Effective Compound
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2022 ◽  
Author(s):  
Mengnan Qi ◽  
Li Pan ◽  
Ying Gao ◽  
Miao Li ◽  
Yanjin Wang ◽  
...  

African swine fever (ASF) is a highly contagious disease with high morbidity and mortality caused by African swine fever virus (ASFV). Cleaning and disinfection remain one of the most effective biosecurity measures to prevent and control the spread of ASFV. In this study, we evaluated the inactivation effects of highly complexed iodine (HPCI) combined with compound organic acids (COAs) against ASFV under different conditions. The results showed that the inactivation rates of the disinfectants on the reporter ASFV increased in dose- and time-dependent manners, the best inactivation effects were obtained when the compatibility ratio of HPCI and COAs was 5:1 at 25°C. Furthermore, there were no significant differences by comparing the efficacy of HPCI combined with COAs (HPCI+COAs) in inactivating wild-type ASFV and the reporter ASFV (P > 0.05). ASFV of 104.0 TCID50/mL was completely inactivated by 0.13% HPCI (0.0065% effective iodine), 0.06% COAs or 0.13% HPCI+COAs (approximately 0.0054% effective iodine), respectively, while 106.0 TCID50/mL ASFV was completely inactivated by 1.00% HPCI (0.05% effective iodine), 0.50% COAs or 1.00% HPCI+COAs (0.042% effective iodine), respectively. Therefore, HPCI+COAs had synergistic effects to inactivate ASFV. This study demonstrated that HPCI+COAs could rapidly and efficiently inactivate ASFV and represent an effective compound disinfectant for the control of ASF.


2022 ◽  
Author(s):  
Dao-jin Xue ◽  
Zheng Zhen ◽  
Ke-xin Wang ◽  
Jia-lin Zhao ◽  
Yao Gao ◽  
...  

Abstract Background Chinese herbal medicine (CHM) is characterized by “multi- compounds, multi-targets and multi-pathway”, which has advanced benefits for the preventing and treating complex diseases, but still exists unsolved issues, mainly include unclear material basis and underling mechanism of prescription. Integrated pharmacology is a hot cross research area based on system biology, mathematic and poly-pharmacology. It can systematically and comprehensively investigate the therapeutic reaction of compounds or drugs on pathogenic genes network, and is especially suitable for the study of complex CHM systems. Intracerebral Hemorrhage (ICH) is one of the main causes of death among Chinese residents, which is characterized by high mortality and high disability rate. In recent years, the treatment of ICH by CHM has been deeply researched. Xue Fu Zhu Yu Decoction (XFZYD), one of the commonly used prescriptions in treating ICH at clinic level, has not been clear about its mechanism in treating ICH. Methods Here, we established a strategy, which based on compounds-targets, pathogenetic genes, network analysis and node importance calculation. Using this strategy, the core compounds group (CCG) of XFZYD was predicted and validated by in vitro experiments. The molecular mechanism of XFZYD in treating ICH was deduced based on CCG and their targets. Results The results show that the CCG with 43 compounds predicted by this model is highly consistent with the corresponding Compound-Target (C-T) network in terms of gene coverage, enriched pathway coverage and accumulated contribution of key nodes at 89.49%, 88.72% and 90.11%, respectively, which confirmed the reliability and accuracy of the effective compound group optimization and mechanism speculation strategy proposed by us. Conclusions Our strategy of optimizing the effective compound groups and inferring the mechanism provides a strategic reference for explaining the optimization and inferring the molecular mechanism of prescriptions in treating complex diseases of CHM.


Author(s):  
C Martina ◽  
L Krenn ◽  
L Krupicka ◽  
H Yamada ◽  
R Hood-Nowotny ◽  
...  

Abstract Plant-based repellents represent a safe, economic, and viable alternative to managing invasive insects that threaten native fauna. Observations of self-medication in animals can provide important cues to the medicinal properties of plants. A recent study in the Galapagos Islands found that Darwin’s finches apply the leaves of Psidium galapageium (Hooker 1847) to their feathers, extracts of which were repellent to mosquitoes and the parasitic fly Philornis downsi (Dodge & Aitkens 1968; Diptera: Muscidae). Introduced mosquitoes are suspected vectors of avian pathogens in the Galapagos Islands, whereas the larvae of P. downsi are blood-feeders, causing significant declines of the endemic avifauna. In this study, we investigated the volatile compounds found in P. galapageium, testing each against a model organism, the mosquito Anopheles arabiensis (Patton 1905; Diptera: Culicidae), with the aim of singling out the most effective compound for repelling dipterans. Examinations of an ethanolic extract of P. galapageium, its essential oil and each of their respective fractions, revealed a mixture of monoterpenes and sesquiterpenes, the latter consisting mainly of guaiol, trans-nerolidol, and β-eudesmol. Of these, trans-nerolidol was identified as the most effective repellent to mosquitoes. This was subsequently tested at four different concentrations against P. downsi, but we did not find a repellence response. A tendency to avoid the compound was observed, albeit significance was not achieved in any case. The lack of repellence suggests that flies may respond to a combination of the volatile compounds found in P. galapageium, rather than to a single compound.


2021 ◽  
Vol 23 (Supplement_6) ◽  
pp. vi78-vi78
Author(s):  
Tadeusz Wroblewski ◽  
Philip Tatman ◽  
Anthony Fringuello ◽  
Sam Scherer ◽  
William Foreman ◽  
...  

Abstract BACKGROUND Glioma and glioblastoma comprise 28% of all primary central nervous system tumors and cause the majority of primary brain tumor deaths. Despite substantial research into the molecular pathogenesis and genetic landscape of glioma, no currently approved therapies are curative for any glioma or glioblastoma. Patients with glioblastoma have an average survival time of 12-15 months, while patients with grade III gliomas have an average survival time of 3-5 years, and patients with grade II gliomas have an average survival time of 8-15 years. The lack of a curative treatment for these tumors necessitates additional research into novel therapies. METHODS In this study, we developed a high-throughput drug screen and culture system to identify existing FDA-approved therapies with the potential to inhibit glioma viability. RESULTS In total, we screened 39 tumors: 21 glioblastoma, 10 oligodendroglioma, and 8 astrocytoma. Carfilzomib was the most effective compound across the cohort, decreasing the average tumor viability to 39.0% +/- 16.5%SD. Regardless of tumor grade, MGMT methylation, EGFR amplification, tumor recurrence and etiology, tumor histology, prior treatment, and patient gender, carfilzomib significantly reduced cell viability in every tumor; though was not necessarily the most effective compound in each of these groups. We found HDAC inhibition to be the most effective treatment in grade 1 astrocytomas. However, HDAC inhibition was surpassed by carfilzomib and RNA transcription inhibitors in all higher grades. Interestingly, EGFR inhibition, while significantly effective in 36 tumors, was consistently less effective than carfilzomib across the cohort, though did surpass the effectiveness of HDAC inhibition in grade III gliomas. CONCLUSIONS FDA approved compounds can effectively inhibit glioma tumor viability. Specifically, carfilizomib holds great promise. Further in vivo studies are needed to confirm these findings.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Agnieszka Gęgotek ◽  
Sinemyiz Atalay ◽  
Elżbieta Skrzydlewska

AbstractUV radiation is known to induce a multiple changes in the metabolism of skin-building cells, what can affect the functioning not only neighboring cells, but also, following signal transduction releasing into the blood vessels, the entire body. Therefore, the aim of this study was to analyze the proteomic disturbances occurred in plasma of chronically UVA/UVB irradiated rats and define the effect on these changes of skin topically applied cannabidiol (CBD). Obtained results showed significant changes in the expression of numerous anti-inflammatory and signaling proteins including: NFκB inhibitor, 14-3-3 protein, protein kinase C, keratin, and protein S100 after UV irradiation and CBD treatment. Moreover, the effects of UVA and UVB were manifested by increased level of lipid peroxidation products—protein adducts formation. CBD partially prevented all of these changes, but in a various degree depending on the UV radiation type. Moreover, topical treatment with CBD resulted in the penetration of CBD into the blood and, as a consequence, in direct modifications to the plasma protein structure by creating CBD adducts with molecules, such as proline-rich protein 30, transcription factor 19, or N-acetylglucosamine-6-sulfatase, what significantly changed the activity of these proteins. In conclusion, it may be suggested that CBD applied topically may be an effective compound against systemic UV-induced oxidative stress, but its effectiveness requires careful analysis of CBD's effects on other tissues of the living organism.


Author(s):  
C. Muñoz-Shugulí ◽  
F. J. Rodríguez ◽  
A. Guarda ◽  
M. J. Galotto

Eugenol (EUG) is the principal component of clove essential oil. It has demonstrated excellent antifungal properties against B. cinerea, one of the most important fungus in the fresh fruit decay. However, this substance is highly volatile, thermolabile and the direct contact with a food induce undesirable changes in the organoleptic properties. For this reason, the application of EUG represents a big challenger and its encapsulation through inclusion complexes formation with β-cyclodextrin (β-CD) is presented as a solution. In this way, the aim of this work was to develop, characterize and assess the antifungal capacity of inclusion complexes β-CD:EUG. For this, co-precipitation was used as method of inclusion complexes synthesis. The quantity of entrapped EUG was determined by gaseous chromatography. The inclusion complexes were characterized by thermogravimetric analysis (TGA) and Fourier transform infrared (FTIR). Moreover, the antifungal activity was probed in a headspace system. Results showed that the EUG entrapped quantity was of 68,5 mg/g inclusion complexes. Furthermore, the characteristic peaks of EUG did not appear in inclusion complexes TGA thermogram and FTIR spectrum which confirm the effective compound encapsulation. Finally, inclusion complexes inhibited the growing of A. cinerea at 53% and avoided the fungal sporulation. These findings suggest that the β- CD:EUG inclusion complexes are suitable to use in the storage and transportation of fresh fruits to prevent their deterioration. Keywords: Botrytis cinerea, fresh fruits, headspace. Resumen El eugenol (EUG) es el principal componente del aceite esencial de clavo de olor. Éste ha destacado por su efectivo control de Botrytis cinerea, uno de los hongos más importantes que provoca la pudrición de frutas frescas. Sin embargo, esta sustancia es altamente volátil, termolábil y provoca cambios desagradables en las propiedades organolépticas del alimento si está en contacto directo con el mismo, por lo que su aplicación presenta un gran desafío. Ante esto, se propone su encapsulación a través de la formación de complejos de inclusión con β-ciclodextrina (β-CD). En este sentido, el objetivo de la presente investigación fue desarrollar, caracterizar y evaluar la capacidad antifúngica de complejos de inclusión β-CD:EUG. Éstos se sintetizaron mediante el método de co-precipitación, y la cantidad de EUG atrapada en la β-CD fue cuantificada por cromatografía de gases. Los complejos de inclusión se caracterizaron a través de análisis termogravimétrico (TGA) y espectroscospía infrarroja con transformada de Fourier (FTIR). Además, su actividad antifúngica se evaluó en un sistema de espacio de cabeza. Los resultados mostraron que la cantidad de EUG atrapada fue de 68,5 mg/g de complejo de inclusión. Además, en su termograma TGA y espectro FTIR no se observaron los picos característicos del EUG, confirmando la efectiva encapsulación del compuesto. Finalmente, los complejos de inclusión inhibieron el 53% del crecimiento de B. cinerea y evitaron su esporulación. Estos resultados permiten sugerir el uso de complejos de inclusión β-CD:EUG en el almacenamiento y transporte de frutas frescas para prevenir su deterioro. Palabras clave: Botrytis cinerea, frutas frescas, espacio de cabeza.


2021 ◽  
pp. 139-162
Author(s):  
Edward Shorter

This chapter considers the physicians who advised the pharmaceutical industry in the interest of bringing an effective compound to the attention of the profession. It mentions Roland Kuhn, the Swiss asylum psychiatrist who in 1957 discovered the effectiveness of imipramine in depression and advised about marketing strategies to use to sell the drug. It also highlights the true nature of the testimonials of physicians, which is well known to the industry. The industry’s contempt for them is shown by its vernacular term for sources, which are called “stables.” The chapter focuses on the “stables” of the 1980s that later became Key Opinion Leaders (KOLs). It points out that the sardonic term KOL first appeared in industry correspondence as an insider expression for academics.


2021 ◽  
Vol 22 (13) ◽  
pp. 6764
Author(s):  
Tomoshige Kino ◽  
Irina Burd ◽  
James H. Segars

The coronavirus disease 2019 (COVID-19) caused by infection of the severe respiratory syndrome coronavirus-2 (SARS-CoV-2) significantly impacted human society. Recently, the synthetic pure glucocorticoid dexamethasone was identified as an effective compound for treatment of severe COVID-19. However, glucocorticoids are generally harmful for infectious diseases, such as bacterial sepsis and severe influenza pneumonia, which can develop respiratory failure and systemic inflammation similar to COVID-19. This apparent inconsistency suggests the presence of pathologic mechanism(s) unique to COVID-19 that renders this steroid effective. We review plausible mechanisms and advance the hypothesis that SARS-CoV-2 infection is accompanied by infected cell-specific glucocorticoid insensitivity as reported for some other viruses. This alteration in local glucocorticoid actions interferes with undesired glucocorticoid to facilitate viral replication but does not affect desired anti-inflammatory properties in non-infected organs/tissues. We postulate that the virus coincidentally causes glucocorticoid insensitivity in the process of modulating host cell activities for promoting its replication in infected cells. We explore this tenet focusing on SARS-CoV-2-encoding proteins and potential molecular mechanisms supporting this hypothetical glucocorticoid insensitivity unique to COVID-19 but not characteristic of other life-threatening viral diseases, probably due to a difference in specific virally-encoded molecules and host cell activities modulated by them.


Author(s):  
Wei Hu ◽  
Rongkun Zheng ◽  
Yihong Liao ◽  
Fan Kuang ◽  
Zhaolan Yang ◽  
...  

Abstract The insecticides of microbial origin may be promising biocontrol agents to control pests. In this study, a major metabolite was extracted and purified from Serratia marcescens KH-001 and identified as prodigiosin with a molecule weight of 324.2094, and our primary aim was to evaluate the effects of prodigiosin against Diaphorina citri Kuwayama (Hemiptera: Liviidae) in the laboratory and in the field. Toxicity of purified prodigiosin to nymphs increased with increasing temperature from 25 to 35°C. The laboratory experiment results observed inhibition effects of purified prodigiosin at LC50 on oviposition and egg hatch of D. citri at 30°C. Furthermore, adults that fed on citrus leaves treated with LC20 and LC50 solution of purified prodigiosin at 30°C excreted less honeydew (28–35%) compared with controls, suggesting moderate antifeedant activity of prodigiosin. The results of field experiment showed that 10% prodigiosin emulsifiable concentrate exhibited better control efficacy (70–100%) at three concentrations (100, 200, and 500 mg/liter) in July and August than in October. These data indicate that prodigiosin will be a highly effective compound for the control of D. citri depending on the prevailing temperature conditions and may become a commercially available product to be widely used in citrus orchards.


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