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1.
Fitoterapia ; : 104800, 2020 Dec 08.
Artigo em Inglês | MEDLINE | ID: mdl-33307175

RESUMO

This report illustrated isolation and identification of 42 compounds comprising five (spicatainoids A-E) undescribed eremophilanolide type sesquiterpenoids and one undescribed nor-eremophilane (spicatainoid F) from Ligularia subspicata.. Among all the isolated new compounds, 4 is reported as the first enantiomeric form of novel eremophilanolide type sesquiterpenoid. Comprehensive analysis of HRESIMS, 1D/2D NMR, experimental circular dichroism (CD), calculated ECD analysis, and X-ray crystallographic (XRD) analysis validated the complete configuration and confirmation of these isolated compounds. All the isolated compounds were tested for the anti-inflammatory potential by measuring the amount of nitric oxide production. Among the tested compounds, 4 was the most effective with 90% NO-inhibition activity. Compounds 1, 2, 3, 9, 10 18, 29, 34, 35 exhibited moderate inhibitory effects against the production of NO, while other compounds displayed no activity even at the concentration of 50 µM. Additionally, compounds 1, 3 and 4 presented moderate anti-inflammatory activity by inhibiting the release of pro-inflammatory cytokines (TNF-α, IL-1ß, and IL-6) in LPS-stimulated N9 cells. The IC50 values of compounds 1, 3 and 4 were calculated 39.6 ±â€¯2.7, 42.5 ±â€¯3.8 and 27.60 ±â€¯1.9 µΜ.

2.
J Ophthalmol ; 2020: 3949735, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33133675

RESUMO

Purpose: To determine the effectiveness and safety of trabeculectomy along with amniotic membrane transplantation (AMT) for glaucoma. Methods: This systematic review was performed using RevMan 5.3. We searched PubMed, EMBASE, and the Cochrane Library and included studies published until September 2019. The treatment group included patients with AMT and trabeculectomy (group A), and the control group had only trabeculectomy (group B). We only included randomized controlled trials. The outcomes were intraocular pressure (IOP), complete success rate, number of antiglaucoma medications, and complications. Results: Five studies, including 174 eyes (87 eyes in the AMT group and 87 eyes in the control group), were eligible in this review. The parameters had no significant difference in heterogeneity between the AMT and control groups preoperatively. In the AMT group, the mean IOP was significantly lower at 3 and 12 months after operation (P < 0.0001 and P = 0.02, respectively), while the number of complete successes in the AMT group was significantly higher at 6 and 12 months (P = 0.02 and P = 0.003, respectively) compared with the control group. Complications, including a flat anterior chamber and hyphema, appeared to be decreased in the AMT group compared to the control group (P = 0.02 and P = 0.02, respectively). No differences were observed in the number of antiglaucoma medications, hypotony, encapsulated bleb, or choroidal detachment. Conclusion: Compared with only trabeculectomy, it is more efficient and safer to add AMT to trabeculectomy during glaucoma filtering surgery.

3.
Phytomedicine ; 79: 153330, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32932202

RESUMO

BACKGROUND: Compound Dan Zhi tablet (DZT) is a commonly used traditional Chinese medicine formula. It has been used for the treatment of ischemic stroke for many years in clinical. However, its pharmacological mechanism is unclear. PURPOSE: The aim of the current study was to understand the protective effects and underlying mechanisms of DZT on ischemic stroke. METHODS: Fifteen representative chemical markers in DZT were determined by ultra-performance liquid chromatography coupled with tandem quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS). The protective effect of DZT against ischemic stroke was studied in a rat model of middle cerebral artery occlusion (MCAO), and the mechanism was further explored through a combination of network pharmacology and experimental verification. RESULTS: Quantitative analysis showed that the contents of phenolic acids, furan sulfonic acids, tanshinones, flavonoids, saponins and phthalides in DZT were calculated as 7.47, 0.788, 0.627, 0.531 and 0.256 mg/g, respectively. Phenolic acids were the most abundant constituents. Orally administered DZT (1.701 g kg-1) significantly alleviated the infarct size and neurological scores in MCAO rats. The network analysis predicted that 53 absorbed active compounds in DZT-treated plasma targeted 189 proteins and 47 pathways. Ten pathways were associated with anti-platelet activity. In further experiments, DZT (0.4 and 0.8 mg mL-1) markedly inhibited in vitro prostaglandin G/H synthase 1 (PTGS1) activity. DZT (0.4 and 0.8 mg mL-1) significantly inhibited in vitro platelet aggregation in response to ADP or AA. DZT (113 and 226 mg kg-1, p.o.) also produced a marked inhibition of ADP- or AA-induced ex vivo platelet aggregation with a short duration of action. DZT decreased the level of thromboxane A2 (TXA2) in MCAO rats. In the carrageenan-induced tail thrombosis model and ADP-induced acute pulmonary thromboembolism mice model, DZT (113 and 226 mg kg-1, p.o.) prevented thrombus formation. Importantly, DZT (113 and 226 mg kg-1, p.o.) exhibited a low bleeding liability. CONCLUSION: DZT protected against cerebral ischemic injury. The inhibition of TXA2 level, platelet aggregation and thrombosis formation might involve in the protective mechanism.

4.
J Biomol Struct Dyn ; : 1-15, 2020 Sep 02.
Artigo em Inglês | MEDLINE | ID: mdl-32876526

RESUMO

Natural products of herbal origin are prodigious to display diverse pharmacological activities. In the present study, five guaiane-type sesquiterpene dimers, xylopidimers A - E (1-5), isolated from Xylopia vielana species were tested against COX-2 protein target (PDB: 1CX2), a potent target for anti-inflammatory agents. To better understand the pharmacological properties of all these compounds, in this work, a systemic in silico study was performed on xylopidimers A-E using molecular docking, ADMET analysis and MD simulations. During ADMET predictions the two compounds xylopidimer C, D displayed best results as compared to others. The compound xylopidimer C was further evaluated for its MD simulations and its molecular interactions with COX2 complex showed clear interactions with active gorge of the enzyme through hydrogen bonding as well as hydrophobic contacts. The xylopidimer C has shown the best binding potential with -10.57Kcal/mol energy with 17.92 nano molar of predicted inhibition constant better than Ibuprofen and Felbinac. These findings provide enough significant information for designing and developing novel targeted base anti-inflammatory drugs from guaiane dimers.

5.
Curr Pharm Des ; 2020 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-32723250

RESUMO

Marine fungi with their successful pharmacological effects were considered to be the treasure of ocean medicines concerning the striking ability of their secondary metabolites. Literature over literature has been published on fungi derived bioactive molecules to probe its therapeutic potential. Marine fungi have an implicit to cede future medicines against life-threatening diseases, such as cancer and several emerging inflammations. The biological actions of many marine fungi-derived secondary metabolites are still unlocked, for an assorted number of bioactive compounds by which they interact with human diseases are discussed here with comprehensive diagrams. This knowledge is one of the main track to be established specifically for the successful transformation of bioactive compounds to medicines. Marine fungi produce a diverse range of biochemical substances with precious carbon scaffolds, which are the main component interplaying with human diseases at distinctive spots. Specific diseases having a flair to fight at distinctive targets within the body can lead to a new trend of raising the chances of developing targeted drugs.

6.
J Pharm Biomed Anal ; 184: 113197, 2020 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-32120187

RESUMO

Untargeted mass spectrometry analysis is one of the most challenging and meaningful steps in the rapid structural elucidation of the highly complex and diverse constituents of traditional Chinese medicine. Specifically, it is a laborious and time-consuming way to identify unknown compounds. Herein, a workflow was proposed to expedite the annotations of the chemical structures in Pheretima aspergillum (E. Perrier) (Di-Long, DL). First, ultra high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-QTOFMS) was performed to obtain the untargeted mass spectral data. Then, the spectral data were uploaded to the Global Natural Products Social Molecular Networking (GNPS) platform to create a network and extract the Mass2Motifs (co-occurring fragments and neutral losses) using unsupervised substructure annotation topic modeling (MS2LDA). Finally, a structural analysis was performed using the proposed workflow of MS2LDA in combination with mass spectral molecular networking and in silico fragmentation prediction. As a result, a total of 124 compounds from DL were effectively characterized, of which 89 (7 furan sulfonic acids, 57 phospholipids and 25 carboxamides) were identified as potentially new compounds from DL. The results presented in this article significantly improve the understanding of the chemical composition of DL and provide a solid scientific basis for the future study of the quality control, underlying pharmacology and mechanism of DL. Moreover, the proposed workflow was used for the first time to accelerate the annotations of unknown molecules from TCM. Furthermore, this workflow will increase the efficiency of characterizing the 'unknown knowns' and elucidation of the 'unknown unknowns' from TCM, which are crucial steps of discovering the natural product drugs in TCM.

7.
Nat Prod Res ; : 1-14, 2020 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-33929917

RESUMO

Three undescribed guaiane-type sesquiterpenes (1-3), and a monoterpenoid (4) along with eleven known compounds (5 - 15) were isolated from the crude extract of Litsea lancilimba Merr. The structures of all the isolated compounds were extensively elucidated on the basis of comprehensive spectroscopic techniques (HRESIMS, 1 D NMR, and 2 D NMR). Their relative and absolute configurations were comprehensively established by NOESY spectroscopy, circular dichroism (ECD) and the calculated ECD analysis. All the isolates were tested for anti-inflammatory activity by measuring the amount of nitric oxide production. Amongst tested compounds, compounds 1 - 3 exhibited moderate inhibitory activities against the production of nitric oxide with IC50 value of 35.5, 32.1, 46.7 µM in RAW264.7 cells stimulated by LPS, respectively.

8.
ACS Omega ; 4(1): 2047-2052, 2019 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-31459455

RESUMO

Five new guaiane dimers, xylopidimers A-E (1-5), were isolated and identified from the roots of Xylopia vielana. The structures of 1-5 were elucidated by spectroscopic analysis and further confirmed by single-crystal X-ray diffraction. On the basis of the results of single-crystal X-ray analysis, 1-5 showed different carbon skeletons. Among these compounds, the unique connecting patterns of 1 and 2 caused significant differences on their carbon skeletons, which have not been reported. Moreover, 3-5 were also three new guaiane dimers. Among these compounds, 4 exhibited potent inhibitory activity against the production of nitric oxide with an IC50 value of 4.59 µM in RAW264.7 cells stimulated by lipopolysaccharide.

9.
Biomed Pharmacother ; 109: 459-467, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30399582

RESUMO

Elicitation by chemical means including heavy metals is one of a novel technique for drug discoveries. In this review, the effect of heavy metals on animal, plants and microorganisms for the production of novel compounds with the unique structures has been discussed. The number of parameters such as metal concentration, type, dose, treatment schedule, duration of metal exposure, and nutrient composition are significant factors altering the secondary metabolites production. The detailed illustrated diagram representing the mode of action of metal stress has also been discussed. This is the first article reporting all the novel compounds produced from plants and microorganisms in response to metal-stress with their pharmacological potential. This new technique opens the new way for drug discovery from natural products.


Assuntos
Produtos Biológicos/uso terapêutico , Descoberta de Drogas/tendências , Exposição Ambiental/prevenção & controle , Metais Pesados/toxicidade , Estresse Oxidativo/efeitos dos fármacos , Animais , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Descoberta de Drogas/métodos , Exposição Ambiental/análise , Humanos , Estresse Oxidativo/fisiologia , Plantas Medicinais
10.
Org Biomol Chem ; 16(37): 8408-8412, 2018 09 26.
Artigo em Inglês | MEDLINE | ID: mdl-30221279

RESUMO

Four unprecedented guaiane dimers, xylopsides A-D (1-4), were isolated and identified from the roots of Xylopia vielana. The structures of 1-4 were elucidated by spectroscopic analysis, Cu Kα X-ray crystallography and CD spectra. 1-4 showed two bridged pentacyclic skeletons between two guaiane-type sesquiterpenes, which were characterized as two different bridged ring systems. Among these compounds, 4 exhibited a moderate inhibitory activity against the production of nitric oxide with an IC50 value of 25.7 µM in RAW264.7 cells stimulated by LPS.


Assuntos
Dimerização , Sesquiterpenos de Guaiano/química , Sesquiterpenos de Guaiano/farmacologia , Xylopia/química , Animais , Camundongos , Modelos Moleculares , Conformação Molecular , Óxido Nítrico/biossíntese , Raízes de Plantas/química , Células RAW 264.7
11.
Fitoterapia ; 130: 43-47, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30076886

RESUMO

Five new guaiane-type sesquiterpenoid dimers vielopsides A-E, connecting patterns through two direct CC bonds (C-2 to C-2', C-4 to C-1'), were isolated from the roots of Xylopia vielana. Their absolute configurations were established by NOE analysis, the Cu Kα X-ray crystallographic and circular dichroism (CD) experiment. Among them, compound 5 showed moderate activity IC50 values of 33.8 µM on NO production in RAW 264.7 macrophages.


Assuntos
Compostos Fitoquímicos/isolamento & purificação , Sesquiterpenos/isolamento & purificação , Xylopia/química , Animais , China , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Compostos Fitoquímicos/farmacologia , Raízes de Plantas/química , Células RAW 264.7 , Sesquiterpenos/farmacologia
12.
Fitoterapia ; 127: 96-100, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29421243

RESUMO

Three new aporphine alkaloids, xylopialoids A-C (1-3), along with three known aporphine alkioids (4-6) and three other known compounds (7-9) were isolated from the roots of Xylopia vielana. Among these three new aporphine alkaloids, xylopialoid C (3) showed a special carbamido group directly connected to the nitrogen. The chemical structures of these nine compounds were determined by a combination of 1D and 2D NMR, MS, CD spectrum and Cu Kα X-ray crystallographic analyses. All these six alkaloids were firstly tested for the inhibitory activities against the production of NO in RAW264.7 cells stimulated by lipopolysaccharide (LPS). Among these compounds, 4 showed a potential inhibitory activity against the production of nitric oxide with IC50 value of 1.39 µM.


Assuntos
Alcaloides/isolamento & purificação , Anti-Inflamatórios/isolamento & purificação , Raízes de Plantas/química , Xylopia/química , Alcaloides/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Células RAW 264.7
13.
Fitoterapia ; 125: 18-23, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29242037

RESUMO

One unusual metal complex of cadinane sesquiterpene alkaloid (1), one new cadinane sesquiterpene alkaloid (2) and two new neolignan glycosides (3-4) along with six known cadinane sesquiterpene derivatives (5-10), nineteen known phenolic glycosides (11-29) were isolated from the aerial parts of Alangium alpinum. Structures of new crystals of metal complex were characterized by X-Ray diffraction and ICP-AES analysis. Other new compounds were elucidated by combined use and detailed analysis of HR-ESIMS, 1D and 2D NMR and CD spectroscopic method. In addition, all isolated compounds were tested for their inhibitory effects against TNF-α induced NF-κB activation in Hela cells and NO production in RAW 264.7 macrophages.


Assuntos
Alangiaceae/química , Alcaloides/isolamento & purificação , Glicosídeos/isolamento & purificação , Lignanas/isolamento & purificação , Sesquiterpenos/isolamento & purificação , Alcaloides/química , Animais , Células HeLa , Humanos , Metais/química , Camundongos , Estrutura Molecular , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Componentes Aéreos da Planta/química , Sesquiterpenos Policíclicos , Células RAW 264.7 , Sesquiterpenos/química , Fator de Necrose Tumoral alfa/metabolismo
14.
Fitoterapia ; 121: 152-158, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28733150

RESUMO

Seven new lignan glycosides (1-3, 8-10, and 14) and 17 known compounds were isolated from the branches of Alangium kurzii Craib var. laxifolium. Their structures were established by spectroscopic analysis and circular dichroism (CD) and X-ray analysis. The isolated compounds were evaluated for their antibacterial activities against Staphylococcus aureus CI1011, Streptococcus suis CI1608, Salmonella gallinarum CI0912, Enterococcus faecalis CI1304, Aeromonas hydrophila CI1008, Escherichia coli CI151012, Vibrio parahaemolyticus CI150506, Klebsiella pneumoniae CI131216, Pseudomonas aeruginosa CI1011, Staphylococcus epidermidis CI1110, and Streptococcus agalactiae CI1302. Their minimum inhibitory concentrations (MICs) were determined by serial dilution in 96-well culture plates.


Assuntos
Alangiaceae/química , Antibacterianos/química , Glicosídeos/química , Lignanas/química , Antibacterianos/isolamento & purificação , Glicosídeos/isolamento & purificação , Lignanas/isolamento & purificação , Testes de Sensibilidade Microbiana , Estrutura Molecular , Extratos Vegetais/química
15.
Artigo em Inglês | MEDLINE | ID: mdl-28473862

RESUMO

In a continuing effort to discover more anti-inflammatory medicinal plants in China, the anti-inflammatory activities of 101 extracts from different parts of 84 traditional medicinal plants were evaluated by a panel of in vitro and in vivo assays. Nuclear factor-kappa B (NF-κB) inhibitory effects were determined by luciferase assay in stably transfected Hela cells. Cytotoxic activities were assessed using the MTT assay. Inhibitory effects on LPS-induced nitric oxide production and proinflammatory mediators were assessed by Griess reaction and Real-Time PCR analysis, respectively. In vivo anti-inflammatory activities were examined by xylene-induced mice ear edema model. In total, 22 extracts showed promising NF-κB inhibitory effects whereas 9 of them did not affect the cell viability. The 9 hit extracts were active in at least one of the subsequently performed in vitro pharmacological test systems. The extract from Hemerocallis minor (root) was selected to perform the in vivo study because it demonstrated significant suppressive effects in all the in vitro assays. Results showed that the extract of Hemerocallis minor (Root) was able to alleviate ear edema effectively in xylene-induced mice ear edema mode. Collectively, our study provides evidence for the potential anti-inflammatory effects of the medicinal plants traditionally used in China. Further phytochemical and pharmacological studies remain to be clarified.

16.
Fitoterapia ; 118: 80-86, 2017 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-28285947

RESUMO

Eight new γ-lactam alkaloids, hemerominors A-H (1-8), including two pair of epimers (1-4), together with six known compounds (9-14) were isolated from the roots of Hemerocallis minor Mill. The structures of 1-8 were established on the basis of extensive NMR studies and HR-MS measurements as well as comparison with literature data. The absolute configurations of 1-8 were determined by CD spectral analysis and modified Mosher's method. All of compounds were evaluated for their inhibitory effects against LPS-induced NO production in RAW264.7 macrophages. Among them, compound 13 exhibited moderate inhibitory activity against NO production and with IC50 value of 18.0 µM.


Assuntos
Alcaloides/química , Hemerocallis/química , Lactamas/química , Alcaloides/isolamento & purificação , Animais , Lactamas/isolamento & purificação , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Óxido Nítrico , Raízes de Plantas/química , Células RAW 264.7
17.
Fitoterapia ; 113: 91-6, 2016 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27431772

RESUMO

Phytochemical investigation of Abies faxoniana Rehd. led to the isolation of two pairs of new epimeric spirolactone-type triterpenoids (1/1' and 2/2') and 11 known terpenoids (3-13). Compounds 1/1' and 2/2' were isolated as epimeric mixtures due to the C-23 ketal tautomerism in their spirolactone structures. The dynamic HPLC manifested that the C-23 epimeric mixtures interconverted into each other in solution. Structure determinations were based on extensive NMR and HRESIMS spectroscopic analysis. Meanwhile, their cytotoxic activities were tested by MTT method. Compound 5 showed cytotoxicities against MCF-7 and A549 cells with IC50 values of 6.5 and 5.7µM, respectively. Compounds 1/1' had IC50 values of 10.0 and 12.3µM for Huh7 and SMMC7721 cells, respectively.


Assuntos
Abies/química , Antineoplásicos Fitogênicos/química , Espironolactona/química , Triterpenos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Humanos , Estrutura Molecular , Componentes Aéreos da Planta/química , Espironolactona/isolamento & purificação , Triterpenos/isolamento & purificação
18.
Planta Med ; 82(8): 734-41, 2016 May.
Artigo em Inglês | MEDLINE | ID: mdl-27220079

RESUMO

A phytochemical investigation on the roots of Campylotropis hirtella afforded nine new isoflavones (3-9, 12, 15), two new isoflavans (10 and 11), one new coumestan (1), and three new prenylated benzoic acid derivatives (2, 13, 14), together with twenty-four known compounds. Their structures were established by spectroscopic analysis and circular dichroism data. The isolated compounds were also evaluated for their antibacterial activities against Enterococcus faecalis, Salmonella gallinarum, Streptococcus suis, Streptococcus agalactiae, Aeromonas hydrophila, Pseudomonas aeruginosa, Bacillus subtilis, Riemerella anatipestifer, and Vibrio alginolyticus.


Assuntos
Antibacterianos/isolamento & purificação , Fabaceae/química , Extratos Vegetais/isolamento & purificação , Antibacterianos/química , Antibacterianos/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química
19.
Yao Xue Xue Bao ; 51(6): 843-52, 2016 06.
Artigo em Chinês | MEDLINE | ID: mdl-29878736

RESUMO

The international cooperated research projects of the Human Microbiome Project (HMP) and Metagenomics of The Human Intestinal Tract (MetaHIT) were officially launched in 2007, which indicated the era of metagenomics research of microorganisms in human gastrointestinal tract had been coming. Each human body is a superorganism which is composed of 90% commensal microorganisms, especially the intestinal microorganisms. The intestinal microorganisms play an important role on health maintenance since they are involved in the absorption and metabolism of nutrients in the human bodies. Herein, we review the research progress in the mechanism of intestinal microorganisms in human diseases. Our purpose is to provide novel ideas on human health and therapeutic targets of diseases.


Assuntos
Microbioma Gastrointestinal , Intestinos/microbiologia , Metagenômica , Humanos , Simbiose
20.
J Asian Nat Prod Res ; 18(2): 200-5, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26243444

RESUMO

A new phenyldilactone, maysedilactone B (1), together with twenty known compounds, were isolated from the aerial parts of Lespedeza cuneata. The structural elucidation of the isolated compounds was primarily based on HR-ESI-MS, IR and 1D and 2D NMR analyses. Compounds 1-8 and 15-21 were tested for cytotoxicity against four human tumor cell lines (A549, HCT116, SKOV3, and HepG2) using MTT method in vitro, while no significant activities were observed for the evaluated compounds.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Lactonas/isolamento & purificação , Lactonas/farmacologia , Lespedeza/química , Antineoplásicos Fitogênicos/química , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Células HCT116 , Células Hep G2 , Humanos , Lactonas/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Componentes Aéreos da Planta/química
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