This book describes the phytochemical investigations carried out on two indigenous medicinal plants of Pakistan namely, Isatis costata and Leucas urticifolia. Part A is about the isolation and structure elucidation of five new alkaloids named as costinone A, costinone B, isatinone A, isatinone B and isamide. In addition, five known compounds caffeic acid ester, docosyl caffeate, methyl-2 acetoamidobenzoate, -sitosterol and ursolic acid have also been isolated and characterized for the first time from this species. Compounds costinone A and costinone B inhibited lipoxygenase and butyrylcholinesterase enzymes non-competitively in concentration-dependent fashion with promising inhibitory potentials. Compounds isatinone A and isatinone B showed vital antifungal activity. Part B describes the isolation and structure elucidation of two new compounds named as leucisterol and urticic acid, along with four known compounds named as 2-methoxybenzyl benzoate , 4-hydroxy benzoic acid , -sitosterol and ursolic acid which are reported first time from this species. The compound leucisterol showed potent inhibitory activity against butyrylcholinesterase enzyme.