Evaluation of Anxiolytic potential of various extracts of Caesalpinia pulcherrima leaves

Caesalpinia pulcherrima Swartz native to India referred to as Guletura is widely distributed in South India, and its leaves, flower, bark, and seeds are employed in Indian medicine. The plant contains many active elemental fractions like caesalpin-type diterpenoids, sitosterol, pulcherrimin, lupeol, lupeol acetate, myricetin, quercetin and rutin, flavonoids, carotenoids, glycosides, peltogynoids, phenols, and steroids. The current study was designed to gauge the anti-anxiety activity of varied extracts viz n-hexane, chloroform, ethyl acetate, and methanol of the leaves of Caesalpinia pulcherrima by using elevated plus maze (EPM) model in albino mice. Albino mice have ministered orally with different doses of the extracts (i.e. 200 and 400mg/kg) and behavior was observed on the EPM. Diazepam (2mg/kg, P.O) was used as a standard (positive control). Results indicate that the methanol extract of Caesalpinia leaves showed maximum and significant dose-dependent effect at 200 and 400mg/kg on EPM, the results were just like the standard antianxiety agent diazepam (2mg/kg). In the Actophoptometer model, two different doses of Caesalpinia pulcherrima (200 and 400mg/kg) showed a dose-dependent decrease within the locomotor activity, compared to the control animals. As the phytochemical screening of methanol extract exhibited the presence of polyphenols could be liable for the anxiolytic potential of C.pulcherrima. Hence this plant could also be developed as a potentially useful anti-anxiety agent.

Isolation, Chemical Characterization, Evaluation of Analgesic and Anti-Inflammatory Activities of Triterpenoids from the Tubers of Raphionacme vignei E. A. Bruce (Apocynaceae)

Raphionacme vignei E. A. Bruce (Apocynaceae) is a plant of the traditional African pharmacopoeia, whose parts are used in the treatment of various pathologies. Water-soaked R. vignei tubers are edible. The objective of this study was to isolate triterpenoids from the acetonic extract of R. vignei tubers, evaluate the analgesic and anti-inflammatory activities of each molecule. The isolated compounds, characterized by NMR and mass spectrometry, is composed of six triterpenoids: beta-amyrin dodecanoate 1(DDQ1), lupeol dodecanoate 2(DDQ2), beta-amyrin acetate 3(DDQ3), lupeol acetate 4(DDQ4), luepol 5(DDQ5) and β-sitosterol 6(DDQ6). These molecules (DDQ2, DDQ3, DDQ4, DDQ5, DDQ6) are anti-inflammatory in carrageenan induced rat paw edema, with better anti-inflammatory power for DDQ2 and DDQ4, which would be related to the presence of acetate function and cycle E. DDQ2 and DDQ4 are also analgesic in acetic acid induced contortions and the removal test of rat tail on the heating plate. The analgesic action of DDQ2 and DDQ4, superior to that salicylic acetyl acid, identical to that morphine, suggests a central action of these two molecules. The potent analgesic effect of DDQ2 and DDQ4, could be attributed to the presence of cyclopentane and isoprene substitution in position 19 of the lupane family. DDQ2 and DDQ4 represent a potential for the synthesis of structural analogues with analgesic and/or anti-inflammatory properties.

Lupeol acetate as a potent antifungal compound against opportunistic human and phytopathogenic mold Macrophomina phaseolina

Antifungal activity of Monothecabuxifolia methanolic extract and its various fractions were assessed against Macrophominaphaseolina, a soil-borne fungal pathogen of more than 500 vegetal species as well as rare and emerging opportunistic human pathogen. Different concentrations of methanolic extract (3.125 to 200 mg mL−1) inhibited fungal biomass by 39–45%. Isolated n-hexane, chloroform and ethyl acetate fractions suppressed fungal biomass by 32–52%, 29–50% and 29–35%, respectively. Triterpenes lupeol and lupeol acetate (1, 2) were isolated from n-hexane while betulin, β-sitosterol, β-amyrin, oleanolic acid (3–6) were isolated from chloroform fraction. Vanillic acid, protocatechuic acid, kaempferol and quercetin (7–10) were isolated from the ethyl acetate fraction and identified using various spectroscopic techniques namely mass spectroscopy and NMR. Antifungal activity of different concentrations (0.0312 to 2 mg mL−1) of the isolated compounds was evaluated and compared with the activity of a broad spectrum fungicide mancozeb. Different concentrations of mencozeb reduced fungal biomass by 83–85%. Among the isolated compounds lupeol acetate (2) was found the highest antifungal against M.phaseolina followed by betulin (3), vanillic acid (7), protocatechuic acid (8), β-amyrin (5) and oleanolic acid (6) resulting in 79–81%, 77–79%, 74–79%, 67–72%, 68–71% and 68–71%, respectively. Rest of the compounds also showed considerable antifungal activity and reduced M.phaseolina biomass by 41–64%.

Profil Metabolit Daun Kesambi (Schleichera oleosa) Berdasarkan Analisis Histokimia dan In Silico

Kesambi (Schleichera oleosa) is a plant belonging to the Sapindaceae familia. This study aims to determine the secondary metabolite compounds found in kesambi leaves through histochemical analysis and derivatives of active compounds in silico. Descriptive experimental research method was conducted in January using samples of kesambi plants that grow on the island of Madura. Histochemical analysis was carried out by preparing fresh leaves through lower leaf incisions with secondary metabolite detection reagents (CuSO4, FeCl3, Wagner, Sudan III, AlCl3 & FeCl3+NaCO3) then microscopic color changes were observed. In silico testing aims to determine the interaction of active compounds with ER? as a target for ER + breast cancer therapy through molecular docking. Supporting software used is KNApSAcK, Pubchem, Pass Online, PDB ID, PyRx, PyMol and Chimera 1.14. The results showed that through histochemical analysis six secondary metabolite compounds were identified, namely terpenoids, flavonoids, alkaloids, tannins, lipophils and phenols. While in silico analysis, the active compound is scopoletin which is derived from phenol, beta-sitosterol, betulin, betulinic acid, lupeol, lupeol acetate, schleicheol 1&2, schleicherastatin 1-7 which are derivatives of terpenoids. Based on the results of molecular docking, there are interactions of active compounds with 3ERT protein, the compounds that provide the most effective results as candidates for breast cancer drugs are lupeol acetate with a value of Root Mean Square Deviation (RMSD) lb 1,588 Å and ub 2,219 Å . Lupeol acetate compound is predicted to have activity as an Er? inhibitor against ER+ breast cancer. Keywords: Kesambi (Schleichera oleosa), histochemistry, molecular docking and ER?.

New Anti-inflammatory Triterpene Esters and Glycosides from Alstonia scholaris

Background:: Phytochemical studies on the ethanolic extract of aerial parts of Alstonia scholaris lead to the isolation of two new triterpenoid of the lanostanetype, lanosta 5ene,24-ethyl-3-O-β-D-glucopyranoside (1), lanosta,5ene,24-ethyl-3-O-β-D-glucopyranosideester (2) and new ursane type triterpenoidmethylester, 12-ursene-2,3,18,19-tetrol,28 acetate (nighascholarene) (3), together with seven known triterpenes, betuline, triterpene of the lupane type, alstoprenyol (4), 3β-hydroxy-28-β-acetoxy-5-olea triterpene (5),α-amyrin acetate (6), α-amyrin (7), lupeol acetate (8), 3β-hydroxy-24-nor-urs-4,12,28-triene triterpene (9) and ursolic acid (l0). Methodology:: The triterpenoid structures of these colorless compounds were deduced from the 1H and 13C-NMR data, and in particular from the application of two-dimensional 1H, 13C correlation experiments as well as by comparison with reported literature data. Results and Conclusion: This study deals with isolation and structural elucidation of natural new triterpenoidesters and glycosides with anti-inflammatory activity.

Chemical Composition and Antioxidant Activity of Essential Oils and Hexane Extract of Onopordum arenarium from Tunisia

In the present study, volatile oils from Onopordum arenarium fresh flowers and stems were obtained by hydrodistillation and the non-polar aerial part hexane extract was prepared using a Soxhlet apparatus. The constituents of different organs were identified for the first time by gas chromatography equipped with flame ionization detector and gas chromatography coupled to mass spectrometry. A total of 29 and 25 compounds were identified constituting over 91.6 and 89.2% of the whole constituents from flower and stem volatile oils, respectively. Both organs were constituted mainly of long-chain hydrocarbons (23.3–36.4%) followed by oxygenated long-chain hydrocarbons (31.5–33.8%) and oxygenated monoterpenes (14.4–6.6%). The major identified compound was palmitic acid [25.5% in O. arenarium flower essential oil (EO) and 28.7% in the stem EO]. Eighteen compounds representing 80.7% of the whole constituents were identified in the n-hexane extract, which was characterized by high amounts of triterpenoids (39.6%) and dominated by lupeol acetate (19.2%) and β-amyrin acetate (10.1%). Moreover, all extracts were evaluated for antioxidant potential using 1,1-diphenyl-2-picrylhydrazyl radical assay. The obtained results demonstrated that the EOs and the hexane extract could be a new source of natural potentially bioactive molecules.