Aleurites moluccana (L.) Willd. Leaves: Mechanical Antinociceptive Properties of a Standardized Dried Extract and Its Chemical Markers

Abstract

Seeking to develop a new analgesic phytomedicine, a spray-dried extract (SDE) of Aleurites moluccana (L.) Willd. leaves was developed in scale up (5 kg). The SDE was standardized at 3% w/w in relation to the flavonoid 2′′-O-rhamnosylswertisin. The SDE batches were evaluated in relation to their physical, physiochemical, and pharmacological characteristics. The results demonstrated the reproducibility of the scale up SDE process which, when dosed orally, reduced carrageenan-induced mechanical hypernociception, with an ID50% of 443 mg/kg. Similar results were obtained with animals injected with complete Freund's adjuvant (CFA), in which SDE caused inhibition of 48 ± 4%. SDE was effective in preventing prostaglandin E2 (PGE2)-induced mechanical hypernociception (inhibition of 26 ± 10% and 33 ± 3%, at 250 and 500 mg/kg, respectively). Swertisin and 2′′-O-rhamnosylswertisin isolated from the own extract were effective in inhibiting the hypernociceptive response induced by carrageenan (70 ± 2% and 50 ± 5%, resp.). Furthermore, 2′′-O-rhamnosylswertisin was capable of significantly inhibiting the mechanical sensitization induced by CFA or PGE2, with inhibitions of 25 ± 3% and 94 ± 6%, respectively. These results suggest that the effects of SDE are related, at least in part, to the presence of these flavonoids.

Antinociceptive, anti-inflammatory and wound healing features in animal models treated with a semisolid herbal medicine based on Aleurites moluccana L. Willd. Euforbiaceae standardized leaf extract

“…It is commonly known as Kukui (''Light'') in Hawai'i, candlenut in the USA, tuitui in the Cook Islands and Tonga, lama in Samoa, ti'a'iri in Tahiti, 'ama in Marquesas, tutu'i in the Austral Islands, shi li in China, lauci in Fiji and kurup in Papua New Guinea (Leonard, 2012). The antinociceptive effect of A. moluccana was previously demonstrated by Meyre-Silva et al (1998 and mechanical anti-hypersensitivity of the orally dosed standardized spray dried extract of the plant was recently reported, with 3% of the chemical marker, the flavonoid 2*-O-rhamnosylswertisin (Quintão et al, 2011). At least in part, the antinociceptive effect of both A. moluccana spray dried and 2*-O-rhamnosylswertisin is due to its activity on the peripheral and central pathways of pain .…”

“…Considering that the existing drugs for the treatment of post-operative pain present major side effects, such as nausea, vomiting, ileus, respiratory depression, and sedation (Dahl and Kehlet, 2006), several pharmaceutical companies have sought to develop new effective and safe therapy (topical or systemic) for the prevention and treatment of postoperative pain. We have previously demonstrated the antinociceptive activity of A. moluccana spray dried extract and the flavonoids swertisin and 2*-O-rhamnosylswertisin, when administered orally, in different models of mechanical hypersensitivity in mice (Quintão et al, 2011). Recently, Quintão et al (2012) suggest that the compounds present in the A. moluccana dried extract, mainly 2*-O-rhamnosylswertisin, showed antinociceptive effect by interacting with (1) opioid system enhancing the Fig.…”

“…Ketamine and xylazine were purchased from Anasedan s (Miramar, FL, USA) and Dexamethasone from Galena (Campinas, SP, Brazil). The chemical markers swertisin and 2*-O-rhamnosylswertisin were isolated from A. moluccana leaves with HPLC purity of 495% (Quintão et al, 2011) The dried extracts composed by 1:10 dried leaves:solvent (ethanol 70% v/v), submitted to static maceration for 5 day at room temperature, were prepared at Centroflora (Botucatu-SP, Brazil) on a pilot scale (5 kg) composed of 25% (w/w total solids of concentrate extract) of colloidal silicon dioxide as describe in Quintão et al (2011). This dried extract was standardized to 3.0 and 0.4% of I and II, respectively (Cesca et al, 2012).…”

Asthma as a Respiratory Disorder: A Review

“…In fact, asthma patients show an elevated level of anxiety and depressive disorders than general public [74]. The more severe the disease is, the more severe are the psychological disorders and vice versa, especially among children and young adults [75]. Patients with uncontrolled asthma have a higher frequency of anxiety as compared to those with controlled asthma [76].…”

Herbal treatment in asthma and COPD – current evidence

“…More recently, the anti-nociceptive effects of A. molluccana [30,31] and its mechanical anti-hypersensitivity properties [32] have been investigated. A. mollucanna has also been found to possess antiviral [33] and antimicrobial properties [34] demonstrating how the presence of multiple active compounds in plant extracts can have several benefits to patients.…”