New secondary metabolites with immunosuppressive and BChE inhibitory activities from an endophytic fungus Daldinia sp. TJ403-LS1

Five new acetylenic phenol derivatives (1-4 and 7), one new benzofuran derivative (8), one new naphthol derivative (9), and two known analogues (5 and 6), were isolated and identified from an endophytic fungus Daldinia sp. TJ403-LS1 that was isolated from the medicinally valuable plant Anoectochilus roxburghii. Their structures were elucidated by means of extensive spectroscopic analyses and electronic circular dichroism (ECD) calculations. In addition, compound 1 exhibited remarkable immunosuppressive activity against LPS and antiCD3/anti-CD28 mAbs activated murine splenocytes proliferation with the same IC50 values of 0.06 mu M and BChE inhibitory activity with an IC50 value of 6.93 +/- 0.71 mu M, and compounds 6, 8 and 9 showed excellent BChE inhibitory activity with IC50 values of 16.00 +/- 0.30, 23.33 +/- 0.55, and 15.53 +/- 0.39 mu M, respectively (positive drug neostigmine, IC50 = 49.60 +/- 6.10 mu M), highlighting the promising potentials to be designed and developed as immunosuppressive and BChE inhibitory agents.

Automated summary

Several new compounds were isolated from the endophytic fungus Daldinia sp. TJ403-LS1, with compound 1 showing remarkable immunosuppressive and BChE inhibitory activities, indicating their potential for pharmaceutical development.