Evaluation of antimicrobial and antimalarial activities of crude extract, fractions and 4-nerolidylcathecol from the aerial parts ofPiper umbellataL. (Piperaceae)

Abstract

Presently, natural products, such as Piper umbellata L. (Piperaceae), have been evaluated as sources of antimicrobial agents with efficacies against microorganisms. The in vitro antimicrobial activity was performed by broth micro-dilution susceptibility assay, according to the protocols of the National Committee for Clinical Laboratory Standards, and described the antibacterial and antifungal activities of crude ethanolic extract and fractions obtained by partitions sequentially among water-methanol, methylene chloride and ethyl acetate, as well as the major constituent, 4-nerolidylcatechol from the aerial parts of P. umbellata L. Amphotericin B and ciprofloxacin were used as controls. Among the microorganism cultures, hydromethanol fraction demonstrated the pre-eminent antifungal activity. 4-Nerolidylcathecol was the only tested plant component that exhibited activity against all the selected microorganisms, suggesting its great potential as a source for the development of new drugs. In order to estimate the antimalarial activity of P. umbellata L., a micro-dilution method protocol, parasite lactate dehydrogenase assay, with a Plasmodium falciparum Sierra Leone (D6) clone was utilised. The antimalarial agent artemisinin was used as control. 4-Nerolidylcathecol exhibited the best antimalarial activity; however, it was not significant when compared with control. These in vitro results do not justify the use of P. umbellata L. in malaria patients. However, there is a possibility of 4-nerolidylcathecol, after biotransformation, exhibiting a significant antimalarial activity in in vivo assays. However, 4-nerolidylcathecol demonstrated to possess a broad antimicrobial activity which is, in fact, a promising source for the development of new therapeutic agents.

3D QSAR modeling of 4-nerolidylcatechol derivatives and virtual screening for identification of potent <i>plasmodium</i> inhibitor

“…4-nerolidylcatechol is a semi synthetic derivative of catechol known for its antimalarial activity. (Bagatela et al, 2013;Pinto et al, 2009;Rocha et al, 2011;Silva Lima et al, 2012).…”

“…The 4-Nerolidylcatechol has been studied for strong antimalarial property including antioxidant and anti-inflammatory activities as per the data of previous studies. In a recent investigation, new derivatives of 4-NC were synthesized and experimentally validated for the inhibition of Plasmodium (Bagatela et al, 2013;Pinto et al, 2009;Rocha et al, 2011;Silva Lima et al, 2012 …”

Investigation of the inhibitory effects from the Brazilian medicinal plant Pothomorphe umbellata L. (Piperaceae) on the molecular pathways of cyclooxygenase-2 and nuclear factor kappa B

“…The isolation of 4-nerolidylcatechol was performed by column chromatography and identified by nuclear magnetic resonance (NMR) through 13 C NMR and 1 H NMR analyses (Kijjoa et al, 1980;Bagatela et al, 2013) (Figure 1). …”

“…(Piperaceae) demonstrated the presence of several chemical constituents, such as β-stigmasterol, β-sitosterol, and campesterol (Perazzo et al, 2005;Pino et al, 2005;Baldoqui et al, 2009;Bagatela et al, 2013). Plants containing these bioactive molecules have previously demonstrated a significant anti-inflammatory activity (Navarro et al, 2001).…”

Anticholinesterases and antioxidant alkamides from Piper nigrum fruits

“…The family Piperaceae is composed of four major genera and nearly 4000 species, and they are reputed in various systems of medicine for their numerous medicinal properties, such as the Indian Ayurvedic system of medicine and folklore medicine of Latin America (Bagatela et al 2013;Lemos et al 2013;de Queiroz et al 2014;Sarwar et al 2015). Black pepper is the dried ripe fruit of Piper nigrum L., previous studies have revealed its chemical compositions (amide alkaloids, terpenoids, multimeric alkaloids and volatile oil) and activities (immunomodulatory, stimulatory, larvicidal, anti-inflammatory, antioxidant, antifertility, antiulcer, antifungal, antibacterial and anticholinesterase activities) (Ingkaninan et al 2003;Meghwal & Goswami 2013;Santiago et al 2015).…”