ABSTRACT
Two novel dissymmetric diterpenoids, biselisabethoxanes A and B (1 and 2), were isolated from the hexane extracts of the gorgonian coral Pseudopterogorgia elisabethae. Biselisabethoxane A (1) represents the first example of a marine-derived C40 dimer made of two distinct diterpene fragments, whereas biselisabethoxane B (2) is a fused heterodimer stemming from coupling of two amphilectane-based fragments. The structures of 1 and 2 were elucidated based on 1D and 2D NMR spectral data analysis. The molecular structure of 1 was subsequently confirmed by X-ray crystallographic analysis. When evaluated for their inhibitory effects in a series of well-established biological activity assays the isolated compounds were shown to moderately inhibit the growth of Mycobacterium tuberculosis.
Subject(s)
Anthozoa , Diterpenes , Mycobacterium tuberculosis , Animals , Anthozoa/chemistry , Diterpenes/chemistry , Caribbean Region , Molecular StructureABSTRACT
OBJETIVO: Analizar si un programa de ejercicio físico (EF) modifica la hemoglobina glucosilada (HbA1c), la presión arterial (PA), el índice de masa corporal (IMC), la lipidemia, el riesgo cardiovascular (RCV), el estado de salud autopercibido (ESA) y el gasto farmacéutico (GF). DISEÑO: Ensayo clínico aleatorizado controlado, simple ciego. Intervención: programa de EF aeróbico supervisado. Análisis por intención de tratar. Emplazamiento: Atención primaria: 2 zonas de salud rurales. Área Salud Navalmoral, Cáceres, Servicio Extremeño de Salud. PARTICIPANTES: Cien diabéticos tipo 2, de 65-80 años, sedentarios; 50% grupo control (GC), 50% grupo intervención (GI). Abandonos: 12%. Intervención: EF aeróbico supervisado: 50 min, 2 días/semana, 3 meses. MEDICIONES PRINCIPALES: : HbA1c, PA, IMC, lipidemia, RCV, ESA, GF, complicaciones durante EF. RESULTADOS: Diferencias postintervención entre grupos en HbA1c, PA, IMC, colesterol y ESA. En GI disminución de HbA1c: 0,2 ± 0,4% (IC del 95%, 0,1 a 0,3); PA sistólica: 8,5 ± 11,8 mmHg (IC del 95%, 5,1 a 11,9); IMC: 0,5 ± 1 (IC del 95%, 0,2 a 0,8); colesterol: 14 ± 28,2 mg/dl (IC del 95%, 5,9 a 22,2); LDL: 18,3 ± 28,2 mg/dl (IC del 95%, 10,2 a 26,3), RCV: 6,7 ± 7,7% (IC del 95%, 4,5 a 8,9), GF: 3,9 ± 10,2 Euros (IC del 95%, 0,9 a 6,8) y aumento del ESA: 4,7 ± 5,7 (IC del 95%, 3 a 6,3). CONCLUSIONES: En diabéticos mayores de 65 años un programa de EF aeróbico supervisado de fácil ejecución mejora la HbA1c, la PA, la colesterolemia, el RCV, el GF y el ESA
OBJECTIVE: To analyze whether an exercise program can modify glycated hemoglobin (HbA1c), blood pressure (BP), body mass index (BMI), lipids, cardiovascular risk profile (CVR), self-perceived health status (SHS), and pharmaceutical expenditure (PE). DESIGN: A randomized, single blind, controlled trial. Intervention: program of supervised aerobic physical exercise. Analysis by intention to treat. LOCATION: Primary Care: 2 rural health areas. Health Area of Navalmoral. Cáceres. Extremadura. Spain. PARTICIPANTS: 100 type 2 diabetic patients, aged 65 to 80 years, sedentary. Distribution: 50% control group (CG) and 50% intervention group (IG). Abandoned 12%. Intervention: monitored aerobic exercise: 40 minutes, 2 days/week, 3 months. Key measures: HbA1c, BP, BMI, lipid, CVR, SHS, PE.complications during exercise. RESULTS: There were post-intervention differences between groups in HbA1c, BP, BMI, cholesterol and SHS. In the IG, there was a significant decrease in; HbA1c: 0.2 ± 0.4% (95% CI: 0.1 to 0.3), systolic BP: 11.8 ± 8.5 mmHg (95% CI: 5.1 to 11.9), BMI: 0.5 ± 1 (95% CI: 0.2 to 0.8), total cholesterol: 14 ± 28.2 mg/dl (95% CI: 5.9 to 22.2), LDL: 18.3 ± 28.2 mg/dl 95% CI: 10.2 to 26.3), CVR: 6.7 ± 7.7% (95% CI: 4.5 to 8.9), PE: 3.9 ± 10.2 Euros (95% CI: 0.9 to 6.8), and an increase in SHS; 4.7 ± 5.7 (95% CI: 3 to 6.3). CONCLUSIONS: In diabetics over 65 years, a program of monitored aerobic exercise, of easy implementation, improves HbA1c, BP, cholesterol, CVR, PE, and SHS
Subject(s)
Humans , Male , Female , Middle Aged , Aged , Aged, 80 and over , Exercise/physiology , Sedentary Behavior , Diabetes Mellitus, Type 2/epidemiology , Diabetes Mellitus, Type 2/prevention & control , Arterial Pressure/physiology , Body Mass Index , Cardiovascular Diseases/prevention & control , Primary Health Care/economics , Primary Health Care/organization & administration , Rural Health Services/organization & administration , Case-Control Studies , 28599 , Helsinki DeclarationABSTRACT
OBJECTIVE: To analyze whether an exercise program can modify glycated hemoglobin (HbA1c), blood pressure (BP), body mass index (BMI), lipids, cardiovascular risk profile (CVR), self-perceived health status (SHS), and pharmaceutical expenditure (PE). DESIGN: A randomized, single blind, controlled trial. INTERVENTION: program of supervised aerobic physical exercise. Analysis by intention to treat. LOCATION: Primary Care: 2 rural health areas. Health Area of Navalmoral. Cáceres. Extremadura. Spain. PARTICIPANTS: 100 type 2 diabetic patients, aged 65 to 80 years, sedentary. Distribution: 50% control group (CG) and 50% intervention group (IG). Abandoned 12%. INTERVENTION: monitored aerobic exercise: 40minutes, 2 days/week, 3 months. KEY MEASURES: HbA1c, BP, BMI, lipid, CVR, SHS, PE. Complications during exercise. RESULTS: There were post-intervention differences between groups in HbA1c, BP, BMI, cholesterol and SHS. In the IG, there was a significant decrease in; HbA1c: 0.2±0.4% (95% CI: 0.1 to 0.3), systolic BP: 11.8±8.5mmHg (95% CI: 5.1 to 11.9), BMI: 0.5±1 (95% CI: 0.2 to 0.8), total cholesterol: 14±28.2mg/dl (95% CI: 5.9 to 22.2), LDL: 18.3±28.2mg/dl 95% CI: 10.2 to 26.3), CVR: 6.7±7.7% (95% CI: 4.5 to 8.9), PE: 3.9±10.2 (95% CI: 0.9 to 6.8), and an increase in SHS; 4.7±5.7 (95% CI: 3 to 6.3). CONCLUSIONS: In diabetics over 65 years, a program of monitored aerobic exercise, of easy implementation, improves HbA1c, BP, cholesterol, CVR, PE, and SHS.
Subject(s)
Cardiovascular Diseases/prevention & control , Diabetes Mellitus, Type 2/therapy , Exercise Therapy , Glycated Hemoglobin , Sedentary Behavior , Aged , Aged, 80 and over , Blood Pressure , Body Mass Index , Female , Humans , Male , Risk Factors , Rural Population , Single-Blind Method , SpainABSTRACT
A marine metabolite based on a previously undescribed carbon skeleton, aberrarone (1), is reported as a natural product from the Caribbean sea whip, Pseudopterogorgia elisabethae. The molecular structure of the crystalline metabolite was established by spectral analysis and subsequently confirmed by X-ray crystallographic analysis. Aberrarone shows in vitro antimalarial activity against a chloroquine-resistant strain of the protozoan parasite Plasmodium falciparum.
Subject(s)
Anthozoa/chemistry , Biological Factors/chemistry , Diterpenes/chemistry , Animals , Antimalarials/chemistry , Antimalarials/isolation & purification , Antimalarials/pharmacology , Biological Factors/isolation & purification , Biological Factors/pharmacology , Crystallography, X-Ray , Diterpenes/isolation & purification , Diterpenes/pharmacology , Models, Molecular , Molecular Structure , StereoisomerismABSTRACT
Analysis of the terpene metabolites of Pseudopterogorgia elisabethae collected in San Andrés island, Colombia has resulted in the discovery of a novel metabolite, elisapterosin F (1). The tangled molecular structure of 1, which was elucidated after extensive spectroscopic data interpretation, possesses hydrophilic and hydrophobic groups located on two opposite faces, rather than at two ends as in the more conventional head/tail amphiphiles.
ABSTRACT
The extraction of two specimens of Pseudopterogorgia elisabethae, each collected from a different location at the San Andrés Archipelago, afforded two new norditerpenes, caribenols A (1) and B (2). Metabolites 1 and 2 contain unusual carbon skeletons that are previously undescribed and therefore constitute new classes of C19 rearranged terpenes. Their molecular structures were established by a combination of single-crystal X-ray analysis and comprehensive 2D NMR measurements.
Subject(s)
Anthozoa/chemistry , Diterpenes/chemistry , Animals , Crystallography, X-Ray , Diterpenes/isolation & purification , Molecular Conformation , Nuclear Magnetic Resonance, Biomolecular , Polycyclic Compounds/chemistry , Polycyclic Compounds/isolation & purificationABSTRACT
As part of an ongoing program to explore the chemical constituents of Caribbean marine invertebrates, a family of 13 new diterpene glycosides, pseudopterosins P-Z (1-11) and seco-pseudopterosins H (12) and I (13), have been isolated from the organic extracts of two collections of the sea whip Pseudopterogorgia elisabethae procured near the Colombian Southwestern Caribbean Sea. The structures of compounds 1-13, including absolute stereochemistry, have been proposed on the basis of comprehensive spectral analyses, chemical transformations, specific rotation, and TLC chromatographic analyses. Pseudopterosin Q (2) inhibited thromboxane B2 (TXB2) (IC50 = 4.7 microM) and superoxide anion (O2-) (IC50 = 11.2 microM) generation from E. coli lipopolysaccharide (LPS) activated rat neonatal microglia in vitro. In contrast, pseudopterosins P (1), U (6), V (7), W (8), and X (9) as well as seco-pseudopterosins H (12) and I (13) demonstrated minimal effects on both TXB2 and O2- release. In addition, some of the new compounds displayed strong antituberculosis, antiviral, antimalarial, and anticancer activity.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/isolation & purification , Antimalarials/isolation & purification , Antineoplastic Agents/isolation & purification , Antitubercular Agents/isolation & purification , Antiviral Agents/isolation & purification , Cnidaria/chemistry , Diterpenes/isolation & purification , Glycosides/isolation & purification , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Antimalarials/chemistry , Antimalarials/pharmacology , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Antitubercular Agents/chemistry , Antitubercular Agents/pharmacology , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Diterpenes/chemistry , Diterpenes/pharmacology , Glycosides/chemistry , Glycosides/pharmacology , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Oceans and Seas , RatsABSTRACT
In the course of our study to find novel antimycobacterial secondary metabolites from Caribbean gorgonian octocorals, we have isolated a new diterpene alkaloid, namely, homopseudopteroxazole (1), as a minor constituent of the hexane extract from the sea plume Pseudopterogorgia elisabethae. Its structure was deduced by interpretation of combined spectroscopic data, including extensive 1D and 2D NMR measurements, and NMR spectral comparisons with known amphilectane models. Biological screening studies indicate that homopseudopteroxazole (1) is a strong growth inhibitor of Mycobacterium tuberculosis H(37)Rv.
