Natural compounds and extracts from Mexican medicinal plants with anti-leishmaniasis activity: An update

Leishmaniasis is considered as an emerging, uncontrolled disease and is endemic in 98 countries. Annually, about 2 million cases of cutaneous and 500000 cases of visceraltype leishmaniasis are recorded and 60000 persons died from the disease. In Mexico,cutaneous leishmaniasis is known as chiclero's ulcer and is reported in 22 states, it is considered as a health problem. For its treatment, pentavalent antimonial drugs are administered. These drugs cause severe side effects, are costly. Drug-resistant cases have been reported and have been developing for over 70 years. One alternative to the drugs that are currently available is to find active molecules in medicinal plants. Dihydrocorynantheine, corynantheine and corynantheidine are active against Leishmania major,while harmane, pleiocarpin, buchtienin, luteolin and quercetin are active against Leishmania donovani. In Mexico, about 20 medicinal plants have been evaluated against Leishmania mexicana, among which the most active are Tridax procumbens, Lonchocarpus xuul and Pentalinon andrieuxii. From these plants, active compounds with IC_(50)≤30 mg/mL or m M have been isolated, such as 3(S)-16,17-didehydrofalcarinol or Oxylipin, cholestra-4,20,24-trien-3-one or pentalinosterol, 24-methylcholest-4-24(28)-dien-3-one, cholest-4-en-3-one, 6,7-dihydroneridie-none, neridienone, cholest-5,20,24-trien-3β-ol, and isocordoin. Today, only pentalinonsterol has been synthesized and assayed in the visceral leishmaniasis experimental model using BALB/c mice infected with Leishmania donovani. Liposome formulation of this compound administered by intravenous route at 2.5 mg/kg showed a significant reduction of parasite load in mouse liver and spleen.

Cytotoxic Effect of Methanol Extracts and Partitions of Two Mexican Desert Plants against the Murine Lymphoma L5178Y-R

Pachycereus marginatus (DC.) Britton & Rose and Ibervillea sonorae (S. Watson) Greene have been used in the Mexican traditional medicine for the treatment of various diseases, including cancer. The present study aims to investigate the cytotoxic activity of these plants against a murine lymphoma. Soxhlet extraction of dried and powdered plant material was performed with methanol. Also, a further partitioning of these methanolic extracts with hexane and ethyl acetate was achieved. The in vitro cytotoxic activity against the murine lymphoma L5178Y-R cell line was assessed via the colorimetric MTT assay. The methanol extract from P. marginatus exhibited high cytotoxic activity (up to 94%) at concentrations ranging from 3.9 to 500 μg/mL;however, hexane and ethyl acetate partitions from this methanolic extract showed lower but significant (p < 0.05) concentration-dependent cytotoxicity (hexane partition up to 94% at 500 μg/mL;ethyl acetate partition up to 94% at 65.5 μg/mL). The methanolic extract and partitions derived from I. sonorae also showed significant (p < 0.05) and concentration-dependent cytotoxicity against L5178Y-R cells at concentrations ranging from 7.81 to 500 μg/mL (methanolic extract up to 63% at 500 μg/mL;hexane partition up to 76% at 250 μg/mL;ethyl acetate partition up to 73% at 500 μg/mL). These results demonstrate that the methanol extracts and partitions from P. marginatus and I. sonorae possess significant cytotoxic activity against the murine lymphoma L5178Y-R and validate the ethnobotanical use of these plants for the treatment of diseases consistent with cancer symptomatology. Previous scientific reports describe the isolation of isoquinoline alkaloids of P. marginatus as well as cucurbitacins from I. sonorae, phytochemicals that could be responsible for their observed cytotoxic activity in this research. The direct extraction with methanol of medicinal plants allows extracting of both high and low-polarity compounds, contrary to the simple extraction with water that only allows obtaining compounds of high polarity. The subsequent partition of the methanol extract with a solvent of low polarity (hexane) and another of medium polarity (ethyl acetate) allows making a preliminary fractionation of the bioactive molecules present in the plant that will facilitate the bioguided chromatographic isolation of the pure compounds responsible for the biological activity of the plant.

Anti-inflammatory evaluation and acute toxicity of three food supplements that contain Moussonia deppeana

Objective:To identify the anti-inflammatory activity through two murine models and in the median Lethal Dose(LD_(50)) of three dietary supplements that contain Moussonia deppeana.Methods:The anti-inflammatory activity of three dietary supplements(Cicatrisan/Gastricus^(R),Gastinol^(R),and Gastrovita^(R)) EtOH extracts was evaluated by TPA and by carrageenan murine models;also,median Lethal Dose(LD_(50)) was determined.Verbascoside was quantified by High-Performance Liquid Chromatography.β-sitosterol,stigmasterol and the mixture of ursolic and oleanolic acids were identified in all supplements by TLC;however,none of these dietary supplements contain verbascoside.Results:For the TPA model,Cicatrisan/Gastricus^(R)generated a notable effect with 38.24%inhibition.While in the carrageenan model,it also exhibited noteworthy anti-inflammatory activity of ear edema with 66.39%of paw edema inhibition at 150 mg/kg,followed by Gastinol^(R) and Gastrovita^(R) with 50%at 300 mg/kg.Finally,LD_(50) was >2 g/kg for all supplements,when was administered intragastrically and Body Weight(BW) gain in mice was not altered after 14 days.Conclusions:Of the three food supplements containing M.deppeana,only the EtOH extract from the Cicatrisan/Gastricus^(R)formulation(tablets) showed significant anti-inflammatory activity in both experimental models and the LD_(50) was > 2 g/kg.