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During last three decades, plants have well proved their potential to produce a wide array of natural products with interesting biological activities. Among these, cyclopolypeptides and related congeners have received special attention due to their unique structures and wide pharmacological profile which may prove better candidates to overcome the problem of wide spread increase of resistance towards conventional drugs. Diverse bioactivities exhibited by plant-derived cyclic peptides include cytotoxic activity, immunosuppressive and antimalarial activity, vasorelaxant activity, tyrosinase inhibitory activity and estrogen-like activity. A natural cyclic polypeptide, segetalin D, was isolated from the seeds of higher plant Vaccaria segetalis (Caryophyllaceae) which have been used to activate blood flow and for treatment of amenorrhea and breast infections.