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1.
Int J Mol Sci ; 23(22)2022 Nov 13.
Article in English | MEDLINE | ID: covidwho-2143225

ABSTRACT

Target-based drug design, a high-efficiency strategy used to guide the development of novel pesticide candidates, has attracted widespread attention. Herein, various natural-derived ferulic acid derivatives incorporating substituted isopropanolamine moieties were designed to target the tobacco mosaic virus (TMV) helicase. Bioassays demonstrating the optimized A19, A20, A29, and A31 displayed excellent in vivo antiviral curative abilities, affording corresponding EC50 values of 251.1, 336.2, 347.1, and 385.5 µg/mL, which visibly surpassed those of commercial ribavirin (655.0 µg/mL). Moreover, configurational analysis shows that the R-forms of target compounds were more beneficial to aggrandize antiviral profiles. Mechanism studies indicate that R-A19 had a strong affinity (Kd = 5.4 µM) to the TMV helicase and inhibited its ability to hydrolyze ATP (50.61% at 200 µM). Meanwhile, A19 could down-regulate the expression of the TMV helicase gene in the host to attenuate viral replication. These results illustrate the excellent inhibitory activity of A19 towards the TMV helicase. Additionally, docking simulations uncovered that R-A19 formed more hydrogen bonds with the TMV helicase in the binding pocket. Recent studies have unambiguously manifested that these designed derivatives could be considered as promising potential helicase-based inhibitors for plant disease control.


Subject(s)
Tobacco Mosaic Virus , Structure-Activity Relationship , Antiviral Agents/pharmacology , Antiviral Agents/chemistry , DNA Helicases
2.
Int J Mol Sci ; 23(16)2022 Aug 14.
Article in English | MEDLINE | ID: covidwho-1981428

ABSTRACT

The emergence of phytopathogenic bacteria resistant to antibacterial agents has rendered previously manageable plant diseases intractable, highlighting the need for safe and environmentally responsible agrochemicals. Inhibition of bacterial cell division by targeting bacterial cell division protein FtsZ has been proposed as a promising strategy for developing novel antibacterial agents. We previously identified 4'-demethylepipodophyllotoxin (DMEP), a naturally occurring substance isolated from the barberry species Dysosma versipellis, as a novel chemical scaffold for the development of inhibitors of FtsZ from the rice blight pathogen Xanthomonas oryzae pv. oryzae (Xoo). Therefore, constructing structure-activity relationship (SAR) studies of DMEP is indispensable for new agrochemical discovery. In this study, we performed a structure-activity relationship (SAR) study of DMEP derivatives as potential XooFtsZ inhibitors through introducing the structure-based virtual screening (SBVS) approach and various biochemical methods. Notably, prepared compound B2, a 4'-acyloxy DMEP analog, had a 50% inhibitory concentration of 159.4 µM for inhibition of recombinant XooFtsZ GTPase, which was lower than that of the parent DMEP (278.0 µM). Compound B2 potently inhibited Xoo growth in vitro (minimum inhibitory concentration 153 mg L-1) and had 54.9% and 48.4% curative and protective control efficiencies against rice blight in vivo. Moreover, compound B2 also showed low toxicity for non-target organisms, including rice plant and mammalian cell. Given these interesting results, we provide a novel strategy to discover and optimize promising bactericidal compounds for the management of plant bacterial diseases.


Subject(s)
Oryza , Xanthomonas , Anti-Bacterial Agents/chemistry , Bacterial Proteins/metabolism , Cell Division , Plant Diseases/microbiology , Plant Diseases/prevention & control , Podophyllotoxin/metabolism , Podophyllotoxin/pharmacology , Structure-Activity Relationship
3.
Geo Journal of Tourism and Geosites ; 42:824-831, 2022.
Article in English | ProQuest Central | ID: covidwho-1934960

ABSTRACT

The study aims to explore and review the scientific documents published in the pandemic covid-19 and tourism sector. The bibliometric analysis was used to collect and analyze scientific documents in the Web of Science database. The analysis used the R program to get information and map the main idea related to contributors in different objects, including the authors, institution, country and publication source, thematic mapping of the paper in covid-19 and tourism sector. The finding discovers 791 scientific documents and 320 sources. The finding emphasizes that the research topic in pandemic covid-19 and tourism sector is generally given information and benefit.

4.
Heliyon ; 7(10): e08230, 2021 Oct.
Article in English | MEDLINE | ID: covidwho-1474596

ABSTRACT

The Pandemic covid-19 spread globally has been given impact in the tourism industry, especially in the tourism destination. This study investigated to build the concept and theoretical framework that explains the decision of local tourist intention to visit a local destination in Indonesia post-pandemic covid-19. This study was considered the perception of Covid-19, non-pharmaceutical intervention and health consciousness by implying of Theory of Planned Behavior constructs. This study, health consciousness is the moderator variable to predict the decision of tourist to visit a destination. Structural Equation Model-Partial Least Square (SEM-PLS) was used to analyze the construct of study. The model found that the Theory of Planned Behavior was successfully broadened in making the decision of tourist to visit a destination post-covid-19 with considering non-pharmaceutical intervention and health consciousness. The results showed that generally the constructs of Theory Planned Behavior are significantly impacted in intention to visit a local destination in Indonesia, except Hypothesis of subjective norm and intention to visit was rejected. The variable health consciousness through intention to visit also was rejected. The framework also used moderating variable health consciousness between subjective norm and intention to visit was rejected. This study was given insight an issue of covid-19 in the tourism sector, and the implication was providing government, stakeholders, tourism marketers and policy-making with considering non-pharmaceutical and health consciousness during and post-pandemic covid-19.

5.
World J Clin Cases ; 9(15): 3644-3648, 2021 May 26.
Article in English | MEDLINE | ID: covidwho-1244999

ABSTRACT

BACKGROUND: Since the outbreak of the coronavirus disease 2019 (COVID-19) pandemic, the exclusion of a patient from COVID-19 should be performed before surgery. However, patients with type A acute aortic dissection (AAD) during pregnancy can seriously endanger the health of either the mother or fetus that requires emergency surgical treatment without the test for COVID-19. CASE SUMMARY: A 38-year-old woman without Marfan syndrome was admitted to the hospital because of chest pain in the 34th week of gestation. She has diagnosed as having a Stanford type-A AAD involving an aortic arch and descending aorta via aortic computed tomographic angiography. The patient was transferred to the isolated negative pressure operating room in one hour and underwent cesarean delivery and ascending aorta replacement. All medical staff adopted third-level medical protection measures throughout the patient transfer and surgical procedure. After surgery, the patient was transferred to the isolated negative pressure intensive care unit ward. The nucleic acid test and anti-COVID-19 immunoglobulin (Ig) G and IgM were performed and were negative. The patient and infant were discharged without complication nine days later and recovered uneventfully. CONCLUSION: The results indicated that the procedure that we used is feasible in patients with a combined cesarean delivery and surgery for Stanford type-A AAD during the COVID-19 outbreak, which was mainly attributed to rapid multidisciplinary consultation, collaboration, and quick decision-making.

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