ABSTRACT
Metabolomic profiles were explored to understand environmental and taxonomic influences on the metabolism of two congeneric zoanthids, Palythoa caribaeorum and P. variabilis, collected across distinct geographical ranges. Integrated mass spectrometry data suggested the major influence of geographical location on chemical divergence when compared to species differentiation.
Subject(s)
Anthozoa/chemistry , Anthozoa/metabolism , Metabolomics , Animals , Brazil , Geography , Mass Spectrometry , Molecular Structure , Species SpecificityABSTRACT
The use of natural products in therapeutics has been growing over the years. Lignans are compounds with large pharmaceutical use, which has aroused interest in the search for new drugs to treat diseases. The present study evaluated the cytotoxicity of (-)-trachelogenin, a dibenzylbutyrolactone type lignan isolated from Combretum fruticosum, against several tumor and non-tumor cell lines using the MTT assay and its possible mechanism of action. (-)-Trachelogenin showed IC50 values ranging of 0.8-32.4µM in SF-295 and HL-60 cell lines, respectively and IC50 values >64µM in non-tumor cell lines. (-)-trachelogenin persistently induced autophagic cell death, with cytoplasmic vacuolization and formation of autophagosomes mediated by increasing LC3 activation and altering the expression levels of Beclin-1.
Subject(s)
4-Butyrolactone/analogs & derivatives , Antineoplastic Agents, Phytogenic/pharmacology , Autophagy/drug effects , Colonic Neoplasms/drug therapy , Combretum/chemistry , Drug Discovery , Plant Stems/chemistry , 4-Butyrolactone/adverse effects , 4-Butyrolactone/chemistry , 4-Butyrolactone/isolation & purification , 4-Butyrolactone/pharmacology , Antineoplastic Agents, Phytogenic/adverse effects , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Autophagosomes/drug effects , Autophagosomes/pathology , Beclin-1/agonists , Beclin-1/metabolism , Brazil , Cell Line , Cell Line, Tumor , Cell Survival/drug effects , Colonic Neoplasms/pathology , Combretum/growth & development , Ethnopharmacology , HCT116 Cells , Humans , Inhibitory Concentration 50 , Medicine, Traditional , Microtubule-Associated Proteins/agonists , Microtubule-Associated Proteins/metabolism , Molecular Structure , Neoplasm Proteins/agonists , Neoplasm Proteins/metabolism , Plant Stems/growth & development , Vacuoles/drug effects , Vacuoles/pathologyABSTRACT
The anti-inflammatory effect of physalin E, a seco-steroid isolated from Physalis angulata L. was evaluated on acute and chronic models of dermatitis induced by 12-O-tetradecanoyl-phorbol-13-acetate (TPA) and oxazolone, respectively, in mouse ear. The changes in ear edema/thickness, production of pro-inflammatory cytokines (TNF-alpha and IFN-gamma), myeloperoxidase (MPO) activity, and histological and immunohistochemical findings were analysed, as indicators of dermal inflammation. Similar to dexamethasone, topically applied Physalin E (0.125; 0.25 and 0.5 mg/ear) potently inhibited the TPA and oxazolone-induced dermatitis, leading to substantial reductions in ear edema/thickness, pro-inflammatory cytokines, and MPO activity. These effects were reversed by mifepristone, a steroid antagonist and confirmed by immunohistochemical and histopathological analysis. The data suggest that physalin E may be a potent and topically effective anti-inflammatory agent useful to treat the acute and chronic skin inflammatory conditions.
Subject(s)
Anti-Inflammatory Agents/therapeutic use , Dermatitis, Contact/drug therapy , Physalis/chemistry , Secosteroids/therapeutic use , Animals , Immunohistochemistry , Male , Mice , Oxazolone/toxicity , Tetradecanoylphorbol Acetate/toxicityABSTRACT
BACKGROUND AND PURPOSE: Oncocalyxone A (OncoA) has a concentration-dependent anti-platelet activity. The present study aimed to further understand the mechanisms related to this effect. EXPERIMENTAL APPROACH: Human platelet aggregation was measured by means of a turbidimetric method. OncoA (32-256 microM) was tested against several platelet-aggregating agents, such as adenosine diphosphate (ADP), collagen, arachidonic acid (AA), ristocetin and thrombin. KEY RESULTS: OncoA completely inhibited platelet aggregation with a calculated mean inhibitory concentration (IC50-microM) of 122 for ADP, 161 for collagen, 159 for AA, 169 for ristocetin and 85 for thrombin. The anti-aggregatory activity of OncoA was not inhibited by 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ). OncoA, at a concentration that caused no significant anti-aggregatory activity, potentiated sodium nitroprusside (SNP) anti-aggregatory activity (18.8+/-2.9%-SNP vs 85.0+/-8.2%-SNP+OncoA). The levels of nitric oxide (NO) or cAMP were not altered by OncoA while cGMP levels were increased more than 10-fold by OncoA in resting or ADP-activated platelets. Flow cytometry revealed that OncoA does not interact with receptors for fibrinogen, collagen or P-selectin. Nevertheless, OncoA decreased the binding of antibodies to GP Ibalpha, a glycoprotein that is related both to von Willebrand factor and to thrombin-induced platelet aggregation. CONCLUSION AND IMPLICATIONS: OncoA showed anti-aggregatory activity in platelets that was associated with increased cGMP levels, not dependent on NO and with blocking GP Ibalpha glycoprotein. This new mechanism has the prospect of leading to new anti-thrombotic drugs.
Subject(s)
Anthraquinones/pharmacology , Cyclic AMP/biosynthesis , Platelet Aggregation Inhibitors/pharmacology , Platelet Aggregation/drug effects , Platelet Glycoprotein GPIb-IX Complex/metabolism , Adenosine Diphosphate/pharmacology , Adenosine Triphosphate/metabolism , Adolescent , Adult , Anthraquinones/isolation & purification , Anthraquinones/metabolism , Blood Platelets/drug effects , Blood Platelets/metabolism , Cyclic AMP/blood , Cyclic GMP/blood , Cyclic Nucleotide Phosphodiesterases, Type 5/blood , Cyclic Nucleotide Phosphodiesterases, Type 5/metabolism , Female , Flow Cytometry , Guanylate Cyclase/blood , Guanylate Cyclase/metabolism , Humans , In Vitro Techniques , Male , Middle Aged , Nitric Oxide/metabolism , Platelet Aggregation Inhibitors/metabolism , Protein Binding , Thromboxane A2/physiologyABSTRACT
The essential oil of fresh leaves of Lippia aff. gracillis was analyzed by GC/MS and evaluated for its antibacterial effects. The results showed a moderate antibacterial activity and confirm the traditional uses of L. aff. gracillis.
Subject(s)
Anti-Bacterial Agents/pharmacology , Lippia/chemistry , Oils, Volatile/pharmacology , Escherichia coli/drug effects , Microbial Sensitivity Tests , Oils, Volatile/analysis , Plant Leaves/chemistry , Staphylococcus aureus/drug effectsABSTRACT
A atividade larvicida de quatro saponinas monodesmosídicas (1-4) isoladas de Pentaclethra macroloba e de uma saponina bidesmosídica (5) isolada de Cordia piauhiensis foi avaliada sobre larvas de estágio 3 de Aedes aegypti. As larvas foram expostas a várias concentrações (500, 250, 100, 50, 25 e 12,5 mg/mL) das saponinas por um período de 24 h. Os resultados indicam que somente as saponinas 1-3 mostraram alta atividade larvicida, com CL50 variando de 18,6 a 27,9 mg/mL. Estes resultados ressaltam as potencialidades destas saponinas como possíveis agentes larvicidas naturais.
The larvicidal activity of the four monodesmoside saponins (1-4) isolated from Pentaclethra macroloba and one bidesmoside saponin (5) from Cordia piauhiensis was evaluated on 3rd instar larvae of Aedes aegypti. The larvae were exposed to serial concentrations (500, 250, 100, 50, 25 and 12.5 mg/mL) saponins for a period of 24 h. The results indicate that, only the saponins 1-3 showed high larvicidal activity, with LC50 ranging of 18,6-27,9 mg/mL. These results suggest that these can be used as natural larvicidal agents.
ABSTRACT
No período de janeiro à dezembro de 2003 foram enviados ao Laboratório Central do estado do Ceará ( LACEN-Ce), 1.028 espécimes clínicos (urina), coletados de 112 pacientes com suspeita de tuberculose urogenital, onde 79 (7,7) destes espécimes apresentaram baciloscopia e cultura positiva para o complexo Mycobacterium tuberculosis. Dos 112 pacientes apenas 40 (35,7)...
Subject(s)
Male , Female , Humans , Tuberculosis, Urogenital , Clinical Laboratory Techniques , Mycobacterium tuberculosisABSTRACT
The present study evaluated the cytotoxic activity of nepetin and quercetin-3-O-glucoside, compounds isolated from the aerial parts of Eupatorium ballotaefolium. The antimitotic activity was determined as the ability to inhibit sea urchin eggs development and five tumor cells lines growth. Moreover, the activities of these compounds were compared to quercetin in the same models. Nepetin inhibited the proliferation of the five tumor cell lines, once quercetin-3-O-glucoside did not present any activity even at the highest tested concentration and quercetin only inhibited proliferation of the B16 cell line. On the sea urchin assay, nepetin and quercetin induced a dose-dependent inhibition on egg development, while quercetin-3-O-glucoside did not modify normalegg cleavage, even at the highest tested concentration (100 microg/ml).
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Eupatorium/chemistry , Flavonoids/pharmacology , Quercetin/analogs & derivatives , Quercetin/pharmacology , Animals , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cell Survival/drug effects , Drug Screening Assays, Antitumor , Flavones , Humans , Sea UrchinsABSTRACT
Auxemma oncocalyx Taub. belongs to the Boraginaceae family and is native to the Brazilian northeast where it is known as "pau-branco". We investigated the ability of the water soluble fraction isolated from the heartwood of A. oncocalyx to inhibit sea urchin egg development. This fraction contains about 80% oncocalyxone A (quinone fraction), a compound known to possess strong cytotoxic and antitumor activities. In fact, the quinone fraction inhibited cleavage in a dose-dependent manner [IC50 of 18.4 (12.4-27.2) microg/ml, N = 6], and destroyed the embryos in the blastula stage [IC50 of 16.2 (13.7-19.2) microg/ml, N = 6]. We suggest that this activity is due to the presence of oncocalyxone A. In fact, these quinones present in A. oncocalyx extract have strong toxicity related to their antimitotic activity.
Subject(s)
Anthraquinones/toxicity , Boraginaceae/chemistry , Ovum/drug effects , Quinones/toxicity , Animals , Anthraquinones/isolation & purification , Antineoplastic Agents/toxicity , DNA Damage , Plant Extracts/toxicity , Quinones/isolation & purification , Sea UrchinsABSTRACT
Auxemma oncocalyx Taub. belongs to the Boraginaceae family and is native to the Brazilian northeast where it is known as "pau-branco". We investigated the ability of the water soluble fraction isolated from the heartwood of A. oncocalyx to inhibit sea urchin egg development. This fraction contains about 80 percent oncocalyxone A (quinone fraction), a compound known to possess strong cytotoxic and antitumor activities. In fact, the quinone fraction inhibited cleavage in a dose-dependent manner [IC50 of 18.4 (12.4-27.2) æg/ml, N = 6], and destroyed the embryos in the blastula stage [IC50 of 16.2 (13.7-19.2) æg/ml, N = 6]. We suggest that this activity is due to the presence of oncocalyxone A. In fact, these quinones present in A. oncocalyx extract have strong toxicity related to their antimitotic activity
