Abstract:Two new limonoids, kostchyienones A (1) and B (2), along with 12 known compounds 3-14 were isolated from the roots of Pseudocedrela kostchyi. Compound (7) was isolated for the first time from a natural source. Their structures were elucidated on the basis of spectroscopic evidence. Compounds 1-6 and 13-14 gave IC50 values ranging from 0.75 to 5.62 μg/mL for antiplasmodial activity against chloroquine-sensitive (Pf3D7) and chloroquine-resistant (PfINDO) strains of Plasmodium falciparum. Compound 5 showed modera… Show more
“…Antiplasmodial activity of the new compounds against 3D7 and Pf INDO strains was selective, and the compounds were not toxic to HEK239T cells (IC 50 > 200 µg/mL). The antiplasmodial activity of limonoids has been attributed to the presence of the α, β-unsaturated carbonyl moiety in the structures, which may be involved in Michael-type addition reactions [182]. Fig.…”
BackgroundMalaria remains a significant public health challenge in regions of the world where it is endemic. An unprecedented decline in malaria incidences was recorded during the last decade due to the availability of effective control interventions, such as the deployment of artemisinin-based combination therapy and insecticide-treated nets. However, according to the World Health Organization, malaria is staging a comeback, in part due to the development of drug resistance. Therefore, there is an urgent need to discover new anti-malarial drugs. This article reviews the literature on natural products with antiplasmodial activity that was reported between 2010 and 2017.MethodsRelevant literature was sourced by searching the major scientific databases, including Web of Science, ScienceDirect, Scopus, SciFinder, Pubmed, and Google Scholar, using appropriate keyword combinations.Results and DiscussionA total of 1524 compounds from 397 relevant references, assayed against at least one strain of Plasmodium, were reported in the period under review. Out of these, 39% were described as new natural products, and 29% of the compounds had IC50 ≤ 3.0 µM against at least one strain of Plasmodium. Several of these compounds have the potential to be developed into viable anti-malarial drugs. Also, some of these compounds could play a role in malaria eradication by targeting gametocytes. However, the research into natural products with potential for blocking the transmission of malaria is still in its infancy stage and needs to be vigorously pursued.
“…Antiplasmodial activity of the new compounds against 3D7 and Pf INDO strains was selective, and the compounds were not toxic to HEK239T cells (IC 50 > 200 µg/mL). The antiplasmodial activity of limonoids has been attributed to the presence of the α, β-unsaturated carbonyl moiety in the structures, which may be involved in Michael-type addition reactions [182]. Fig.…”
BackgroundMalaria remains a significant public health challenge in regions of the world where it is endemic. An unprecedented decline in malaria incidences was recorded during the last decade due to the availability of effective control interventions, such as the deployment of artemisinin-based combination therapy and insecticide-treated nets. However, according to the World Health Organization, malaria is staging a comeback, in part due to the development of drug resistance. Therefore, there is an urgent need to discover new anti-malarial drugs. This article reviews the literature on natural products with antiplasmodial activity that was reported between 2010 and 2017.MethodsRelevant literature was sourced by searching the major scientific databases, including Web of Science, ScienceDirect, Scopus, SciFinder, Pubmed, and Google Scholar, using appropriate keyword combinations.Results and DiscussionA total of 1524 compounds from 397 relevant references, assayed against at least one strain of Plasmodium, were reported in the period under review. Out of these, 39% were described as new natural products, and 29% of the compounds had IC50 ≤ 3.0 µM against at least one strain of Plasmodium. Several of these compounds have the potential to be developed into viable anti-malarial drugs. Also, some of these compounds could play a role in malaria eradication by targeting gametocytes. However, the research into natural products with potential for blocking the transmission of malaria is still in its infancy stage and needs to be vigorously pursued.
“…The trypanocidal and leishmanicidal activity of compounds 1-6 are in good agreement with previously reported antiprotozoal activities. For instance, the GI 50 values for their anti-plasmodial activity were found to be within the range of 1.7-19.3 μM [8]. Compounds 3 and 4 have been previously reported to inhibit the growth of bloodstream forms of T. brucei rhodesiense with GI 50 values of 3.4 μM [21].…”
Section: Resultsmentioning
confidence: 92%
“…However, it should be pointed out that in this study a cancer cell line was used for determining selectivity and that, compared with non-malignant cells, the cytotoxicity of compound 1 may, therefore, be overestimated. For example, the cytotoxicity of 1 for the immortalised human embryonic kidney cell line HEK239T was previously determined to be > 200 μg/mL [8]. Based on this cytotoxicity, compound 1 would match the selectivity index activity criteria for drug candidates for both bloodstream forms of T. brucei and intracellular amastigotes of L. major.…”
Section: Resultsmentioning
confidence: 99%
“…The limonoids 1-6 were isolated from the roots of P. kotschyi as previously described [8]. The compounds have been characterized by NMR (kotschyienone A and B (1, 2 [8], 7-deacetylgedunin (3) [9, 10], 7-deacetyl-7-oxogedunin (4) [9,11], andirobin (5) [12] and methyl angolensate (6) [11]) and their purity was judged to be about 95% by TLC. The 1 H-NMR and 13 C-NMR spectra of 1-6 are shown in Supplementary Figures S1-6.…”
Six limonoids [kotschyienone A and B (1, 2), 7-deacetylgedunin (3), 7-deacetyl-7-oxogedunin (4), andirobin (5) and methyl angolensate (6)] were investigated for their trypanocidal and leishmanicidal activities using bloodstream forms of Trypanosoma brucei and promastigotes of Leishmania major. Whereas all compounds showed anti-trypanosomal activity, only compounds 1-4 displayed anti-leishmanial activity. The 50% growth inhibition (GI 50) values for the trypanocidal and leishmanicidal activity of the compounds ranged between 2.5 and 14.9 μM. Kotschyienone A (1) was found to be the most active compound with a minimal inhibition concentration (MIC) value of 10 μM and GI 50 values between 2.5 and 2.9 μM. Only compounds 1 and 3 showed moderate cytotoxicity against HL-60 cells with MIC and GI 50 values of 100 μM and 31.5-46.2 μM, respectively. Compound 1 was also found to show activity against intracellular amastigotes of L. major with a GI 50 value of 1.5 μM. The results suggest that limonoids have potential as drug candidates for the development of new treatments against trypanosomiasis and leishmaniasis.
“…antiparasitary [8][9][10] antidiabetic [11] and others pathologies [12]. But, also, Ceiba pentandra and Pseudocedrela kotschyi are used to treat fever [13][14][15].…”
Background: Several classical antipyretics are used to treat fever. But their harmful sides effects have led to the research of the others alternative based on medicine herbals. Rarely, studies are focused on the onset of action and assess the effects of Drugs Herbal interaction in vivo using experimental models. The main objective of this work is to assess potential antipyretic activities of two African plants (Ceiba pentandra and Pseudocedrela kotschyi concerning the onset of action and evaluate the effects of their association to the combination based on artemisinin (CTA). Methods: Turpentine 2 ml/kg, yeast brewers 20%, boiled milk 1 ml/kg were used to induce fever in young rats. The crudes of the extract of Ceiba pentandra 200 mg/kg; 400 mg/kg and Pseudocedrela kotschyi 100 and 150 mg/kg were administered orally and the temperatures (°C) were taken each 10 minutes. The Drugs-Herbal medicine interactions were also assessed (Extracts of our plants plus CTA). GraphPad Prism software version 7 was used to analyse the data. The difference was considered significant when P<0.05. Results: Aqueous extract of the Ceiba pentandra and Pseudocedrela kotschyi quickly reduce the fever by reducing the onset time of action (10-30 minutes). P-value<0.001 but our study has shown pharmacodynamics interaction between CTA and Pseudocedrela. There may have some interaction between CTA and the natural compounds contained in these medicine plants that reduce their efficacy. Conclusion: This present study showed the onset action of our two plants is between 10-30 minutes. Their association with CTA reduce the efficacy of extracts aqueous of leaves of Pseudocedrela kotschyi 150 mg/kg but no Ceiba pendantra 400 mg. They may be used as an alternative to classical drugs as antipyretics especially in children. But others studies may be done to assess the pharmacokinetic pharmacodynamics interactions with association based on artemisinin.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
