title: Unsaponifiable Fraction of Unripe Fruits of Olea europaea: An Interesting Source of Anti-inflammatory Constituents.
abstract: The unsaponifiable fraction of olive oil from unripe fruits of Olea europaea at different stages of maturation (from 20 to 32 weeks after flowering) was analyzed by gas chromatography-mass spectrometry in order to select the time associated to the unsaponifiable fraction with the maximal yield in bioactive constituents. According to quantitative gas chromatography-mass spectrometry analysis, the unsaponifiable fraction (2.46% of the total oil) from olive fruits at the 22nd week was found to contain the maximal yield in anti-inflammatory constituents. Its composition was lanosterol (2.60 mg/g oil), stigmasterol (2.15), cycloartanol acetate (2.04), stigmastan-3,5-diene (2.01), obtusifoliol (1.93), cholesta-4,6-dien-3-one (1.42), α-amyrin (1.42), α-tocopherol (1.32), squalene (1.02), β-amyrin (0.57), and β-sitosterol (0.22). At later times, there was a decrease in the quantitative unsaponifiable fraction yield and a qualitative shift in the bioactive constituents. The 22nd week unsaponifiable fraction was subsequently incorporated into a topical preparation to be utilized for a small pilot clinical study in five patients affected by osteoarthrosis. According to clinical observation, the application of the ointment (three times daily for three weeks) attenuated hand and knee joint inflammatory features in all patients and was not associated to any adverse reactions.
authors.affiliation: Department of Pharmaceutical Sciences, Università degli Studi di Milano, Milan, Italy.
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Gelmini
authors.affiliation: Department of Pharmacological and Biomolecular Sciences, Università degli Studi di Milano, Milan, Italy.
authors.forename: Massimiliano
authors.initials: M
authors.lastname: Ruscica
authors.affiliation: Department of Pharmacological and Biomolecular Sciences, Università degli Studi di Milano, Milan, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Macchi
authors.affiliation: Department of Pharmaceutical Sciences, Università degli Studi di Milano, Milan, Italy.
authors.forename: Viviana
authors.initials: V
authors.lastname: Bianchi
authors.affiliation: Department of Pharmaceutical Sciences, Università degli Studi di Milano, Milan, Italy.
authors.forename: Roberto
authors.initials: R
authors.lastname: Maffei Facino
authors.affiliation: Department of Pharmaceutical Sciences, Università degli Studi di Milano, Milan, Italy.
authors.forename: Giangiacomo
authors.initials: G
authors.lastname: Beretta
authors.affiliation: Department of Pharmacological and Biomolecular Sciences, Università degli Studi di Milano, Milan, Italy.
authors.forename: Paolo
authors.initials: P
authors.lastname: Magni
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000302:isolation & purification* / Q000627:therapeutic use*; D005591:Chemical Fractionation; D005260:Female; D005638:Fruit / Q000737:chemistry; D006801:Humans; D008297:Male; D008875:Middle Aged; D009824:Ointments; D031658:Olea / Q000737:chemistry; D010003:Osteoarthritis / Q000188:drug therapy*; D010865:Pilot Projects; D012503:Saponins
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D009824:Ointments; D012503:Saponins