HPLC based activity profiling of Ganoderma lucidum extract for antiplasmodial activity and isolation of new active lanostane triterpenoids

Ganoderma lucidum mushroom (Curtis) P. Karst (Ganodermataceae) is known as lingzhi in Chinese and reishi or mannentake in Japanese. It has been used medicinally for thousands of years and is apraised as one of the most powerful remedies in traditional Chinese medicine [1]. Over 200 substances from this source have been isolated and structurally identified, mostly polysaccharides and lanostane triterpenes.

In a medium throughput screen of plant and fungal extracts for antiplasmodial activity [2] an ethyl acetate extract from lingzhi mushroom was active with a 79% inhibition at 4.9µg/ml. With analytical scale time-based HPLC separation and testing of one-minute fractions for their antiplasmodial activity in combination with hyphenated methods (HPLC-PDA, -MSⁿ, HR-MS, off line microprobe NMR) the active substances were identified. The substances were isolated using normal phase medium pressure column chromatography and semi-preparative HPLC, and structure elucidation was achieved by extensive ¹H and ¹³C NMR analysis. HPLC based activity profiling is an efficient tool to identify active minor compounds in complex extract matrices [3]. This way we could identify new active compounds from lingzhi mushroom despite the fact that it has already been studied extensively. This is the first report of antiplasmodial activity of this triterpenoid class.

References: [1] Pattersen R.R. et al. (2006) Phytochemistry 67:1985–2001.

[2] Kunert, O. et al. (2008) Phytochem. Lett. 1:171–174.

[3] Potterat, O. et al. (2006) Curr. Org. Chem. 10:899–920.