title: Tubulin polymerization-stimulating activity of Ganoderma triterpenoids.
abstract: Tubulin polymerization is an important target for anticancer therapies. Even though the potential of Ganoderma triterpenoids against various cancer targets had been well documented, studies on their tubulin polymerization-stimulating activity are scarce. This study was conducted to evaluate the effect of Ganoderma triterpenoids on tubulin polymerization. A total of twenty-four compounds were investigated using an in vitro tubulin polymerization assay. Results showed that most of the studied triterpenoids exhibited microtuble-stabilizing activity to different degrees. Among the investigated compounds, ganoderic acid T-Q, ganoderiol F, ganoderic acid S, ganodermanontriol and ganoderic acid TR were found to have the highest activities. A structure-activity relationship (SAR) analysis was performed. Extensive investigation of the SAR suggests the favorable structural features for the tubulin polymerization-stimulating activity of lanostane triterpenes. These findings would be helpful for further studies on the potential mechanisms of the anticancer activity of Ganoderma triterpenoids and give some indications on the design of tubulin-targeting anticancer agents.
authors.affiliation: Division of Systematic Forest and Forest Products Sciences, Department of Agro-Environmental Sciences, Graduate School of Bioresource and Bioenvironmental Sciences, Kyushu University, Fukuoka, 812-8581, Japan.|Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, 812-8582, Japan.
authors.forename: Toshitaka
authors.initials: T
authors.lastname: Kohno
authors.affiliation: Division of Systematic Forest and Forest Products Sciences, Department of Agro-Environmental Sciences, Graduate School of Bioresource and Bioenvironmental Sciences, Kyushu University, Fukuoka, 812-8581, Japan.
authors.forename: Tran
authors.initials: T
authors.lastname: Hai-Bang
authors.affiliation: Division of Systematic Forest and Forest Products Sciences, Department of Agro-Environmental Sciences, Graduate School of Bioresource and Bioenvironmental Sciences, Kyushu University, Fukuoka, 812-8581, Japan.|Department of Pharmacy, School of Medicine, Shenzhen University, 3688 Nanhai Boulevard, Nanshan District, Shenzhen, Guangdong, 518060, China.
authors.forename: Qinchang
authors.initials: Q
authors.lastname: Zhu
authors.affiliation: Division of Systematic Forest and Forest Products Sciences, Department of Agro-Environmental Sciences, Graduate School of Bioresource and Bioenvironmental Sciences, Kyushu University, Fukuoka, 812-8581, Japan.|Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt.
authors.forename: Yhiya
authors.initials: Y
authors.lastname: Amen
authors.affiliation: Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, 812-8582, Japan.
authors.forename: Seiichi
authors.initials: S
authors.lastname: Sakamoto
authors.affiliation: Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, 812-8582, Japan.
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Tanaka
authors.affiliation: Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, 812-8582, Japan.
authors.forename: Satoshi
authors.initials: S
authors.lastname: Morimoto
authors.affiliation: Division of Systematic Forest and Forest Products Sciences, Department of Agro-Environmental Sciences, Graduate School of Bioresource and Bioenvironmental Sciences, Kyushu University, Fukuoka, 812-8581, Japan. shimizu@agr.kyushu-u.ac.jp.
authors.forename: Kuniyoshi
authors.identifier: http://orcid.org/0000-0003-3803-6060
authors.initials: K
authors.lastname: Shimizu
mesh_terms: D032902:Ganoderma / Q000737:chemistry*; D006801:Humans; D058105:Polymerization; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000737:chemistry*; D014404:Tubulin / Q000378:metabolism*
chemical_list: D014315:Triterpenes; D014404:Tubulin
keywords: Ganoderma; Microtubule; Paclitaxel; Triterpenes; Tubulin polymerization