful as a new tool for phenotyping polymorphic CYP isoforms.

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Letter
  • Kanako Sonoda-Shimada, Ikko Kajihara, Masatoshi Jinnin, Hironobu Ihn
    Type: letter
    2020 Volume 14 Issue 4 Pages 209-210
    Published: August 31, 2020
    Released: September 08, 2020
    [Advance publication] Released: August 29, 2020
    JOURNALS FREE ACCESS

    Lupus myelitis is a rare but serious condition characterized by myelopathy in patients with systemic lupus erythematosus (SLE). Its presentation is usually acute or subacute, and it is often refractory to treatment. We reported a rare presentation of lupus myelitis in a 38-year-old Japanese woman with a 20-year history of SLE. She developed paraparesis and bladder/bowel dysfunction 6 months prior to presentation. Magnetic resonance imaging revealed atrophy of the entire thoracic spinal cord with high intensity on T1-weighted sequence. She was initially treated with intravenous pulse steroid therapy, and prednisolone (20 mg/day) was continued; mizoribine was changed to azathioprine (100 mg/day). In addition, she underwent a rehabilitation program to improve lower-extremity muscle weakness. Moreover, because of the refractory clinical condition, intravenous cyclophosphamide pulse therapy was added. Within 1 month, she could walk with a cane and had a desire to urinate and defecate. In conclusion, early and aggressive treatment improves the permanent damage of lupus myelitis.

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  • Atman Dash, Nitin Gupta, Yogiraj Ray, Parul Kodan, Binit Kumar Singh, ...
    Type: letter
    2020 Volume 14 Issue 4 Pages 211-212
    Published: August 31, 2020
    Released: September 08, 2020
    [Advance publication] Released: August 24, 2020
    JOURNALS FREE ACCESS

    The management of neurological infections due to non-tubercular mycobacteria is extremely challenging because of scarce literature, issues with penetration, lack of easily available susceptibility platforms and adverse effects associated with long term therapy. We report a case of a young girl with neurological infection due to rapidly growing mycobacteria to discuss the factors that should be considered while choosing the therapy for such rare and persistent infections.

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