Abstract
Cnidoscolus tehuacanensis is an endemic medicinal species used to treat some inflammatory diseases, and biosynthesizes triterpenes and sterols, being Lupeol Acetate (LuAc) the main compound. It was submitted to biological assay to determine the anti-inflammatory and leishmanicidal potential. Anti-inflammatory effect was determined on acute (12-O-tetradecanoylphorbol-13-acetate -TPA- and Carragenan models) and chronic inflammatory models (induce with Complet Freud´s Adjuvant -CFA-) using Indomethacin and Phenylbutazone (PBZ) as reference drugs. In vitro leishmanicidal activity was determined on Leishmania mexicana promastigotes and amastigotes, Miltefosine and amphotericin B were used as reference drugs. In TPA assay, LuAc showed an ED50=1.79 mg/ear (Ind, ED50=0.91 mg/ear) and on Carragenan model, the antiinflammatory effect was not dose-dependent, in this case LuAc at 100, 150 and 250 mg/kg showed 43.31, 40.22 and 51.25% of inhibition, respectively at 5 h. On CFA chronic inflammatory model, LuAc and PBZ groups showed similar anti-inflammatory effect and similar Body Weight (BW) gain although this value was less respect to healthy and CFA groups. Also, inhibited the COX-2 activity being this effect slightly better that PBZ, and the joints and soft tissue from LuAc and PBZ groups did not show any alteration with respect to CFA group. In soft tissue, CFA group showed a significant increase size and leukocyte infiltrate as a result of the chronic inflammatory process; it group also showed sinusoidal hyperplasia in the joint. In liver histological analysis, the healthy and LuAc groups showed no alteration, and the CFA group showed a slight microabscess and scarce hematopoiesis, while the PBZ group presented scarce steatosis. The fraction (rich in LuAc) and LuAc pure were less active that extract against L. mexicana promastigotes. C. tehuacanesis is a potential source of LuAc. This natural compound showed a good anti-inflammatory activity (similar effect to PBZ) and did not cause liver damage.
Highlights
Lupeol acetate (LuAc) is the main compound isolated from aerial parts of the Cnidoscolus tehuacanensis Breckon (C. tehuacanensis); it is an endemic species located in the Biosphere Reserve located within the valley of Tehuacán, Puebla and Cuicatlán, Oaxaca and Received: January 14, 2020, Accepted: April 25, 2020, Published: May 02, 2020Citation: Juárez-Vázquez MDC, Siordia-Reyes GA, Pérez-González MZ, Chávez-Rueda KA, Legorreta-Haquet MV, Nieto-Meneses R, et al (2020) Leishmanicidal and anti-inflammatory activities of Lupeol Acetate isolated from Cnidoscolus tehuacanensis Breckon
The MS was operated in scan mode from 45-500 m/z; ion source temp was set at 200°C; ionization was performed in the impact ionization mode (I.I.) with ionization voltage set at 70 eV
In primary fraction 40-58 (1400 mg, eluted with Hex 100%), LuAc was detected as a main compound, it was obtained as white powder with m.p. 203-205°C and Retention factor (Rf)=0.55 in Thin-Layer Chromatography (TLC), using Hex:EtOAc (95:5) as elution system and sprayed with H2SO4 10%; in addition, this primary fraction was analyzed by Gas Chromatograph (GC)-MS (Figure 1)
Summary
Lupeol acetate (LuAc) is the main compound isolated from aerial parts of the Cnidoscolus tehuacanensis Breckon (C. tehuacanensis); it is an endemic species located in the Biosphere Reserve located within the valley of Tehuacán, Puebla and Cuicatlán, Oaxaca and Received: January 14, 2020, Accepted: April 25, 2020, Published: May 02, 2020. In Calipán, Puebla, the aerial parts of the plant are used to treat problems related to inflammation and as an antiseptic for the treatment of lesions and skin infections [1,2]. Other minor compounds reported from aerial parts of this medicinal plants are β-amyrin acetate, lupeol, lupenone, α-and β-amyrin, amyrenone, germanicol (3β-olean-18-en3-ol), β-betulin (lup-20(29)-ene-3β,28-diol), 9,19-cyclolanost-24-en-3ol acetate, lanosterol acetate, isoorientin and amentoflavone [2]. It has been reported that LuAc suppresses the expression of cytokines related with inflammation, avoids bone erosion and improves symptoms in cases of Rheumatoid Arthritis (RA); in addition, it favored osteoclastogenesis in in vitro model using the RAW 264.7 cell line. In another study, was reported that LuAc (administered every 48 h by oral via, from day 32 to 40, post adjuvant administration) at 66 mg/kg shown antiAR effect in a model of Complet Freuds Adjuvant (CFA)-induced arthritic rats [4]
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