Bioactivity-directed fractionation of the CHCl3-MeOH extract of the leaves of Celaenodendron mexi... more Bioactivity-directed fractionation of the CHCl3-MeOH extract of the leaves of Celaenodendron mexicanum by means of the brine shrimp lethality test and chromatographic techniques led to the isolation of three carboxylic acid triterpenes, the new tirucalla-type triterpene, 3 alpha-hydroxytirucalla-7,24Z-dien-26-oic acid, 3-oxotirucalla-7,24Z-dien-26-oic acid, and epi-oleanolic acid, and three biflavonoids amentoflavone, podocarpusflavone A, and podocarpusflavone B. Four non-active compounds friedelin, maytensifolin B, 3 beta-hydroxyfriedelan-16-one, and celaenodendrolide were also obtained. epi-Oleanolic acid was the most active against brine shrimps with LC50 value of 23.3 microM. In addition, all isolates were tested for in vitro antiprotozoal and cytotoxic activities. 3-Oxotirucalla-7,24Z-dien-26-oic acid and epi-oleanolic acid showed the highest activity against Leishmania donovani promastigotes with IC50 values of 13.7 and 18.8 microM, respectively. Only 3-oxotirucalla-7,24Z-dien-26-oic acid showed activity against Trypanosoma brucei brucei bloodstream forms with IC50 value of 16.8 microM.
Oral administration of a CH2Cl2–MeOH (1:1) extract of Scaphyglottis livida produced dose-dependen... more Oral administration of a CH2Cl2–MeOH (1:1) extract of Scaphyglottis livida produced dose-dependent antinociceptive and anti-inflammatory effects when tested in mice and rats using the hot-plate (150–600mg/kg) and carrageenan-induced inflammation (150–600mg/kg) models, respectively. Morphine (1.5–6mg/kg, p.o.) and indomethacin (10–40mg/kg, p.o.) were used as positive controls, respectively. Four compounds were isolated from the active extract of Scaphyglottis livida, namely 5α-lanosta-24,24-dimethyl-9(11),25-dien-3β-ol (LDD), 24,24,dimethyl-9,19-cyclolanosta-9(11),25-dien-3-one (cyclobalanone), gigantol and 3,4′-dihydroxy-3′,4,5-trimethoxybibenzyl (DTB). LDD and gigantol (25–100mg/kg, p.o.) significantly increased the hot-plate latency in comparison to vehicle-treated mice and decreased carrageenan-induced inflammation in rats. The antinociception provoked by LDD and gigantol was partially blocked by naloxone (1mg/kg, i.p.). However, pretreatment with l-NAME (100mg/kg, i.p.) and glibenclamide (10mg/kg, i.p.) did not affect the antinociceptive response induced by LDD or gigantol suggesting that their pharmacological effect could be partially due to activation of opioid receptors. Moreover, a CH2Cl2–MeOH (1:1) extract of Maxillaria densa reduced acetic acid-induced abdominal writhes but was not able to produce antinociception in the hot-plate assay. Two compounds were isolated from the active extract of Maxillaria densa, namely fimbriol A and erianthridin. Both compounds partially reduced acetic acid-induced writhes. The results tend to support the popular use of this species in folk medicine for treatment of painful complaints.
Bioactivity-directed fractionation of the CHCl3-MeOH extract of the leaves of Celaenodendron mexi... more Bioactivity-directed fractionation of the CHCl3-MeOH extract of the leaves of Celaenodendron mexicanum by means of the brine shrimp lethality test and chromatographic techniques led to the isolation of three carboxylic acid triterpenes, the new tirucalla-type triterpene, 3 alpha-hydroxytirucalla-7,24Z-dien-26-oic acid, 3-oxotirucalla-7,24Z-dien-26-oic acid, and epi-oleanolic acid, and three biflavonoids amentoflavone, podocarpusflavone A, and podocarpusflavone B. Four non-active compounds friedelin, maytensifolin B, 3 beta-hydroxyfriedelan-16-one, and celaenodendrolide were also obtained. epi-Oleanolic acid was the most active against brine shrimps with LC50 value of 23.3 microM. In addition, all isolates were tested for in vitro antiprotozoal and cytotoxic activities. 3-Oxotirucalla-7,24Z-dien-26-oic acid and epi-oleanolic acid showed the highest activity against Leishmania donovani promastigotes with IC50 values of 13.7 and 18.8 microM, respectively. Only 3-oxotirucalla-7,24Z-dien-26-oic acid showed activity against Trypanosoma brucei brucei bloodstream forms with IC50 value of 16.8 microM.
Oral administration of a CH2Cl2–MeOH (1:1) extract of Scaphyglottis livida produced dose-dependen... more Oral administration of a CH2Cl2–MeOH (1:1) extract of Scaphyglottis livida produced dose-dependent antinociceptive and anti-inflammatory effects when tested in mice and rats using the hot-plate (150–600mg/kg) and carrageenan-induced inflammation (150–600mg/kg) models, respectively. Morphine (1.5–6mg/kg, p.o.) and indomethacin (10–40mg/kg, p.o.) were used as positive controls, respectively. Four compounds were isolated from the active extract of Scaphyglottis livida, namely 5α-lanosta-24,24-dimethyl-9(11),25-dien-3β-ol (LDD), 24,24,dimethyl-9,19-cyclolanosta-9(11),25-dien-3-one (cyclobalanone), gigantol and 3,4′-dihydroxy-3′,4,5-trimethoxybibenzyl (DTB). LDD and gigantol (25–100mg/kg, p.o.) significantly increased the hot-plate latency in comparison to vehicle-treated mice and decreased carrageenan-induced inflammation in rats. The antinociception provoked by LDD and gigantol was partially blocked by naloxone (1mg/kg, i.p.). However, pretreatment with l-NAME (100mg/kg, i.p.) and glibenclamide (10mg/kg, i.p.) did not affect the antinociceptive response induced by LDD or gigantol suggesting that their pharmacological effect could be partially due to activation of opioid receptors. Moreover, a CH2Cl2–MeOH (1:1) extract of Maxillaria densa reduced acetic acid-induced abdominal writhes but was not able to produce antinociception in the hot-plate assay. Two compounds were isolated from the active extract of Maxillaria densa, namely fimbriol A and erianthridin. Both compounds partially reduced acetic acid-induced writhes. The results tend to support the popular use of this species in folk medicine for treatment of painful complaints.
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