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1.
Bol. latinoam. Caribe plantas med. aromát ; 23(1): 152-159, ene. 2024. graf
Article in English | LILACS | ID: biblio-1554187

ABSTRACT

Medicinal plants are used to cure diseases, and their replacement is frequent and affects public health. The genus Baccharis has representatives within the medicinal flora of Argentina, although the replacement of the species of this genus known under the vulgar name of "carqueja" by Baccharis spicata has been detected i n herbalists or markets of herbal products. The genotoxic safety of this species has been established in previous work of our group. The aim of this study was to evaluate the antiviral activity of an infusion made from B. spicata leaves against hepatitis B virus with the HepG2.2.15 cellular system and to determine cytotoxicity in HepG2.2,15, A549 and Vero cell lines. Infusion of B. spicata was active to inhibit HBV replication with an EC 50 of 22.54 µg/mL and a CC 50 of 190 µg/mL.


Las plantas medicinales son empleadas para la cura de enfermedades, y su sustituc ión es frecuente y afecta a la salud pública. El género Baccharis posee representantes dentro de la flora medicinal de Argentina, aunque se ha detectado la sustitución de las especies de dicho género conocidas bajo el nombre vulgar de "carqueja" por Baccha ris spicata en herboristerías o mercados de productos herb arios . Se ha establecido la seguridad genotóxica de esta especie en trabajos previos de nuestro grupo. Este estudio buscó evaluar la actividad antiviral de una infusión elaborada a partir de hojas de B. spicata frente al virus de la hepatitis B con el sistema celular HepG2.2.15 y determinar la citotoxicidad en las líneas celulares HepG2.2.15, A549 y Vero. La infusión de B. spicata fue activa para inhibir la replicación del virus con un EC 50 de 22.54 µg/mL y un CC 50 de 190 µg/mL.


Subject(s)
Baccharis/drug effects , Baccharis/chemistry , Hepatitis B/drug therapy , Plants, Medicinal/chemistry , Cell Line/metabolism , Medicine, Traditional/methods
2.
Bol. latinoam. Caribe plantas med. aromát ; 22(6): 747-769, nov. 2023. ilus, tab, graf
Article in English | LILACS | ID: biblio-1554217

ABSTRACT

Larrea divaricata Cav. is an autochthonous South American plant popularly used in inflammatory and infectious diseases with reported anti - inflammatory, immunomodulatory, antimicrobial and antioxidant activities. Covid - 19 is an infection ca used by the severe acute respiratory syndrome coronavirus 2 (SARS - CoV - 2). This virus can cause pneumonia and even death in about 5% of the cases. The objective of the article was to demonstrate, through a literature review, that L. divaricata has sufficie nt attributes to be assayed against SARS - CoV - 2. For this, the chemical composition, reported activities and docking studies were taken into account. This review demonstrated that the plant extracts are capable of inhibiting the proliferation of fungi, bact eria and viruses and that they exert anti - inflammatory and immunomodulatory actions in different " in vitro " and " in vivo " models. These results suggest that the plant is a good candidate to be studied for the prevention and/or treatment of SARS - CoV - 2.


Larrea divaricata Cav. es una planta autóctona Sudamericana, utilizada popularmente en enfermedades inflamatorias e infecciosas, con activida d anti - inflamatoria, inmunomoduladora, antimicrobiana y antioxidante reportada. El Covid - 19 es una infección causada por una cepa de coronavirus, SARS - CoV - 2 (coronavirus tipo 2 causante del síndrome respiratorio agudo severo). Este virus puede originar neu monía e incluso la muerte en alrededor del 5% de los casos. Nuestro objetivo fue demostrar, a través de una revisión bibliográfica, que esta planta tiene atributos suficientes para ser ensayada en estudios contra SARS - CoV - 2. Se tuvo en cuenta la composici ón química, los antecedentes científicos y los estudios de acoplamiento molecular. Esta revisión permitió demostrar que extractos de la planta son capaces de inhibir la proliferación de hongos, bacterias y virus y que presentan acción anti - inflamatoria en diferentes modelos " in vitro " e " in vivo ", lo que los hace candidatos a ser estudiados en la prevención y/o tratamiento de la infección contra SARS - CoV - 2.


Subject(s)
Larrea/chemistry , COVID-19/prevention & control , COVID-19/therapy , Antiviral Agents/therapeutic use , Plants, Medicinal/chemistry , Plant Extracts/pharmacology
3.
Chinese Journal of Biotechnology ; (12): 4784-4795, 2023.
Article in Chinese | WPRIM | ID: wpr-1008058

ABSTRACT

The aim of this study was to produce recombinant porcine interferon gamma (rPoIFN-γ) by Chinese hamster ovarian (CHO) cells expression system and to analyze its antiviral activity. Firstly, we constructed the recombinant eukaryotic expression plasmid pcDNA3.1-PoIFN-γ and transfected into suspension cultured CHO cells for secretory expression of rPoIFN-γ. The rPoIFN-γ was purified by affinity chromatography and identified with SDS-PAGE and Western blotting. Subsequently, the cytotoxicity of rPoIFN-γ was analyzed by CCK-8 test, and the antiviral activity of rPoIFN-γ was evaluated using standard procedures in VSV/PK-15 (virus/cell) test system. Finally the anti-Seneca virus A (SVA) of rPoIFN-γ activity and the induction of interferon-stimulated genes (ISGs) and cytokines were also analyzed. The results showed that rPoIFN-γ could successfully expressed in the supernatant of CHO cells. CCK-8 assays indicated that rPoIFN-γ did not show cytotoxicity on IBRS-2 cells. The biological activity of rPoIFN-γ was 5.59×107 U/mg in VSV/PK-15 system. Moreover, rPoIFN-γ could induced the expression of ISGs and cytokines, and significantly inhibited the replication of SVA. In conclusion, the high activity of rPoIFN-γ was successfully prepared by CHO cells expression system, which showed strong antiviral activity on SVA. This study may facilitate the investigation of rPoIFN-γ function and the development of novel genetically engineered antiviral drugs.


Subject(s)
Animals , Cricetinae , Swine , Interferon-gamma/pharmacology , Cricetulus , CHO Cells , Sincalide , Recombinant Proteins/pharmacology , Antiviral Agents/pharmacology
4.
Acta Pharmaceutica Sinica ; (12): 360-370, 2023.
Article in Chinese | WPRIM | ID: wpr-965699

ABSTRACT

Carnosic acid (CA) is the main phenolic diterpenoid active ingredient in plants such as rosemary and sage, and has antiviral, antioxidant, anti-inflammatory effects and so on, however, its antiviral activity against influenza virus infections was not reported. In this study, antiviral activities against influenza A virus infections of three main bioactive ingredients from rosemary, including rosmarinic acid, CA and ursolic acid, were evaluated using virus titer titration assay, and CA showed remarkable inhibition on influenza H5N1 replication in A549 cells. The antiviral activity of CA was further confirmed and its mechanism of action was investigated using the indirect immunofluorescence assay (IFA), Western blot and real-time fluorescence quantification polymerase chain reaction (qRT-PCR). The results showed that the 50% effective concentration (EC50) of CA against influenza H5N1 in A549 cells and MDCK cells were 4.30 and 3.64 μmol·L-1, respectively. Meanwhile, CA also showed inhibition on influenza virus 2009panH1N1 (EC50: 10.1 μmol·L-1) and H3N2 (EC50: 12.8 μmol·L-1) replications in A549 cells. Mechanistic studies showed that antiviral activity of CA is related to its induction of heme oxygenase-1 (HO-1) in A549 cells and suppression on production of reactive oxygen in H5N1-infected cells.

5.
Chinese Pharmacological Bulletin ; (12): 1791-1800, 2022.
Article in Chinese | WPRIM | ID: wpr-1014248

ABSTRACT

Aim To investigate the inhibition effects and mechanisms of aristolochic acids(AAs)against herpes simplex virus(HSV)in vitro and in vivo. Methods The cytopathic effect(CPE), plaque assay, indirect immunofluorescence and others were used to explore the anti-HSV effects and mechanisms of aristolochic acid in Vero cells, and the in vivo anti-HSV activity of AAs was evaluated using HSV-1 infected BALB/c mouse model. Results The IC

6.
Tropical Biomedicine ; : 257-264, 2022.
Article in English | WPRIM | ID: wpr-940061

ABSTRACT

@#Newcastle Disease (ND) is a highly pathogenic disease of avian species which is caused by Newcastle Disease Virus (NDV). It is one of the major causes of mortality and morbidity to poultry industry in the third world countries. Currently, there is no treatment measures against ND; the only existing measure is vaccination, though it is incapable to offer 100% immunity. In Tanzania, the leaves of Synadenium glaucescens Pax. are traditionally used for treatment of various ailments including ND. Previously, its leaves extract has been scientifically confirmed to exhibit anti-NDV activity though bioactive compound(s) responsible for this activity is/are unknown. Therefore, this study was aimed to evaluate anti-NDV activity of 3β-Friedelanol (1) and 3α-friedelanol (2) isolated from its leaves extract. Isolation of these compounds was achieved by column chromatography method whereas, their chemical structures were determined by Nuclear Magnetic Resonance (NMR) data and by comparing with the available literature NMR data. Anti-NDV activity study was done in embryonated chicken eggs (ECEs). Treatment of NDV inoculated ECEs with 3β-Friedelanol (1) reduced the viral load to zero and maintained the survival of embryos, this was revealed by continuous organs formation and increase in embryo weights with no significant different (p > 0.05) from un-inoculated ECE. These effects suggest that, 3β-Friedelanol (1) possesses anti-NDV activity. Therefore, existence of 3β-Friedelanol (1) in the leaves of S. glaucescens may justify its earlier described anti-NDV activity and traditional use in the treatment of ND. Hence, its leaves extract may be considered for development of anti-NDV herbal formulation while 3β-Friedelanol could either serve as a drug or lead compound for synthesis of anti-NDV drugs.

7.
Braz. J. Pharm. Sci. (Online) ; 58: e18802, 2022. tab, graf
Article in English | LILACS | ID: biblio-1403736

ABSTRACT

Abstract The flavonoids and xanthones present in the ethanol extracts of leaves and stems of Fridericia samydoides showed that anti-dengue activities in vitro were investigated qualitatively by liquid chromatography-ultraviolet-mass spectrometry in series. Nineteen flavones and fifteen xanthones were detected and characterized on the basis of their fragmentation pattern in the positive and negative ion mode tandem mass spectrometry spectra and ultraviolet bands. Acacetin, chrysin, vitexin, isovitexin, orientin, isoorientin, mangiferin, 2'-O-trans-caffeoylmangiferin, 2'-O-trans-coumaroylmangiferin and 2'-O-trans-cinnamoylmangiferin were identified by comparison with authentic samples. The other compounds detected were tentatively assigned by analysis of the spectral data and by comparison with literature reports. In addition, it performed the fractionation of the leaves extract leading to the isolation of mangiferin, isovitexin and isoorientin. All extracts and isolated compounds inhibited the Dengue virus replication cycle with EC50 less than 25.0 µg/mL for extracts and 272.5, 85.6 and 79.3 µg/mL for mangiferin, isovitexin and isoorientin, respectively.


Subject(s)
Flavonoids/agonists , Bignoniaceae/adverse effects , Dengue Virus , Xanthones/agonists , Mass Spectrometry/methods , In Vitro Techniques/instrumentation , Chromatography, Liquid/methods , Tandem Mass Spectrometry/methods
8.
Article in English | LILACS-Express | LILACS, VETINDEX | ID: biblio-1484783

ABSTRACT

Abstract Background Hepatitis C virus (HCV) infection is a major worldwide health problem that can cause liver fibrosis and hepatocellular carcinoma (HCC). The clinical treatment of HCV infection mainly relies on the use of direct-acting antivirals (DAAs) that are usually expensive and have side effects. Therefore, achieving the discovery of more successful agents is always urgent. In this context, antiviral compounds that inhibit viral infections and disease progression with important therapeutic activities have been identified in animal venoms including arthropod toxins. This indicates that arthropod venoms represent a good natural source of promising candidates for new antivirals. Methods The antiviral activity of the wasp venom (WV), isolated from the Oriental hornet (Vespa orientalis), was assessed using cell culture technique with human hepatocellular carcinoma-derived cell line (Huh7it-1) and the recombinant strain of HCV genotype 2a (JFH1). Results The results revealed that WV inhibited HCV infectivity with 50% inhibitory concentration (IC50) of 10 ng/mL, while the 50% cytotoxic concentration (CC50) was 11,000 ng/mL. Time of addition experiment showed that the WV blocked HCV attachment/entry to the cells probably through virucidal effect. On the other hand, the venom showed no inhibitory effect on HCV replication. Conclusion WV can inhibit the entry stage of HCV infection at non-cytotoxic concentrations. Therefore, it could be considered a potential candidate for characterization of natural anti-HCV agents targeting the entry step.

9.
J. venom. anim. toxins incl. trop. dis ; 27: e20210039, 2021. tab, graf, ilus
Article in English | LILACS, VETINDEX | ID: biblio-1351021

ABSTRACT

Background Hepatitis C virus (HCV) infection is a major worldwide health problem that can cause liver fibrosis and hepatocellular carcinoma (HCC). The clinical treatment of HCV infection mainly relies on the use of direct-acting antivirals (DAAs) that are usually expensive and have side effects. Therefore, achieving the discovery of more successful agents is always urgent. In this context, antiviral compounds that inhibit viral infections and disease progression with important therapeutic activities have been identified in animal venoms including arthropod toxins. This indicates that arthropod venoms represent a good natural source of promising candidates for new antivirals. Methods The antiviral activity of the wasp venom (WV), isolated from the Oriental hornet (Vespa orientalis), was assessed using cell culture technique with human hepatocellular carcinoma-derived cell line (Huh7it-1) and the recombinant strain of HCV genotype 2a (JFH1). Results The results revealed that WV inhibited HCV infectivity with 50% inhibitory concentration (IC50) of 10 ng/mL, while the 50% cytotoxic concentration (CC50) was 11,000 ng/mL. Time of addition experiment showed that the WV blocked HCV attachment/entry to the cells probably through virucidal effect. On the other hand, the venom showed no inhibitory effect on HCV replication. Conclusion WV can inhibit the entry stage of HCV infection at non-cytotoxic concentrations. Therefore, it could be considered a potential candidate for characterization of natural anti-HCV agents targeting the entry step.(AU)


Subject(s)
Antiviral Agents , Wasp Venoms , Carcinoma, Hepatocellular
10.
Chinese Journal of Pharmacology and Toxicology ; (6): 733-733, 2021.
Article in Chinese | WPRIM | ID: wpr-909577

ABSTRACT

OBJECTIVE Human metapneumovirus (hMPV) is semblable to respiratory syncytial virus (RSV) which causes respiratory infections typically characterized by cough, runny nose, fever, and nasal congestion but sometimes progressing to bronchiolitis and pneumonia. Whereas, there is no corresponding drug to inhabit the virus. Studies of new compounds with potential anti-HMPV activity could produce clinical value. Chinese herbal medicine played a great role during COVID-19, therefore we choose some small molecular (JH001) extracted from botany to investigate therapeutic effect on hMPV and the underlying mechanisms. METHODS In this study, 16HBE cells were used as a model to explore in vitro antiviral effect. Cytotoxicity assays were performed before the antiviral tests, cell viability of 16HBE cells handled by different concentration of JH001 was estimated by Cell Counting Kit-8 (CCK-8). Then RT-qPCR, immunofluores?cence, and flow cytometer were used to test the viral titer after cells infected with hMPV. Eventually, 6-8 weeks mice were infected intranasally with 60 μL of hMPV, the control group was treated with 0.9% saline water, other groups were administered with JH001 and ribavirin, then the lung virus titer and protective effect in lung were judged. RESULTS The obtained JH001 exhibited no cytotoxicity to 16HBE cells during 6.25 - 200 μmol · L-1. RT-QPCR demonstrated that JH001 showed obvious inhabitation to the viral replication and showed great significance compared with saline. And fluo?rescence exhibited distinct decrease of hMPV-N protein, flow cytometer results showed that MFI decrease evidently. Sig?nificant reduction of N-gene expression was observed in those mice treated with JH001 compared with saline group, which indicated that JH001 probably had protective and therapeutic effect on viral replication. CONCLUSION This study illustrated that JH001 might be a promising option for small molecular against hMPV and JH001 might be worthy of fur?ther development and used as a potential therapeutic strategy for other respiratory viruses in the future.

11.
Acta Pharmaceutica Sinica ; (12): 793-798, 2021.
Article in Chinese | WPRIM | ID: wpr-876516

ABSTRACT

Dengue virus (DENV) is the most rapidly transmitted mosquito-borne pathogen, which is the main cause of seasonal outbreaks of dengue fever and dengue hemorrhagic fever in tropical and subtropical regions, and may cause serious life-threatening diseases. There is an urgent need to develop effective vaccines or antiviral therapies. In this paper, we found that a podocarpane-type diterpenoid, (3α,5β,10α)-13-methoxypodocarpa-8,11,13-triene-3,12-diol (MPTD), isolated from the stems and leaves of Aleurites moluccana, showed good effect against DENV. The anti-DENV activity of MPTD against four different DENV serotypes was studied by plaque assay. The cytotoxicity of MPTD in Vero and Huh7 cells was tested by MTT assay. qRT-PCR and Western blot assays were used to investigate the anti-DENV activity of MPTD at RNA and protein levels, respectively. The results showed that MPTD greatly reduced the virus titer in DENV infected Vero cells, and its 50% effective concentration (EC50) for DENV (1–4) were 2.72 ± 0.39, 10.99 ± 5.18, 18.72 ± 0.21, and 0.48 ± 0.28 μmol·L-1, respectively. The results showed that MPTD inhibits DENV RNA level and the expression of E protein. In addition, MPTD may inhibit the early stage of DENV replication and exert antiviral activity. Further studies showed that the inhibitory effect of MPTD against DENV infection is not targeting the viral entry stage. Therefore, MPTD has a significant anti-dengue virus effect, and is an anti-DENV compound with potential application value.

12.
Acta Pharmaceutica Sinica ; (12): 1429-1433, 2021.
Article in Chinese | WPRIM | ID: wpr-887079

ABSTRACT

Two dimeric diterpenoid alkaloids were isolated from the whole plant of Aconitum tanguticum (Maxim.) Stapf and their structures were elucidated by extensive analysis of 1D, 2D-NMR and HR-MS data. One is a new compound and named tanguticurine A (1), and the other is the known compound anthoroidine B (2); both were isolated from this plant for the first time. The antiviral activity of compounds 1 and 2 against HCV and EV71 were also evaluated. It was found that compound 1 had a good inhibitory effect on HCV and EV71 with EC50 values of 15.5 and 9.7 μmol·L-1, respectively, and showed low cytotoxicity. Therefore, compound 1 is a good antiviral lead compound and deserves further study.

13.
Article | IMSEAR | ID: sea-210735

ABSTRACT

Two new geldanamycin derivatives such as 17-(tryptamine)-17-demethoxygeldanamycin (2) andC17 methoxyl of geldanamycin (1). Their antiviral activity was evaluated based on influenza virus propagation inembryonated chicken eggs and viral absorption by hemagglutination (HA) inhibition test. The findings indicatedthat these compounds inhibited viral propagation at a concentration of 12.5 µg/ml. For the viral absorption, onlycompounds 2 and 3 inhibited HA at a concentration of 50 µg/ml. The solubility of compounds 2 and 3 in waterwas 290 and 306 µM, higher than that of compound 1 about 1.91 and 2.01 times, respectively. The compounds 2and 3 showed a moderate cytotoxic activity on LLC-MK2 and Vero cells with IC50 values of >200.00 µg/ml. Theseresults demonstrated the invention of tryptamine-geldanamycin hybrids to prevent influenza virus infection in viralabsorption and viral propagation steps.

14.
Rev. colomb. ciencias quim. farm ; 49(1): 218-233, Jan.-Apr. 2020. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1144348

ABSTRACT

SUMMARY Chalcones highlights as an important structure in medicinal chemistry and thus has been widely used as a template in the development of new drugs. In this study, we aim to determine the antibacterial, anti-Candida, and anti-Dengue potential of new chalcone-bearing 2,4-dihydroxyl and tetrahydropyranyl moieties. Antimicrobial activity assays showed that microorganism of the Staphylococcus genus (including methicillin-resistant strains) were susceptible to 2,4-dihydroxychalcones, with minimum inhibitory concentrations (MICs) ranging of 19.5 to 125 µg.mL-1. Compound 4e, which showed the highest bacteriostatic effect, also has bactericidal activity from of 80 µg.mL-1. The growth of oral isolates of Candida albicans was also efficiently inhibited with compound 4e (MIC: 15.6-32.3 µg.mL-1), which was fungicidal at 15.6 µg.mL-1. However, the presence of the tetrahydropyranyl moiety impaired both the antibacterial and antifungal effects. None of the chalcones tested were actives against Dengue virus serotype 2. In conclusion, the compound 4e showed good anti-Staphylococci and anti-Candida activity and may be a promising prototype for the development of new antimicrobial agents.


RESUMEN Las chalconas se destacan como una estructura importante en la química médica y, por lo tanto, se ha empleado como prototipo para el desarrollo de nuevos fármacos. En este estudio, nuestro objetivo fue determinar el potencial antibacteriano, anti Candida y anti-Dengue de las nuevas chalconas que poseen los grupos 2,4-dihidroxilo y tetrahidropiranilo. El ensayo de actividad antimicrobiana mostró que las bacterias del género Staphylococcus (incluidas las cepas resistentes a la meticilina) fueron sensibles a las 2,4-dihidroxicalconas estudiadas, con concentraciones inhibitorias mínimas (CIM) que oscilan entre 19,5 y 125 µg.mL-1. El compuesto 4e, que tuvo el mejor efecto bacteriostático, también mostró un efecto bactericida a partir de la concentración de 80 µg.mL-1. El crecimiento de los aislamientos orales de Candida albicans también se inhibió eficientemente con el compuesto 4e (CIM: 15.6-32.3 µg.mL-1), que fue fungicida a una concentración de 15.6 µg.mL-1. Sin embargo, la presencia del grupo tetrahidropiranilo perjudicó la actividad antibacteriana y anti-fúngica de los análogos de la chalcona. Además, ninguno de los compuestos evaluados mostró un efecto contra el virus del dengue serotipo 2. En conclusión, el compuesto 4e muestra una buena actividad anti-estafilocócica y anti-Candida y puede ser un prototipo prometedor para el desarrollo de nuevos agentes antimicrobianos.


RESUMO As chalconas se destacam como uma importante estrutura na química medicinal e dessa forma tem sido empregada como um protótipo para o desenvolvimento de novos fármacos. Nesse estudo, nós objetivamos determinar o potencial antibacteriano, anti-Candida, e anti-Dengue de novas chalconas que possuem os grupos 2,4-dihidroxil e tetrahidropiranil. O ensaio de atividade antimicrobiana mostrou que bactérias do gênero Staphylococcus (incluindo linhagens resistentes a meticilina) foram sensíveis para as 2,4-dihidroxichalconas estudadas, com concentrações inibitórias mínimas (CIM) variando de 19,5 para 125 Dengue potential of new chalcone µg.mL-1. O composto 4e, o qual apresentou o melhor efeito bacteriostático, também mostrou efeito bactericida a partir da concentração de 80 µg.mL-1. O crescimento de isolados orais de Candida albicans foi também eficientemente inibido com o composto 4e (CIM: 15.6-32.3 µg.mL-1), o qual foi fungicida a concentração de 15,6 µg.mL-1. Entretanto, a presença do grupo tetrahidropiranil prejudicou a atividade antibacteriana e antifúngica dos análogos de chalcona. Adicionalmente, nenhum dos compostos avaliados mostrou efeito contra o vírus da dengue sorotipo 2. Em conclusão, o composto 4e apresenta boa atividade anti-estafilocóccica e anti-Candida, e pode ser um promissor protótipo para o desenvolvimento de novos agentes antimicrobianos.

15.
Acta Pharmaceutica Sinica B ; (6): 512-528, 2020.
Article in English | WPRIM | ID: wpr-792992

ABSTRACT

A series of 2-(((5-akly/aryl-1-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3)-ones were synthesized and their anti-HIV-1 activities were evaluated. Most of these compounds were highly active against wild-type (WT) HIV-1 strain (IIIB) with EC values in the range of 0.0038-0.4759 μmol/L. Among those compounds, had an EC value of 3.8 nmol/L and SI (selectivity index) of up to 25,468 indicating excellent activity against WT HIV-1. anti-HIV-1 activity and resistance profile studies suggested that compounds and displayed potential anti-HIV-1 activity against laboratory adapted strains and primary isolated strains including different subtypes and tropism strains (ECs range from 4.3 to 63.6 nmol/L and 18.9-219.3 nmol/L, respectively). On the other hand, it was observed that those two compounds were less effective with EC values of 2.77 and 4.87 μmol/L for HIV-1A (K103N + Y181C). The activity against reverse transcriptase (RT) was also evaluated for those compounds. Both and obtained sub-micromolar IC values showing their potential in RT inhibition. The pharmacokinetics examination in rats indicated that compound has acceptable pharmacokinetic properties and bioavailability. Preliminary structure-activity relationships and molecular modeling studies were also discussed.

16.
Chinese Traditional and Herbal Drugs ; (24): 256-264, 2020.
Article in Chinese | WPRIM | ID: wpr-846715

ABSTRACT

Euphorbiae Ebracteolatae Radix is the dry root of plant Euphorbia fischeriana or E. ebracteolata of Euphorbiaceae, which is a widely utilized natural medicine with broad development prospect. It has been discovered that Euphorbiae Ebracteolatae Radix contains several biologically active constituents, among which diterpenoids are the most important. The diterpenoids of Euphorbiae Ebracteolatae Radix contain eight types including abietane-type, tigliane-type, pimarane-type, rosane-type, cembrane-type, ent-kaurane-type, ingenane-type and atisane-type. Diterpenoids of Euphorbiae Ebracteolatae Radix have significant anti-tumor, anti-inflammatory, anti-viral and other pharmacological activities. In this paper, the chemical constituents of diterpenoids and pharmacological activities of Euphorbiae Ebracteolatae Radix in recent years were reviewed in order to provide references for better developing the resources of Euphorbiae Ebracteolatae Radix and its clinical application.

17.
Chinese Traditional and Herbal Drugs ; (24): 3070-3077, 2020.
Article in Chinese | WPRIM | ID: wpr-846403

ABSTRACT

Since the coronavirus disease 2019 (COVID-19) outbreak, National Health Commission of the People's Republic of China and local departments have released a number of diagnosis and treatment plans for COVID-19. One of the recommended prescriptions for severe stage treatment is Huanglian Jiedu Decoction, whose TCM syndrome is corresponding to the severe syndrome of dual blaze of qi and nutrient in the COVID-19 protocol of Diagnosis and Treatment of Novel Coronavirus Pneumonia (trial version 7). Huanglian Jiedu Decoction can be used in the treatment of syndrome of dual blaze of qi and nutrient. Syndrome of dual blaze of qi and nutrient is with consumption of nutrient yin of body fluid, pathogenic qi always triumphing over healthy qi, excessive noxious heat from qi and nutrient, Huanglian Jiedu Decoction has the efficacy of clearing heat and detoxicating. It can achieve the therapeutic purpose of nourishing yin and protecting yin by removing evil spirits. Modern pharmacological studies have shown that Huanglian Jiedu Decoction has potential effects of anti-inflammatory and antipyretic, antiviral, antioxidant, regulating immunity and protecting viscera and tissues in the treatment of COVID-19 with severe syndrome of dual blaze of qi and nutrient. In this paper, the pathogenesis evolution of COVID-19 with severe syndrome of dual blaze of qi and nutrient, the relationship between prescriptions and syndromes of Huanglian Jiedu Decoction and its modern pharmacological effects was analyzed, so as to provide a basis for the effective treatment of Huanglian Jiedu Decoction in COVID-19 with severe syndrome of dual blaze of qi and nutrient.

18.
China Pharmacy ; (12): 1166-1171, 2020.
Article in Chinese | WPRIM | ID: wpr-821601

ABSTRACT

OBJECTIVE:To eva luate content constituent characteristics and antiviral activity of main flavonnoids in genuine and non-genuine Scutellaria baicalensis ,and to investigate quality-efficiency relationship and effective substance. METHODS : Totally 8 batches of S. baicalensis from different origins (S1-S8)were collected to prepare its water extract lyophilized powder. UPLC method was used to determine the contents of baicalin ,wogonoside,baicalein and wogonin ,and calculate their content constituent ratio. According to the content constituent ratio of flavonoids in S. baicalensis from different origins ,the mixture of the above four components was prepared as the corresponding simulated sample of flavonoids (E1-E8). Using ribavirin as positive control,MTT assay and CPE method were used to investigate half toxic concentration (TD50)of the water extract from 8 batches of S. baicalensis and their corresponding simulated samples to human laryngeal carcinoma cell Hep-2 and their half inhibition concentration(IC50)to respiratory syncytial virus (RSV);treatment indexes (TI)were calculated. Pearson correlation analysis for the content of baicalin ,wogonoside,baicalein and wogonin with their anti-RSV activity (IC50)was performed by SPSS 17.0 software. RESULTS :The contents of baicalin and wogonoside in sample S 4(from Hebei Chengde )were the highest ,and the contents of baicalein and wogonin in sample S 6(from Inner Mongolia- 2)were the highest. The contents of above 4 components were the lowest in sample S 6,S6,S7(from Beijing ),S4. The contents of flavonoid glycosides in sample S 4 were relatively higher, while those of corresponding glycosides were relatively lower ;the content constituent ratio of baicalin , wogonoside,baicalein and wogonin was 1∶0.224∶0.111∶0.013. The contents of flavonoid glycosides in sample S6 wererelatively lower ,while those of glycosides were relatively 126.com higher;the content constituent ratio of above 4 components was 1∶0.241∶0.713∶0.106. TC 50 of S. bai calensis water extracts from different origins to Hep- 2 cells was all higher than 50 μg/mL, IC50 to RSV was 11.11-51.74 μg/mL;TI was 1.86-5.20. TC 50 of corresponding simulated samples of flavonoids was 23.11-52.23 μg/mL,while IC 50 to RSV was 4.87-14.61 μg/mL;TI was 1.85-4.75. The anti-RSV effects of water extract of S 4 from genuine origins(Hebei Chengde )and its corresponding simulated sample E 4 were the strongest. Correlation analysis showed that the correlation coefficient between the contents of 4 flavonoids and antiviral activity was less than 0.5,and there was no significant correlation between them. CONCLUSIONS :When the content constituent ratio of 4 main flavonoids in S. baicalensis was 1∶0.224∶ 0.111 ∶ 0.013,it has a strong inhibition effect on RSV. S. baicalensis from genuine origins has better constituent characteristics of flavonoids,which may be the important material basis for the best antiviral effect of genuine medicinal material.

19.
Acta Pharmaceutica Sinica ; (12): 703-719, 2020.
Article in Chinese | WPRIM | ID: wpr-820866

ABSTRACT

Long-term use of approved antiviral drugs can lead to drug resistance and side effects. On the other hand, there are currently no antiviral drugs or vaccines available to treat some newly emerging virus infections. Therefore, antiviral drugs research has always been a hot research topic in the field of medicinal chemistry. Natural products are an important source of antiviral drugs. This article reviews the progress of antiviral natural products discovered in the past decade to provide potential lead compounds for drug development.

20.
Chinese Pharmacological Bulletin ; (12): 508-513, 2020.
Article in Chinese | WPRIM | ID: wpr-856994

ABSTRACT

Aim To investigate the antiviral activity and mechanism of myricetin against enterovirus 71 (E V 7 1) infection. Methods The cytopathic effect (CPE) and plaque assay were used to observe the antiviral effect of myricetin against EV71 in Vero cell. The cells were treated with myricetin at different concentrations combined with crystal violet staining to detectthe cytotoxicity of myricetin. The effect of myricetin on VP1 protein expression was detected by Western blot. The effect of myricetin on VP1 gene expressionwas evaluated byRT-PCR. Results Myricetin pretreatment at 2. 5-20 fimol L-1' significantly inhibitedcell death induced by EV71 infection in a dose-dependent manner with the IC50 value of 5. 6 jxmol • L-1. Compared to virus control group, myricetin could significantly reduce the viral titer at the concentration of 2. 5 ~ 20 u,mol • L-1. The results of Western blot and RT-PCR showed that myricetin could markedlyreduce the gene and protein expression levels of viral capsid protein VP1. Conclusion Myricetin has significant antiEV71 activity in vitro.

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