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The plant kingdom, both terrestrial and marine, is an underestimated pool of secondary metabolites some of which have enormous therapeutic potential to be an important source of new and unique agents. The identification of active compounds from complex botanical extracts is the main challenge in natural products discovery. The strategy used to discover active substances has been considerably changed in the last decade from the expensive and laborious methods in which bioactivity was studied only after isolation and identification of the components. The new strategy involves only the effective components being isolated and identified. Since chemical separation of the whole sample does not provide information about biological effects, neither do bioassays of the whole sample extracts provide information on observed therapeutic effects for compounds found in these extracts.