The present invention discloses a process for extraction of anticancer property exhibiting bio-active compounds 5a,8a-epidioxy-24£-methylcholesta-6,22-dien-3P-ol (LT-I) and Ergosta-5, 7, 22-trien-3p-ol (LT-II) from Lentinus tuberregium. The process involves drying and pulverizing the fruit bodies and mycelium of Lentinus tuberregium and extracting LT-I and LT-II by shaking the pulverized dried fruit bodies and mycelia with more than one appropriate organic solvent to obtain a suspension. Further the suspension was separated by centrifugation followed by filtration. Then the filtered suspension was dried in vacuum to obtain a crude organic extract. The crude extract along with silica gel is loaded into a column packed with silica gel and LT-I and LT-II were eluted separately from the column by elution using more than one appropriate organic solvents. The eluted LT-I and LT-II were purified to obtain pure LT-I and LT-II.
