title: Sesquiterpenes from Carpesium macrocephalum inhibit Candida albicans biofilm formation and dimorphism.
abstract: One new xanthanolide, 4-(2-methybutyryl)-4H-tomentosin (1) was isolated from the whole plant of Carpesium macrocephalum together with nine known sesquiterpenes (2-10), including four eudesmane sesquiterpenes (2, 4, 5, and 10), one guaianolide (3), two xanthanolides (6 and 9) and two carabranolides (7 and 8). Their structures were elucidated on the basis of detailed spectroscopic analyses. All isolates were evaluated for their antifungal activities against the growth, biofilm formation and yeast-hyphal transition in Candida albicans. All compounds lacked the antifungal activity (MIC50>256 μg/ml) except compound 6 with the MIC50 value of 128 μg/ml. However, compounds 3, 5 and 10 strongly inhibited biofilm formation with IC50 values ranging from 15.4 to 38.0 μg/mL, and compounds 1, 3, 4, 6 and 7 inhibited the yeast-to-hyphae morphogenetic transition with the IC50 values between 31.6 and 118.4 μg/mL. The above results indicated that sesquiterpenes from C. macrocephalum may have therapeutic potential for candidiasis as virulence inhibitors.
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, People's Republic of China; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.
authors.forename: Chunfeng
authors.initials: C
authors.lastname: Xie
authors.affiliation: Department of Pharmacology, Medical School of Southeast University, Nanjing 210009, People's Republic of China.
authors.forename: Lingmei
authors.initials: L
authors.lastname: Sun
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, People's Republic of China.
authors.forename: Linghao
authors.initials: L
authors.lastname: Meng
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, People's Republic of China.
authors.forename: Meicheng
authors.initials: M
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, People's Republic of China.
authors.forename: Jing
authors.initials: J
authors.lastname: Xu
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology and College of Life Sciences, Nankai University, Tianjin 300071, People's Republic of China.
authors.forename: Mark
authors.initials: M
authors.lastname: Bartlam
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, People's Republic of China. Electronic address: victgyq@nankai.edu.cn.
authors.forename: Yuanqiang
authors.initials: Y
authors.lastname: Guo
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D019659:Asteraceae / Q000737:chemistry*; D018441:Biofilms / Q000187:drug effects*; D002176:Candida albicans / Q000187:drug effects*; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D012717:Sesquiterpenes / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C000612926:4-(2-methybutyryl)-4H-tomentosin; D000935:Antifungal Agents; D012717:Sesquiterpenes
keywords: Candida albicans; Carpesium macrocephalum; Sesquiterpenes; Virulence inhibitors