RESUMEN
Crude extracts (CH(2)Cl(2) and MeOH) of 20 plants in the family Acanthaceae were screened for their antiplasmodial, cytotoxic, antioxidant, and radical scavenging activities. These plants included Asystasia nemorum, Barleria cristata, B. strigosa, Dicliptera burmanni, Eranthemum tetragonum, Hygrophila ringens, Justicia balansae, J. procumbens, Lepidagathis incurva, Peristrophe lanceolaria, Phaulopsis dorsiflora, Ruellia kerrii, Strobilanthes auriculata, S. corrugata, S. cusia, S. dimorphotricha, S. karensium, S. maxwellii, S. pateriformis, and S. brandisii. CH(2)Cl(2) extracts of A. nemorum, S. corrugata, S. cusia, S. maxwellii, S. pateriformis, and S. brandisii, as well as MeOH extracts of J. balansae and J. procumbens, showed antiplasmodial activity with IC(50) values of 10-100 µg/mL. CH(2)Cl(2) extracts of nine plants including D. burmanni, H. ringens, J. balansae, J. procumbens, L. incurva, P. lanceolaria, P. dorsiflora, S. corrugata, and S. maxwellii showed cytotoxic activity with IC(50) values of 3.5-46.0 µg/mL. MeOH extracts (at 100 µg/mL) of R. kerrii and S. auriculata could effectively scavenge DPPH free radicals (82-83% inhibition) and superoxide anion radicals (79% and 88% inhibition). In the ORAC antioxidant assay, MeOH extracts of B. cristata, J. procumbens, R. kerrii, and S. auriculata exhibited activity with ORAC units of 3.1-3.9.
Asunto(s)
Acanthaceae , Antimaláricos/farmacología , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Neoplasias/tratamiento farmacológico , Extractos Vegetales/farmacología , Plasmodium falciparum/efectos de los fármacos , Antineoplásicos Fitogénicos/uso terapéutico , Línea Celular Tumoral , Depuradores de Radicales Libres/farmacología , Células Hep G2 , Humanos , Fitoterapia , Extractos Vegetales/uso terapéuticoRESUMEN
The leaves of Holarrhena pubescens yielded a new naringenin glycoside (1), together with naringin, naringenin 7-O-beta-D-glucoside, lupeol, lupeol beta-hydroxyhexadecanoate and ursolic acid. The structure of 1 was determined by spectral analysis.
Asunto(s)
Holarrhena , Fitoterapia , Extractos Vegetales/química , Humanos , Hojas de la Planta , Relación Estructura-ActividadRESUMEN
Chemical exploration of Camchaya calcarea (family Compositae) has led to the isolation of nine known sesquiterpene lactones 1 - 9, together with caffeic acid methyl ester 10. Sesquiterpenes 1, 2, 3, 4, 5, 7, and 8 exhibited moderate antiplasmodial activity, but showed potent antimycobacterial activity. Interestingly, the cytotoxicity of sesquiterpene lactones 1, 2, and 4 towards small-cell lung cancer cell line (NCI-H187) is stronger (two orders of magnitude) than towards the Vero cell line. Caffeic acid methyl ester (10) was cytotoxic against NCI-H187 and BC cell lines, however the ester 10 showed only mild antimycobacterial activity.
Asunto(s)
Antimaláricos/farmacología , Antineoplásicos Fitogénicos/farmacología , Asteraceae , Fitoterapia , Extractos Vegetales/farmacología , Plasmodium falciparum/efectos de los fármacos , Animales , Antimaláricos/administración & dosificación , Antimaláricos/uso terapéutico , Antineoplásicos Fitogénicos/administración & dosificación , Antineoplásicos Fitogénicos/uso terapéutico , Antituberculosos/administración & dosificación , Antituberculosos/farmacología , Antituberculosos/uso terapéutico , Línea Celular Tumoral/efectos de los fármacos , Concentración 50 Inhibidora , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/efectos de los fármacos , Pruebas de Sensibilidad Parasitaria , Componentes Aéreos de las Plantas , Extractos Vegetales/administración & dosificación , Extractos Vegetales/uso terapéuticoRESUMEN
Chemical investigation of biologically active compounds of Getonia floribunda led to the isolation of two new macrocyclic lactones, combretastatins D-3 (1) and D-4 (2). The structures of these compounds were confirmed by spectroscopic analyses. Combretastatin D-3 (1) exhibited cytotoxicity towards the small-cell lung cancer cell line (NCI-H187, IC50=13.0 +/- 0.2 microg/mL) but was inactive against KB, BC-1, and Vero cell lines. Combretastatin D-3 (1) showed weak antitubercular activity with a minimum inhibitory concentration (MIC) of 100.0 microg/mL, and was inactive towards the malarial parasite. Combretastatin D-4 (2) was inactive in all antitubercular, antiplasmodial, and cytotoxic assays.
Asunto(s)
Bibencilos/farmacología , Combretaceae , Fitoterapia , Estilbenos/farmacología , Antineoplásicos Fitogénicos/administración & dosificación , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/uso terapéutico , Antituberculosos/administración & dosificación , Antituberculosos/farmacología , Antituberculosos/uso terapéutico , Bibencilos/administración & dosificación , Bibencilos/uso terapéutico , Línea Celular Tumoral/efectos de los fármacos , Humanos , Concentración 50 Inhibidora , Lactamas Macrocíclicas/administración & dosificación , Lactamas Macrocíclicas/farmacología , Lactamas Macrocíclicas/uso terapéutico , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/efectos de los fármacos , Extractos Vegetales/administración & dosificación , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Estilbenos/administración & dosificación , Estilbenos/uso terapéuticoRESUMEN
Deoxypreussomerin derivatives, palmarumycins JC1 (1) and JC2 (2), and two dimeric naphthoquinones, isodiospyrin (3) and its new derivative isodiospyrol A (4), were isolated from dried fruits of Diospyros ehretioides. Structures of the isolated compounds were elucidated by spectroscopic analyses. Palmarumycins were not found in the extract of freshly collected fruits; however, they were present in dried fruit extract. The absence of palmarumycins in fresh fruits of D. ehretioides, together with the chemotaxonomic point of view, we proposed that palmarumycins JC1 (1) and JC2 (2) are more likely to be fungal metabolites, i.e., endophytes or epiphytes. The isolation of palmarumycins 1 and 2 from dried D. ehretioides fruits could be reproducible; both plant samples collected in the years 2002 and 2004 provided the same result, and, therefore, symbiont fungal strains should be specific to the plant host, D. ehretioides, and they can grow on the fruits during drying the sample. Palmarumycin JC1 (1) did not exhibit antimalarial, antifungal, antimycobacterial, and cytotoxic activities. Palmarumycin JC2 (2) exhibited antimalarial (IC50 4.5 microg/ml), antifungal (IC50 12.5 microg/ml), antimycobacterial (MIC 6.25 microg/ml), and cytotoxic (IC50 11.0 microg/ml for NCI-H187 cell line) activities. In our bioassay systems, isodiospyrin (3) did not exhibit antimycobacterial, antifungal, antimalarial, and cytotoxic activities. Isodiospyrol A (4) exhibited antimalarial (IC50 2.7 microg/ml) and antimycobacterial (MIC 50 microg/ml) activities, but was inactive towards Candida albicans. Compound 4 also exhibited cytotoxicity against BC cells (IC50 12.3 microg/ml), but not towards KB and Vero cell lines.