Your browser doesn't support javascript.
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 487
Filtrar
Mais filtros










Intervalo de ano de publicação
1.
J Agric Food Chem ; 67(43): 11942-11947, 2019 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-31622090

RESUMO

Manilkara zapota, usually known as Sapodilla, is a fairly slow-growing evergreen tropical tree which belongs to the genus Manilkara (Sapotaceae), indigenous to Central America, southern Mexico, and the Caribbean. The ripe fruits of M. zapota have been widely consumed as an uniquely flavored tropical fruit and verified to hold a variety of health benefits. In order to investigate the potential health-promoting chemical compositions from the fruits of M. zapota cultivated in Hainan Island of China, a systematic and in-depth phytochemical study on this fruit was accordingly implemented. In our current study, three new prenylated coumarins, manizapotins A-C (1-3), together with seven known prenylated coumarins (4-10), were separated from the fruits of M. zapota. The chemical structures of new prenylated coumarins 1-3 were unambiguously established by means of comprehensive spectroscopic analyses, and the known compounds 4-10 were determined by comparing their experimental spectral data with those described data in the literature. This is the first time to discover prenylated coumarins occurring in M. zapota. The potential anti-inflammatory effects and anti-HIV (human immunodeficiency virus) activities of all these separated prenylated coumarins were assessed. Prenylated coumarins 1-10 dispalyed remarkable inhibitory effects against nitric oxide production induced by lipopolysaccharide in mouse macrophage RAW 264.7 cells with the IC50 values equivalent to that of hydrocortisone in vitro. Meanwhile, prenylated coumarins 1-10 exhibited pronounced anti-HIV-1 reverse transcriptase activities with the EC50 values in range of 0.12-8.69 µM. These results suggest that appropriate and reasonable consumption of the fruits of M. zapota might assist people to prevent and reduce the occurrence of inflammatory diseases together with the infection of HIV. Furthermore, the discovery of these prenylated coumarins from the fruits of M. zapota holding pronounced anti-inflammatory effects along with anti-HIV activities could be of great significance to the research and development of new natural anti-inflammatory and anti-HIV agents.


Assuntos
Fármacos Anti-HIV/química , Anti-Inflamatórios/química , Cumarínicos/química , Manilkara/química , Extratos Vegetais/química , Animais , Fármacos Anti-HIV/isolamento & purificação , Fármacos Anti-HIV/farmacologia , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , China , Cumarínicos/isolamento & purificação , Cumarínicos/farmacologia , Frutas/química , Transcriptase Reversa do HIV/antagonistas & inibidores , Transcriptase Reversa do HIV/metabolismo , HIV-1/efeitos dos fármacos , HIV-1/enzimologia , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Camundongos , Estrutura Molecular , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Prenilação , Células RAW 264.7
2.
Fitoterapia ; 139: 104388, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31655087

RESUMO

A new lignan, thoreliin A (1), and a new bisnorlignan, thoreliin B (2), were isolated from a MeOH extract of the rhizomes of Boesenbergia thorelii. In addition, the known bisnorlignans 3 and 4, neolignan 5, phenylpropanoids 6-15, as well as benzenoids 18-21 were also obtained from the same source. The structures were elucidated based on their spectroscopic data. By single crystal X-ray analysis, the relative stereochemistry of 1 was confirmed. All isolated compounds were evaluated for anti-HIV-1 activities. Among them, thoreliin A (1) exhibited anti-HIV-1 activities on both HIV-1 reverse transcriptase (41.43% inhibition at 200 µg/mL) and syncytium reduction assays (EC50 20.6 µM, SI 3.7), while compounds 3-6, 9 and 11-21 showed anti-HIV-1 activity only in the anti-syncytium assay (EC50 6.6-454.1 µM, SI >1.32-7.75).


Assuntos
Fármacos Anti-HIV/farmacologia , HIV-1/efeitos dos fármacos , Lignanas/farmacologia , Rizoma/química , Zingiberaceae/química , Fármacos Anti-HIV/isolamento & purificação , Lignanas/isolamento & purificação , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Tailândia
3.
Anal Chim Acta ; 1056: 79-87, 2019 May 16.
Artigo em Inglês | MEDLINE | ID: mdl-30797464

RESUMO

Combination antiretroviral therapy (cART) regimens are recommended for HIV patients to better achieve and maintain plasma viral suppression. Despite adequate plasma viral suppression, HIV persists inside the brain, which is, in part thought to result from poor brain penetration of antiretroviral drugs. In this study, a simple and ultra-sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for simultaneous determination of tenofovir, emtricitabine, and dolutegravir in cell lysates of an immortalized human brain microvascular endothelial cell line (hCMEC/D3) was developed and validated. Analytes were separated on a reverse phase C18 column using water and 0.1% formic acid in acetonitrile as mobile phases. The analytes were detected using positive electrospray ionization mode with multiple reaction monitoring (MRM). The assay was linear in the concentration range of 0.1-100 ng mL-1 for all analytes. Intra- and inter-assay precision and accuracy were within ±13.33% and ±10.53%, respectively. This approach described herein was used to determine the intracellular accumulation of tenofovir, emtricitabine, dolutegravir simultaneously in hCMEC/D3 cells samples.


Assuntos
Fármacos Anti-HIV/análise , Encéfalo/citologia , Cromatografia Líquida/métodos , Células Endoteliais/citologia , Espaço Intracelular/química , Espectrometria de Massas em Tandem/métodos , Métodos Analíticos de Preparação de Amostras , Fármacos Anti-HIV/isolamento & purificação , Linhagem Celular , Emtricitabina/análise , Emtricitabina/isolamento & purificação , Compostos Heterocíclicos com 3 Anéis/análise , Compostos Heterocíclicos com 3 Anéis/isolamento & purificação , Humanos , Modelos Lineares , Reprodutibilidade dos Testes , Tenofovir/análise , Tenofovir/isolamento & purificação
4.
Bioorg Chem ; 83: 1-5, 2019 03.
Artigo em Inglês | MEDLINE | ID: mdl-30339860

RESUMO

Two new monoterpene indole alkaloids, naucleaoffines A (1) and B (2), together with six known alkaloids (3-8), were isolated from the stems and leaves of Nauclea officinalis. The structures of 1 and 2 were elucidated by extensive spectroscopic methods and the known compounds were identified by comparisons with the data reported in literature. All isolated compounds were evaluated for their anti-inflammatory activities and anti-HIV-1 activities. Compounds 1-8 exhibited significant inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide in mouse macrophage RAW 264.7 cells in vitro with IC50 values comparable to that of hydrocortisone. In addition, compounds 1-8 showed significant anti-HIV-1 activities with EC50 ranged from 0.06 to 2.08 µM. These findings suggest that the discoveries of these indole alkaloids with significant anti-inflammatory activities and anti-HIV-1 activities isolated from N. officinalis could be of great importance to the development of new anti-inflammatory and anti-HIV agents.


Assuntos
Fármacos Anti-HIV/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Alcaloides Indólicos/farmacologia , Monoterpenos/farmacologia , Rubiaceae/química , Animais , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Relação Dose-Resposta a Droga , HIV-1/efeitos dos fármacos , Alcaloides Indólicos/química , Alcaloides Indólicos/isolamento & purificação , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Camundongos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Monoterpenos/química , Monoterpenos/isolamento & purificação , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Células RAW 264.7 , Relação Estrutura-Atividade
5.
Fitoterapia ; 131: 265-271, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30414876

RESUMO

Six new xanthone-derived polyketides, named phomoxanthones F-K (1-6), along with three known ones, were isolated from Phomopsis sp. xy21, which was isolated as an endophytic fungus from the Thai mangrove Xylocarpus granatum. Phomoxanthone F (1) represents the first xanthone-derived polyketide containing a 10a-decarboxylated benzopyranone nucleus that was substituted by a 4-methyldihydrofuran-2(3H)-one moiety at C10a. Phomoxanthones G (2) and H (3) are highly oxidized xanthone-derived polyketides containing a novel 5-methyl-6-oxabicyclo[3.2.1]octane motif. This is the first report of a C6-O-C12 bridge in xanthone-derived polyketides. Additionally, a plausible biogenetic pathway for these xanthone-derived polyketides is proposed.


Assuntos
Ascomicetos/química , Meliaceae/microbiologia , Policetídeos/isolamento & purificação , Xantonas/isolamento & purificação , Fármacos Anti-HIV/isolamento & purificação , Linhagem Celular Tumoral , Endófitos/química , Humanos , Estrutura Molecular , Tailândia
6.
Bioorg Med Chem ; 26(23-24): 6050-6055, 2018 12 15.
Artigo em Inglês | MEDLINE | ID: mdl-30448257

RESUMO

Based on genome mining, a new lasso peptide specialicin was isolated from the extract of Streptomyces specialis. The structure of specialicin was established by ESI-MS and NMR analyses to be a lasso peptide with the length of 21 amino acids, containing an isopeptide bond and two disulfide bonds in the molecule. The stereochemistries of the constituent amino acids except for Trp were determined to be L and the stereochemistry of Trp at C-terminus was determined to be D. Three dimensional structure of specialicin was determined based on NOE experimental data, which indicated that specialicin possessed the similar conformational structure with siamycin I. Specialicin showed the antibacterial activity against Micrococcus luteus and the moderate anti-HIV activity against HIV-1 NL4-3. The biosynthetic gene cluster of specialicin was proposed from the genome sequence data of S. specialis.


Assuntos
Antibacterianos/farmacologia , Fármacos Anti-HIV/farmacologia , HIV/efeitos dos fármacos , Micrococcus luteus/efeitos dos fármacos , Peptídeos/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Relação Dose-Resposta a Droga , Peptídeos e Proteínas de Sinalização Intercelular , Testes de Sensibilidade Microbiana , Conformação Molecular , Família Multigênica , Peptídeos/química , Peptídeos/genética , Peptídeos/isolamento & purificação , Streptomyces/química , Relação Estrutura-Atividade
7.
J Nat Prod ; 81(7): 1619-1627, 2018 07 27.
Artigo em Inglês | MEDLINE | ID: mdl-30010341

RESUMO

A novel cycloartane triterpenoid alkaloid, kleinhospitine E (1), six new cycloartane triterpenoids (2-7), three known cycloartane triterpenoids (8-10), and taraxerone (11) were isolated from a methanol extract of Kleinhovia hospita. Their structures were elucidated by 1D- and 2D-NMR spectroscopy as well as HRMS analysis. The absolute configurations of all isolated compounds were determined from their ECD spectra by comparison with theoretical values. Kleinhospitine E (1) is the first cycloartane alkaloid possessing an unusual γ-lactam with an oxopropylidene side chain. Compounds 2, 3, and 6 were assigned as cycloartane triterpenoids with a 9α,10α-cyclopropyl ring, which is found rarely among naturally occurring compounds, while 4 and 5 were established as isomers of compound 3 containing a 21,23-diacetal side chain. Biological evaluation revealed that compounds 4 and 9 exhibited more potent antiproliferative activities against a multidrug-resistant tumor cell line compared with its parent chemosensitive cell line. Furthermore, compound 6 exhibited submicromolar anti-HIV activity.


Assuntos
Malvaceae/química , Extratos Vegetais/farmacologia , Triterpenos/isolamento & purificação , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Fármacos Anti-HIV/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Extratos Vegetais/química , Triterpenos/química , Triterpenos/farmacologia
8.
Plant Mol Biol ; 97(4-5): 357-370, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29948657

RESUMO

KEY MESSAGE: The potent anti-HIV microbicide griffithsin was expressed to high levels in tobacco chloroplasts, enabling efficient purification from both fresh and dried biomass, thus providing storable material for inexpensive production and scale-up on demand. The global HIV epidemic continues to grow, with 1.8 million new infections occurring per year. In the absence of a cure and an AIDS vaccine, there is a pressing need to prevent new infections in order to curb the disease. Topical microbicides that block viral entry into human cells can potentially prevent HIV infection. The antiviral lectin griffithsin has been identified as a highly potent inhibitor of HIV entry into human cells. Here we have explored the possibility to use transplastomic plants as an inexpensive production platform for griffithsin. We show that griffithsin accumulates in stably transformed tobacco chloroplasts to up to 5% of the total soluble protein of the plant. Griffithsin can be easily purified from leaf material and shows similarly high virus neutralization activity as griffithsin protein recombinantly expressed in bacteria. We also show that dried tobacco provides a storable source material for griffithsin purification, thus enabling quick scale-up of production on demand.


Assuntos
Fármacos Anti-HIV/metabolismo , Inibidores da Fusão de HIV/metabolismo , Infecções por HIV/tratamento farmacológico , HIV-1/efeitos dos fármacos , Lectinas de Plantas/metabolismo , Tabaco/metabolismo , Fármacos Anti-HIV/isolamento & purificação , Cloroplastos/genética , Cloroplastos/metabolismo , Genoma de Cloroplastos/genética , Inibidores da Fusão de HIV/isolamento & purificação , Infecções por HIV/virologia , Humanos , Agricultura Molecular , Folhas de Planta/genética , Folhas de Planta/metabolismo , Lectinas de Plantas/genética , Lectinas de Plantas/isolamento & purificação , Tabaco/genética
9.
Viruses ; 10(7)2018 06 27.
Artigo em Inglês | MEDLINE | ID: mdl-29954099

RESUMO

Natural products originating from marine and plant materials are a rich source of chemical diversity and unique antimicrobials. Using an established in vitro model of HIV-1 latency, we screened 257 pure compounds from a marine natural product library and identified 4 (psammaplin A, aplysiatoxin, debromoaplysiatoxin, and previously-described alotaketal C) that induced expression of latent HIV-1 provirus in both cell line and primary cell models. Notably, aplysiatoxin induced similar levels of HIV-1 expression as prostratin but at up to 900-fold lower concentrations and without substantial effects on cell viability. Psammaplin A enhanced HIV-1 expression synergistically when treated in combination with the protein kinase C (PKC) activator prostratin, but not the histone deacetylase inhibitor (HDACi) panobinostat, suggesting that psammaplin A functions as a latency-reversing agent (LRA) of the HDACi class. Conversely, aplysiatoxin and debromoaplysiatoxin synergized with panobinostat but not prostratin, suggesting that they function as PKC activators. Our study identifies new compounds from previously untested marine natural products and adds to the repertoire of LRAs that can inform therapeutic "shock-and-kill"-based strategies to eliminate latent HIV-infected reservoirs.


Assuntos
Fármacos Anti-HIV/farmacologia , Organismos Aquáticos/química , Produtos Biológicos/farmacologia , Descoberta de Drogas , HIV-1/efeitos dos fármacos , Latência Viral/efeitos dos fármacos , Fármacos Anti-HIV/isolamento & purificação , Produtos Biológicos/isolamento & purificação , Linfócitos T CD4-Positivos/virologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Dissulfetos/farmacologia , Infecções por HIV/virologia , HIV-1/fisiologia , Ensaios de Triagem em Larga Escala , Humanos , Panobinostat/farmacologia , Ésteres de Forbol/farmacologia , Provírus , Tirosina/análogos & derivados , Tirosina/farmacologia , Ativação Viral/efeitos dos fármacos
10.
Bioorg Chem ; 79: 111-114, 2018 09.
Artigo em Inglês | MEDLINE | ID: mdl-29738969

RESUMO

A novel tetrahydrofuran derivative, trigonohowine (1), together with five known tetrahydrofuran derivatives (2-6), were isolated from the stems and leaves of Trigonostemon howii. The structure of 1 was elucidated by extensive spectroscopic methods and the known compounds were identified by comparisons with the data reported in literature. Among them, trigonohowine (1) represents the first example of a new type of tetrahydrofuran derivative, possessing an unprecedented carbon skeleton containing 23 carbon atoms on the carbon skeleton and the known compouds (2-6) are rare tetrahydrofuran derivatives in the plant kingdom with various carbon skeletons. All isolated compounds were evaluated for their anti-HIV-1 activities. Compounds 1-6 showed significant anti-HIV-1 activities with EC50 ranged from 0.08 to 1.03 µM. These findings suggest that the discoveries of these tetrahydrofuran derivatives with significant anti-HIV-1 activities isolated from T. howii could be of great importance to the development of new anti-HIV agents.


Assuntos
Fármacos Anti-HIV/farmacologia , Euphorbiaceae/química , Furanos/farmacologia , HIV-1/efeitos dos fármacos , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Linhagem Celular , Furanos/química , Furanos/isolamento & purificação , Humanos , Estrutura Molecular , Folhas de Planta/química , Caules de Planta/química
11.
Chem Biodivers ; 15(5): e1700557, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29521032

RESUMO

Collagen is the most studied protein with a wide range of applications including pharmaceutical, biomedical, cosmetics, leather, and film industries due to its special characteristics that are high biocompatibility, good bioactivity, and weak antigenicity. Although collagen sources are abundant, the outbreak of varied diseases among land animals posed threat to its utilization in our daily life. Thus, a probe for an alternative source began, which in turn revealed the immense untapped marine sources, such as fish, jellyfish, and some marine Mammals. The present article deals with a brief description of collagen, its characteristics, marine sources, extraction, collagen peptides and their biological activities, potential use and application in various field.


Assuntos
Fármacos Anti-HIV/farmacologia , Anti-Hipertensivos/farmacologia , Antioxidantes/farmacologia , Pesquisa Biomédica , Colágeno/farmacologia , Animais , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Anti-Hipertensivos/química , Anti-Hipertensivos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Colágeno/química , Colágeno/isolamento & purificação , HIV-1/efeitos dos fármacos , Humanos , Envelhecimento da Pele/efeitos dos fármacos , Cicatrização/efeitos dos fármacos
12.
Chem Biodivers ; 15(5): e1700560, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29569369

RESUMO

Three new compounds (1 - 3), including two euphane type triterpenes, 24,24-dimethoxy-25,26,27-trinoreuphan-3ß-ol (1) and (24S)-24-hydroperoxyeupha-8,25-dien-3ß-ol (2), and an ent-atisine diterpene, ent-atisane-3α,16α,17-triol (3), were isolated from an acetone extract of the stems of Euphorbia antiquorum, together with eight known diterpenes (4 - 11). The structures of compounds (1 - 11) were elucidated using NMR and MS spectroscopic methods. Compound 7 showed moderate activity against HIV-1 replication in vitro (EC50 = 1.38 µm).


Assuntos
Fármacos Anti-HIV/farmacologia , Euphorbia/química , HIV-1/efeitos dos fármacos , Terpenos/farmacologia , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Linhagem Celular Transformada , Transformação Celular Viral/efeitos dos fármacos , Relação Dose-Resposta a Droga , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade , Terpenos/química , Terpenos/isolamento & purificação , Replicação Viral/efeitos dos fármacos
13.
Phytochemistry ; 147: 68-79, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29304383

RESUMO

Eleven previously undescribed compounds, including four benzophenones (garciosones A-D), four xanthones (garciosones E-H) and three biphenyls (garciosines A-C), along with eighteen known compounds were isolated from the stems, leaves and twigs of Garcinia speciosa Wall. (Clusiaceae). Their structures were established by extensive spectroscopic analysis. For garciosines A-C, the structures were confirmed by single crystal X-ray diffraction analysis. Most of the isolated compounds were evaluated for their cytotoxic activity and anti-HIV-1 activity using the syncytium inhibition assay and HIV-1 reverse transcriptase (RT) assay. The known compounds, 4,6,3',4'-tetrahydroxy-2-methoxybenzophenone and macluraxanthone, displayed significant cytotoxic activity with the ED50 in the range of 1.85-11.76 µM. 1,5-Dihydroxyxanthone exhibited the most potent anti-HIV activity against syncytium formation with EC50 < 17.13 µM (SI > 25.28) and 2-(3,3-dimethylallyl)-1,3,7-trihydroxyxanthone was the most active compound in the HIV-1 reverse transcriptase assay with IC50 value of 58.24 µM. Structure-activity relationship of some isolated compounds were also discussed.


Assuntos
Fármacos Anti-HIV/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Benzofenonas/farmacologia , Compostos de Bifenilo/farmacologia , Garcinia/química , HIV-1/efeitos dos fármacos , Xantonas/farmacologia , Animais , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Benzofenonas/química , Benzofenonas/isolamento & purificação , Compostos de Bifenilo/química , Compostos de Bifenilo/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Infecções por HIV/tratamento farmacológico , Humanos , Camundongos , Estrutura Molecular , Folhas de Planta/química , Caules de Planta/química , Ratos , Relação Estrutura-Atividade , Xantonas/química , Xantonas/isolamento & purificação
14.
Chem Biodivers ; 15(3): e1700411, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29369483

RESUMO

Two eudesmane sesquiterpene lactones, wedetrilides B (1) and C (2), along with five known analogues (3 - 8), an ent-kaurane diterpenoid (9), a steroid (10), as well as cinnamic acid derivatives (11 - 13), were isolated from the flowers of Wedelia trilobata. Their structures were elucidated on the basis of extensive spectroscopic analyses and by comparison of their NMR data with those of related compounds. Furthermore, the structures of 1 and 3 - 5 were confirmed by X-ray single-crystal diffraction analyses. Compounds 4 and 5 exhibited weak cytotoxic activities against the MCF-7, HeLa, and A549 cell lines. Compounds 3 - 5 were also evaluated for their inhibitory effects against HIV lytic replication.


Assuntos
Fármacos Anti-HIV/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Flores/química , HIV/efeitos dos fármacos , Sesquiterpenos/farmacologia , Wedelia/química , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Relação Estrutura-Atividade , Replicação Viral/efeitos dos fármacos
15.
Phytochemistry ; 145: 1-9, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29031114

RESUMO

Scuteformoids A-J, ten previously undescribed neo-clerodane diterpenoids along with one known analogue, were isolated from petroleum ether soluable fraction of the whole plants of Scutellaria formosana. The differences among these compounds are the substituents and stereochemistry at C-13. Their structures were elucidated by 1D and 2D NMR experiments, and the absolute configurations of Scuteformoids A, C, E, F, and I were further confirmed by single-crystal X-ray diffraction. Scuteformoids A, C, D, F, H, and I were evaluated for their inhibitory effects against HIV lytic replication and cytotoxic activities. All of them showed weak anti-HIV activities, with EC50 values ranging from 48.24 to 79.17 µg/mL.


Assuntos
Fármacos Anti-HIV/farmacologia , Diterpenos Clerodânicos/farmacologia , HIV-1/efeitos dos fármacos , Scutellaria/química , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Linhagem Celular Tumoral , Diterpenos Clerodânicos/química , Diterpenos Clerodânicos/isolamento & purificação , Relação Dose-Resposta a Droga , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade , Replicação Viral/efeitos dos fármacos
16.
Phytochemistry ; 145: 40-47, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29080411

RESUMO

Six previously undescribed diterpenoids, named euphorantins S-T and euphorneroids A-D, including ingol and ent-atisane types, along with eleven known diterpenoids, were isolated from Euphorbia neriifolia. Their structures were elucidated on the basis of extensive NMR analysis and high resolution mass spectrometry. Euphorneroid D and ent-3-oxoatisan-16α,17-acetonide exhibited moderate anti-HIV-1 activities, with EC50 values of 34 µM (SI = 2.3) and 24 µM (SI = 1.9), respectively.


Assuntos
Fármacos Anti-HIV/farmacologia , Diterpenos/farmacologia , Euphorbia/química , HIV-1/efeitos dos fármacos , Casca de Planta/química , Caules de Planta/química , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Linhagem Celular , Diterpenos/química , Diterpenos/isolamento & purificação , Relação Dose-Resposta a Droga , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade
17.
Phytochemistry ; 146: 63-74, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29247893

RESUMO

Seven previously undescribed compounds, including three polycyclic polyprenylated acylphloroglucinols (garcinuntins A-C), three biphenyl derivatives (garcinuntabiphenyls A-C) and a lanostane triterpene (garcinuntine), along with thirteen known compounds were isolated from the root of Garcinia nuntasaenii Ngerns. & Suddee. Their structures were elucidated on the basis of spectroscopic techniques. For garcinuntins A-C, the absolute configurations were confirmed by the combination of single X-ray crystallography and ECD calculations. Anti-HIV activity using anti-HIV-1 reverse transcriptase and syncytium inhibition assays, and cytotoxic activity against a panel of cultured mammalian cancer cell lines of isolated compounds were investigated.


Assuntos
Fármacos Anti-HIV/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Compostos de Bifenilo/farmacologia , Garcinia/química , Transcriptase Reversa do HIV/antagonistas & inibidores , HIV-1/efeitos dos fármacos , Floroglucinol/farmacologia , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Compostos de Bifenilo/química , Compostos de Bifenilo/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Cristalografia por Raios X , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células HEK293 , Transcriptase Reversa do HIV/metabolismo , Humanos , Modelos Moleculares , Estrutura Molecular , Floroglucinol/análogos & derivados , Floroglucinol/isolamento & purificação , Raízes de Plantas/química , Relação Estrutura-Atividade
18.
Infect Disord Drug Targets ; 18(1): 15-22, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-28474549

RESUMO

AIDS (acquired immune deficient syndrome) is a deadly human viral infectious disease caused by HIV (human immune-deficient virus) infection. Almost every AIDS patient losses his/her life before mid 1990s. AIDS was once the 1st disease killer in US (1993). After one decade hard work, antiviral drug cocktails-high active anti-retroviral therapy (HAART) have been invented for almost all HIV infection treatments. Due to the invention of HAART, 80-90% HIV/AIDS patients still effectively response to HAART for deadly AIDS episode controls and life saving. Yet, this type of HIV therapeutics is incurable. HIV/AIDS patients need to take HAART medications regularly and even life-long. To counteract this therapeutic drawback, more revolutionary efforts (different angles of therapeutic modes/attempts) are urgently needed. In this article, the major progresses and drawbacks of HIV/AIDS chemotherapy (HAART) to HIV/AIDS patients have been discussed. Future trends (updating pathogenesis study, next generations of drug developments, new drug target discovery, different scientific disciplinary and so on) are highlighted.


Assuntos
Síndrome de Imunodeficiência Adquirida/tratamento farmacológico , Terapia Antirretroviral de Alta Atividade/tendências , Descoberta de Drogas/tendências , Infecções por HIV/tratamento farmacológico , Síndrome de Imunodeficiência Adquirida/virologia , Fármacos Anti-HIV/isolamento & purificação , Fármacos Anti-HIV/uso terapêutico , Terapia Antirretroviral de Alta Atividade/métodos , Química Farmacêutica/métodos , Reservatórios de Doenças/virologia , Sistemas de Liberação de Medicamentos , Feminino , Humanos , Masculino , Farmacogenética/métodos , Farmacogenética/tendências
19.
J Ethnopharmacol ; 210: 133-155, 2018 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-28807850

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The African continent is home to a large number of higher plant species used over centuries for many applications, which include treating and managing diseases such as HIV. Due to the overwhelming prevalence and incidence rates of HIV, especially in sub-Saharan Africa, it is necessary to develop new and affordable treatments. AIM OF THE STUDY: The article provides an extensive overview of the status on investigation of plants from the southern African region with ethnobotanical use for treating HIV or HIV-related symptoms, or the management of HIV. The review also provide an account of the in vitro assays, anti-viral activity and phytochemistry of these plants. MATERIALS AND METHODS: Peer-reviewed articles investigating plants with ethnobotanical information for the treatment or management of HIV or HIV-related symptoms from the southern African region were acquired from Science Direct, PubMed central and Google Scholar. The selection criteria was that (1) plants should have a record of traditional/popular use for infectious or viral diseases, HIV treatment or symptoms similar to HIV infection, (2) if not traditionally/popularly used, plants should be closely related to plants with popular use and HIV activity identified by means of in vitro assays, (3) plants should have been identified scientifically, (4) should be native to southern African region and (5) anti-HIV activity should be within acceptable ranges. RESULTS: Many plants in Africa and specifically the southern African region have been used for the treatment of HIV or HIV related symptoms and have been investigated suing various in vitro techniques. In vitro assays using HIV enzymes such as reverse transcriptase (RT), integrase (IN) and protease (PR), proteins or cell-based assays have been employed to validate the use of these plants with occasional indication of the selectivity index (SI) or therapeutic index (TI), with only one study, that progressed to in vivo testing. The compounds identified from plants from southern Africa is similar to compounds identified from other regions of the world, and the compounds have been divided into three groups namely (1) flavonoids and flavonoid glycosides, (2) terpenoids and terpenoid glycosides and (3) phenolic acids and their conjugated forms. CONCLUSIONS: An investigation of the plants from southern Africa with ethnobotanical use for the treatment of HIV, management of HIV or HIV-related symptoms, therefore provide a very good analysis of the major assays employed and the anti-viral compounds and compound groups identified. The similarity in identified anti-viral compounds worldwide should support the progression from in vitro studies to in vivo testing in development of affordable and effective anti-HIV agents for countries with high infection and mortality rates due to HIV/AIDS.


Assuntos
Fármacos Anti-HIV/farmacologia , Infecções por HIV/tratamento farmacológico , Extratos Vegetais/farmacologia , Animais , Fármacos Anti-HIV/isolamento & purificação , Etnobotânica , Humanos , Medicina Tradicional Africana/métodos , Fitoterapia/métodos , Extratos Vegetais/química , Plantas Medicinais/química
20.
J Nat Prod ; 80(10): 2595-2601, 2017 10 27.
Artigo em Inglês | MEDLINE | ID: mdl-29016131

RESUMO

Thirty-three metabolites including five phenalenone derivatives (1-5), seven cytochalasins (6-12), thirteen butenolides (13-25), and eight phenyl derivatives (26-33) were isolated from Aspergillus sp. CPCC 400735 cultured on rice. The structures of all compounds were elucidated by NMR, MS, and CD experiments, of which 1-5 (asperphenalenones A-E), 6 (aspochalasin R), and 13 (aspulvinone R) were identified as new compounds. Specifically, asperphenalenones A-E (1-5) represent an unusual structure composed of a linear diterpene derivative linked to a phenalenone derivative via a C-C bond. Compounds 1, 4, 10, and 26 exhibited anti-HIV activity with IC50 values of 4.5, 2.4, 9.2, and 6.6 µM, respectively (lamivudine 0.1 µM; efavirenz, 0.4 × 10-3 µM).


Assuntos
4-Butirolactona/análogos & derivados , Fármacos Anti-HIV/isolamento & purificação , Fármacos Anti-HIV/farmacologia , Aspergillus/química , Citocalasinas/isolamento & purificação , Citocalasinas/farmacologia , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Fenalenos/isolamento & purificação , Fenalenos/farmacologia , 4-Butirolactona/química , 4-Butirolactona/isolamento & purificação , 4-Butirolactona/farmacologia , Fármacos Anti-HIV/química , China , Citocalasinas/química , Diterpenos/química , Endófitos/química , Concentração Inibidora 50 , Kadsura/microbiologia , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Fenalenos/química
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA