Espécies de Pilocarpus Vahl (Rutaceae) da Amazônia brasileira

Skorupa, L. A.

doi:10.1590/1809-43922000301070

Cited by 11 publications

(9 citation statements)

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“…Brazilian biodiversity has been studied extensively and increasing numbers of studies related to plant species and natural resources have contributed to new therapeutic alternatives. An example of this development concerns the Pilocarpus microphyllus Stapf ex Wardlew species, popularly known as jaborandi, originating from North and Northeast Brazil [ 1 , 2 ]. Pilocarpine alkaloid is produced commercially by extraction from jaborandi leaves; the alkaloid is used commercially for eye procedures and treatment of glaucoma, and is therefore of great economic interest [ 3 , 2 ].…”

Section: Introductionmentioning

confidence: 99%

Epiisopilosine alkaloid has activity against Schistosoma mansoni in mice without acute toxicity

et al. 2018

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Schistosomiasis is a disease caused by parasites of the genus Schistosoma, currently affecting more than 200 million people. Among the various species of this parasite that infect humans, S. mansoni is the most common. Pharmacological treatment is limited to the use of a single drug, praziquantel (PZQ), despite reports of parasite resistance and low efficacy. It is therefore necessary to investigate new potential schistosomicidal compounds. In this study, we tested the efficacy of epiisopilosine (EPIIS) in a murine model of schistosomiasis. A single dose of EPIIS (100 or 400 mg/kg) administered orally to mice infected with adult S. mansoni resulted in reduced worm burden and egg production. The treatment with the lower dose of EPIIS (100 mg/kg) significantly reduced total worm burden by 60.61% (P < 0.001), as well as decreasing hepatosplenomegaly and egg excretion. Scanning electron microscopy revealed morphological changes in the worm tegument after treatment. Despite good activity of EPIIS in adult S. mansoni, oral treatment with single dose of EPIIS 100 mg/kg had only moderate effects in mice infected with juvenile S. mansoni. In addition, we performed cytotoxicity and toxicological studies with EPIIS and found no in vitro cytotoxicity (in HaCaT, and NIH-3T3 cells) at a concentration of 512 μg/mL. We also performed in silico analysis of toxicological properties and showed that EPIIS had low predicted toxicity. To confirm this, we investigated systemic acute toxicity in vivo by orally administering a 2000 mg/kg dose to Swiss mice. Treated mice showed no significant changes in hematological, biochemical, or histological parameters compared to non-treated animals. Epiisopilosine showed potential as a schistosomicidal drug: it did not cause acute toxicity and it displayed an acceptable safety profile in the animal model.

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Section: Introductionmentioning

confidence: 99%

Epiisopilosine alkaloid has activity against Schistosoma mansoni in mice without acute toxicity

et al. 2018

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“…Pilocarpus microphyllus Stapf ex Wardlew is a species native to Brazil and is found in the north (Pará State) and northeast (Maranhão and Piauí States) macroregions of Brazil. Also known as jaborandi, this shrub occurs in less dense forests, often on rocky outcrops and in habitats with high light intensity (Skorupa, ) . Members of this family contain a wide variety of secondary metabolites such as alkaloids, coumarins, lignans and terpenoids (Guerreiro et al ., ).…”

Section: Introductionmentioning

confidence: 99%

Anthelmintic, Antibacterial and Cytotoxicity Activity of Imidazole Alkaloids fromPilocarpus microphyllusLeaves

et al. 2017

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Pilocarpus microphyllus Stapf ex Wardlew (Rutaceae), popularly known as jaborandi, is a plant native to the northern and northeastern macroregions of Brazil. Several alkaloids from this species have been isolated. There are few reports of antibacterial and anthelmintic activities for these compounds. In this work, we report the antibacterial and anthelmintic activity of five alkaloids found in P. microphyllus leaves, namely, pilosine, epiisopilosine, isopilosine, epiisopiloturine and macaubine. Of these, only anthelmintic activity of one of the compounds has been previously reported. Nuclear magnetic resonance, HPLC and mass spectrometry were combined and used to identify and confirm the structure of the five compounds. As regards the anthelmintic activity, the alkaloids were studied using in vitro assays to evaluate survival time and damaged teguments for Schistosoma mansoni adult worms. We found epiisopilosine to have anthelmintic activity at very low concentrations (3.125 μg mL ); at this concentration, it prevented mating, oviposition, reducing motor activity and altered the tegument of these worms. In contrast, none of the alkaloids showed antibacterial activity. Additionally, alkaloids displayed no cytotoxic effect on vero cells. The potent anthelmintic activity of epiisopilosine indicates the potential of this natural compound as an antiparasitic agent. Copyright © 2017 John Wiley & Sons, Ltd.

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“…The flowers are actinomorphic tetramers or pentamers. The pistil has carpels fused at the base resulting in mericarps (Skorupa 2000).…”

Section: Introductionmentioning

confidence: 99%

Screening species of Pilocarpus (Rutaceae) as sources of pilocarpine and other imidazole alkaloids

Sawaya

Vaz

Eberlin

et al. 2011

Genet Resour Crop Evol

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Plants of the Pilocarpus genus (Rutaceae) are popularly known as jaborandi and are the only source of pilocarpine, an imidazole alkaloid used in eye-drops for the treatment of glaucoma as well as for the stimulation of sweat and lachrymal glands. Alkaloid extracts from leaf samples of seven species of Pilocarpus, from the states of São Paulo and Maranhão in Brazil, were analyzed using HPLC-ESI-MS/MS. The samples contained between 0.88 ± 0.04 and 1.00 ± 0.14% of alkaloids in relation to the dry weight of their leaves, with significant differences in results (P B 0.05) found only between Pilocarpus microphyllus planted in the state of Maranhão and Pilocarpus spicatus, Pilocarpus trachyllophus, Pilocarpus pennatifolius and Pilocarpus jaborandi; as well as between Pilocarpus spicatus and Pilocarpus racemosus. Pilocarpine was not found in P. spicatus, whereas in the other species it ranged from 2.6 ± 0.1 to 70.8 ± 1.2% of total alkaloids. P. microphyllus planted in the state of Maranhão for pilocarpine extraction had the highest total alkaloid content, but it had only 35% of pilocarpine in relation to total alkaloids. Three other species contained more pilocarpine in relation to total alkaloids: P. jaborandi (70.8%), P. racemosus (45.6%) and P. trachyllophus (38.7%); and could be candidates for pilocarpine extraction. Differences in alkaloid content were significant for all these samples (P B 0.05). Imidazole alkaloids were observed and partially characterized based on their retention times and high resolution mass. The seven species analyzed had different imidazole alkaloid profiles, but only one did not present quantifiable pilocarpine contents in its leaves. The Pilocarpus genus shows potential for the prospection of novel alkaloids.

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Espécies de Pilocarpus Vahl (Rutaceae) da Amazônia brasileira

Cited by 11 publications

References 0 publications

Epiisopilosine alkaloid has activity against Schistosoma mansoni in mice without acute toxicity

Epiisopilosine alkaloid has activity against Schistosoma mansoni in mice without acute toxicity

Anthelmintic, Antibacterial and Cytotoxicity Activity of Imidazole Alkaloids fromPilocarpus microphyllusLeaves

Screening species of Pilocarpus (Rutaceae) as sources of pilocarpine and other imidazole alkaloids

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