28 research outputs found

    GC/MS analysis, free radical scavenging, anticancer and β-glucuronidase inhibitory activities of Trillium govanianum rhizome

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    The current study aims to investigate the phytochemical constituents, antioxidant, \u3b2-glucuronidase inhibitory and anticancer activities of Trillium govanianum rhizome. Phytochemical screening revealed the presence of steroidal glycosides, saponins, sterols, flavonoids and carbohydrates. GC/MS analyses of n-hexane fraction identified 12 compounds, including 70% unsaturated and 30% saturated fatty acids. Higher free radical scavenging capacity was observed in n-hexane and chloroform fraction compared with the other fractions. Based on IC50 (\u3bcg/mL) values, antiproliferative activity on HeLa cells was observed for chloroform (0.8 \ub1 0.2), ethyl acetate (1.4 \ub1 0.1) and butanol (1.6 \ub1 0.3) fractions by comparison to anticancer drug doxorubicin (0.3 \ub1 0.0). Similarly, all fractions exhibited cytotoxicity on PC-3 cells. Moreover, the methanol extract (IC50: 140.8 \ub1 3.8) and butanol fraction (196.2 \ub1 1.9) exhibited a moderate level of \u3b2-glucuronidase inhibitory activity. These findings may validate the folkloric uses of T. govanianum rhizome in cancer management, and can be a promising candidate as an anticancer agent

    Biological screening and docking studies of unique hybrids synthesized by conventional versus microwave assisted techniques

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    Purpose: To carry out the synthesis of various hybrids of 1,2,4-triazole in search of potential therapeutic enzyme inhibitory agents, and carry out docking and bovine serum albumin (BSA) binding studies on docking and bovine serum albumin (BSA) binding studies on the hybrids. Methods: The target compounds were synthesized by following a multistep protocol. Compound 1 was synthesized from 4-methoxybenzenesulfonyl chloride (a) and ethyl isonipecotate (b). Compound 1 was refluxed with hydrazine to synthesize compound 2, which was converted to compound 3 through two consecutive steps. Compound 4 and different amines (5a-5i), were utilized to synthesize an array of electrophiles (6a-6i). A series of 1,2,4-triazole hybrids (7a-7i) were synthesized at room temperature by stirring together 3 and 6a-6i. The final structures of 7a-7i were elucidated through 1H-NMR, 13C-NMR and EI-MS spectroscopy. The BSA binding studies were performed by fluorometric titration. Furthermore, antioxidant and enzyme inhibition activities were determined colorimetrically. Results: Compound 7d was the most active antioxidant agent, compared to butylated hydroxyanisole (BHA), while compounds 7d, 7e, 7f, 7g and 7i proved to be potent urease inhibitors with half-maximal inhibitory concentration (IC50) values of 19.5 ± 0.12, 21.1 ± 0.68, 18.2 ± 0.78, 19.9 ± 0.77 and 17.9 ± 0.10 µM, respectively, compared to thiourea with an IC50 of 24.3 ± 0.24 µM. Compounds 7a, 7b, 7d, and 7e exhibited high butyrylcholinesterase inhibition potential, compared to eserine. Conclusion: The synthesized compounds require studies further as potential therapeutic enzyme inhibitory agents in view of their urease inhibition as well as antioxidant activity

    Beneficial effects of Trillium govanianum rhizomes in pain and inflammation

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    Trillium govanianum rhizome is used as an analgesic and anti-inflammatory remedy in traditional medicine in northern Pakistan. In an attempt to establish its medicinal value, the present research evaluated the analgesic and anti-inflammatory potential of T. govanianum. The in vivo anti-inflammatory activity of extract and fractions was investigated in the carrageenan induced paw edema assay. The in vitro suppression of oxidative burst of extract, fractions and isolated compounds was assessed through luminol-enhanced chemiluminescence assay. The in vivo analgesic activity was assayed in chemical and thermal induced nociceptive pain models. The crude methanol extract and its solvent fractions showed anti-inflammatory and analgesic responses, exhibited by significant amelioration of paw edema and relieve of the tonic visceral chemical and acute phasic thermal nociception. In the oxidative burst assay, based on IC50 , the crude methanol extract and n-butanol soluble fraction produced a significant inhibition, followed by chloroform and hexane soluble fractions as compared to ibuprofen. Similarly, the isolated compounds pennogenin and borassoside E exhibited significant level of oxidative burst suppressive activity. The in vivo anti-inflammatory and analgesic activities as well as the in vitro inhibition of oxidative burst validated the traditional use of T. govanianum rhizomes as a phytotherapeutic remedy for both inflammatory conditions and pain. The observed activities might be attributed to the presence of steroids and steroid-based compounds. Therefore, the rhizomes of this plant species could serve as potential novel source of compounds effective for alleviating pain and inflammation

    Global Retinoblastoma Presentation and Analysis by National Income Level

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    Importance: Early diagnosis of retinoblastoma, the most common intraocular cancer, can save both a child's life and vision. However, anecdotal evidence suggests that many children across the world are diagnosed late. To our knowledge, the clinical presentation of retinoblastoma has never been assessed on a global scale. Objectives: To report the retinoblastoma stage at diagnosis in patients across the world during a single year, to investigate associations between clinical variables and national income level, and to investigate risk factors for advanced disease at diagnosis. Design, Setting, and Participants: A total of 278 retinoblastoma treatment centers were recruited from June 2017 through December 2018 to participate in a cross-sectional analysis of treatment-naive patients with retinoblastoma who were diagnosed in 2017. Main Outcomes and Measures: Age at presentation, proportion of familial history of retinoblastoma, and tumor stage and metastasis. Results: The cohort included 4351 new patients from 153 countries; the median age at diagnosis was 30.5 (interquartile range, 18.3-45.9) months, and 1976 patients (45.4) were female. Most patients (n = 3685 84.7%) were from low-and middle-income countries (LMICs). Globally, the most common indication for referral was leukocoria (n = 2638 62.8%), followed by strabismus (n = 429 10.2%) and proptosis (n = 309 7.4%). Patients from high-income countries (HICs) were diagnosed at a median age of 14.1 months, with 656 of 666 (98.5%) patients having intraocular retinoblastoma and 2 (0.3%) having metastasis. Patients from low-income countries were diagnosed at a median age of 30.5 months, with 256 of 521 (49.1%) having extraocular retinoblastoma and 94 of 498 (18.9%) having metastasis. Lower national income level was associated with older presentation age, higher proportion of locally advanced disease and distant metastasis, and smaller proportion of familial history of retinoblastoma. Advanced disease at diagnosis was more common in LMICs even after adjusting for age (odds ratio for low-income countries vs upper-middle-income countries and HICs, 17.92 95% CI, 12.94-24.80, and for lower-middle-income countries vs upper-middle-income countries and HICs, 5.74 95% CI, 4.30-7.68). Conclusions and Relevance: This study is estimated to have included more than half of all new retinoblastoma cases worldwide in 2017. Children from LMICs, where the main global retinoblastoma burden lies, presented at an older age with more advanced disease and demonstrated a smaller proportion of familial history of retinoblastoma, likely because many do not reach a childbearing age. Given that retinoblastoma is curable, these data are concerning and mandate intervention at national and international levels. Further studies are needed to investigate factors, other than age at presentation, that may be associated with advanced disease in LMICs. © 2020 American Medical Association. All rights reserved

    Management of acute coronary syndromes, a questionnaire survey of the clinical practice of cardiologists and other medical physicians belonging to west midland hospitals

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    OBJECTIVE: To assess the management of acute coronary syndromes by cardiologists and other medical physicians in a clinical setting. DESIGN: Questionnaire survey consisting of 10 hypothetical clinical scenarios and four possible therapeutic options for each scenario. SETTING: Consultants and specialist registrars in Cardiology (with or without access to interventional facilities) and consultant physicians belonging to various hospitals in the west midland region of United Kingdom. MAIN OUTCOME MEASURES: Respondents' ability to recognise high risk patients and their management of the hypothetical clinical cases. To establish any differences in management strategy between cardiologists and general physicians, and whether these differences, if any, relate to access to interventional cardiac facilities. RESULTS: Overall no significant differences were found in the responses between cardiologists and general physicians with or without access to cardiac interventional facilities. However, cardiologists were more inclined to use percutaneous transluminal coronary angioplasty (PTCA) compared to other physicians (scenario 8, 18.4% vs. 6.7%, p = 0.05 and scenario 9, 44.9% vs. 26.7%, p = 0.01). In two other situations, physicians from institutions with access to interventional facilities were more inclined to use 'other' treatment strategies (intravenous nitrates, antiplatelet treatment, inotropes, Intra-aortic balloon pump) compared to their colleagues from non-tertiary hospitals with no interventional facility on site (scenario 3, 21.7% vs. 2.4%, p = 0.04) and more use of PTCA ( scenario 6, 52.2% vs. 26.8%, p = 0.04). CONCLUSIONS: The management of acute coronary syndromes in this questionnaire survey was satisfactory and evidence based. No real differences were found between the management strategies adopted by cardiologists or non-cardiologists. Physicians working in centres with interventional facilities were no more inclined towards using primary PTCA or rescue angioplasty than those working in centres without such facilities

    Epidemiological and clinical characteristics of cases during the early phase of covid-19 pandemic: A systematic review and meta-analysis

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    10.3389/fneur.2020.00384Frontiers in Medicine715-Ja

    A Physics-Based Pattern Dictionary for EBSD Image Segmentation

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