Abstract:O estudo fitoquímico das flores e frutos verdes de Senna spectabilis forneceu um novo alcaloide 2,6-dialquilpiperidin-3-ol chamado de (-)-7-hidróxi-cassina, juntamente com cinco alcaloides conhecidos: (-)-cassina, (-)-espectalina, (-)-3-O-acetil-espectalina, (-)-7-hidróxi-espectalina e (-)-6-iso-espectalina. Além dos alcaloides, também foram isolados constituintes químicos de outras classes como o esteroide β-sitosterol, os flavonoides luteolina e 3-metóxi-luteolina, o triterpeno ácido betulínico e o ácido tra… Show more
“…In the 1 H-NMR spectra, compound C.8.3.1 showed similarities to the compound (−)-7-hydroxycassine (Fig. 6 ) in the presence of several similar chemical shifts [ 26 ]. Fig.…”
Background
In previous studies, Cassia spectabilis DC leaf has shown a good antiplasmodial activity. Therefore, this study is a follow-up study of the extract of leaf of C. spectabilis DC on its in vitro and in vivo antiplasmodial activity and mechanism as an antimalarial.
Methods
The extract was fractionated, sub-fractionated and isolated to obtain the purified compound. In vitro antiplasmodial activity test against Plasmodium falciparum to find out the active compound. In vivo test against P. berghei ANKA-infected mice was conducted to determine prophylactic activity and antiplasmodial activity either alone or in combination with artesunate. The inhibition of heme detoxification test as one of the antimalarial mechanisms was carried out using the Basilico method.
Results
The results showed that active antimalarial compound isolated from C. spectabilis DC leaf had a structural pattern that was identical to (−)-7-hydroxycassine. Prophylactic test of 90% ethanolic extract of C. spectabilis DC leaf alone against P. berghei ANKA-infected mice obtained the highest percentage inhibition was 68.61%, while positive control (doxycycline 13 mg/kg) was 73.54%. In combination with artesunate, 150 mg/kg three times a day of C. spectabilis DC (D0-D2) + artesunate (D2) was better than the standard combination of amodiaquine + artesunate where the inhibition percentages were 99.18 and 92.88%, respectively. The IC50 of the extract for the inhibitory activity of heme detoxification was 0.375 mg/ml which was better than chloroquine diphosphate (0.682 mg/ml).
Conclusion
C. spectabilis DC leaf possessed potent antiplasmodial activity and may offer a potential agent for effective and affordable antimalarial phytomedicine.
“…In the 1 H-NMR spectra, compound C.8.3.1 showed similarities to the compound (−)-7-hydroxycassine (Fig. 6 ) in the presence of several similar chemical shifts [ 26 ]. Fig.…”
Background
In previous studies, Cassia spectabilis DC leaf has shown a good antiplasmodial activity. Therefore, this study is a follow-up study of the extract of leaf of C. spectabilis DC on its in vitro and in vivo antiplasmodial activity and mechanism as an antimalarial.
Methods
The extract was fractionated, sub-fractionated and isolated to obtain the purified compound. In vitro antiplasmodial activity test against Plasmodium falciparum to find out the active compound. In vivo test against P. berghei ANKA-infected mice was conducted to determine prophylactic activity and antiplasmodial activity either alone or in combination with artesunate. The inhibition of heme detoxification test as one of the antimalarial mechanisms was carried out using the Basilico method.
Results
The results showed that active antimalarial compound isolated from C. spectabilis DC leaf had a structural pattern that was identical to (−)-7-hydroxycassine. Prophylactic test of 90% ethanolic extract of C. spectabilis DC leaf alone against P. berghei ANKA-infected mice obtained the highest percentage inhibition was 68.61%, while positive control (doxycycline 13 mg/kg) was 73.54%. In combination with artesunate, 150 mg/kg three times a day of C. spectabilis DC (D0-D2) + artesunate (D2) was better than the standard combination of amodiaquine + artesunate where the inhibition percentages were 99.18 and 92.88%, respectively. The IC50 of the extract for the inhibitory activity of heme detoxification was 0.375 mg/ml which was better than chloroquine diphosphate (0.682 mg/ml).
Conclusion
C. spectabilis DC leaf possessed potent antiplasmodial activity and may offer a potential agent for effective and affordable antimalarial phytomedicine.
“…1), a natural homologue that was previously isolated from C. spectabilis DC flower and fruit (12). 12 In spectra 1 H-NMR, it was possible to observe…”
Background In previous studies, Cassia spectabilis DC leaf has shown a good antimalarial activity. Therefore, this study is a follow-up study of leaf activity and mechanism of C. spectabilis DC as an antimalarial. Methods In vitro antimalarial activity testing using P. falciparum which was done with bioassay guide isolation in order to obtain the active compound. In vivo testing towards infected P. berghei mice was conducted to determine the effects of antimalarial prophylaxis and antimalarial activity in combination with artesunate. Whereas, heme detoxification inhibition testing as one of the antimalarial mechanisms was carried out using the Basilico method. Results The results showed that active antimalarial isolate obtained from C. spectabilis DC leaf had a structural pattern that was identical to (-)-7-hydroxyspectaline. Prophylactic test on infected P. berghei mice obtained the highest dose of inhibition percentage of 90% ethanol extract of C. spectabilis DC leaf was 68.61% while positive (doxycycline) control at 100 mg kg-1 was 73.54%. In antimalarial testing in combination with artesunate, it was found that administering 150 mg kg-1 (three times a day) of C. spectabilis DC (D0 − D2) + artesunate (D2) was better than the standard combination of amodiaquine + artesunate with 99.18% and 92.88% inhibition percentage. For the inhibitory activity of heme detoxification from ethanol extract 90%, C. spectabilis DC leaf had IC50 value of 0.375 mg mL-1 which was better than chloroquine diphosphate. Conclusion These results showed that C. spectabilis DC leaves possesses potent antimalarial activity and may offer a potential agent for effective and affordable antimalarial phytomedicine.
“…People consume medicinal plants especially caffeinated products without knowing the toxicity profile, in this paper, Drosophila melanogaster is used as a model for testing the toxicity profile of the isolated compound which is considered one of the most important genetic models' organisms for biomedical science (Nicholas, 2017). It is very much used for genetic research because the relationship between humans and the fruit fly (Tadeusz, 2007;Junior, et al, 2013).…”
Caffeine is the most frequently ingested pharmacologically active substance in the World. It is found in common coffee, tea, soft drinks, in products containing cocoa or chocolate, and in medications among others. Because of its wide consumption at different levels by most of the people, the scientific community as well as the general public have expressed interest in the potential for caffeine to produce adverse effects on human health. This study was carried out to isolate and characterize caffeine from root bark extract of Piliostigma thonningii and to study the toxicity profile of the isolated isolate. The ethyl acetate fraction was gradiently eluted in a silica gel column to afford an isolate coded EA, in which its purity was confirmed by preparative thin layer chromatography (TLC). Structure of the isolate was elucidated using spectroscopic techniques such as 1H NMR, 13C {H}NMR and Infrared spectroscopy (IR). and literature comparison suggested the isolated compound EA as an alkaloid namely 1,3,7-Trimethylpurine-2,6 dione. Drosophila melanogaster oral toxicity of the EA against 30 adults fruit flies (15 males and 15 females) was carried out using standard procedure. results showed mortality rate of 0 % at 14 mg/10g diet for 7 days. The Locomotor assay was done using negative geo-axis assay, results showed 70 % of flies reached the top of the glass bottle (10 cm height) at concentration of 5 mg/10g diet. The isolate EA from P. thonningii root bark is safe for oral consumption up to a concentration of 14 mg/10gdiet.
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