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. 2012 Apr 16;2(2):303-36.
doi: 10.3390/metabo2020303.

A historical overview of natural products in drug discovery

Daniel A Dias  1 , Sylvia Urban  2 , Ute Roessner  3
Affiliations

A historical overview of natural products in drug discovery

Daniel A Dias et al. Metabolites. .

Abstract

Historically, natural products have been used since ancient times and in folklore for the treatment of many diseases and illnesses. Classical natural product chemistry methodologies enabled a vast array of bioactive secondary metabolites from terrestrial and marine sources to be discovered. Many of these natural products have gone on to become current drug candidates. This brief review aims to highlight historically significant bioactive marine and terrestrial natural products, their use in folklore and dereplication techniques to rapidly facilitate their discovery. Furthermore a discussion of how natural product chemistry has resulted in the identification of many drug candidates; the application of advanced hyphenated spectroscopic techniques to aid in their discovery, the future of natural product chemistry and finally adopting metabolomic profiling and dereplication approaches for the comprehensive study of natural product extracts will be discussed.

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Figures

Figure 1
Figure 1
Acetylsalicyclic acid (1), Salicin (2), Morphine (3), Digitoxin (4), Quinine (5) and Pilocarpine (6).
Figure 2
Figure 2
Penicillin (7), Norcardicin (8), Imipenem (9) and Aztreonam (10).
Figure 3
Figure 3
Vancomycin (11) and Erythromycin (12).
Figure 4
Figure 4
Betulinic acid (13), Bevirimat (PA-457) (14) and Ganoderic acid β (15).
Figure 5
Figure 5
Amrubicin hydrochloride (16), Doxorubicin (17) and Torreyanic acid (18).
Figure 6
Figure 6
Paclitaxel (Taxol®) (19) and baccatin III (20).
Figure 7
Figure 7
ingenol 3-O-angelate (21), PG490-88 (22) and Combretastatin A-4 phosphate (23).
Figure 8
Figure 8
Calanolide A (24), Calanolide B (25) and Prostratin (26).
Figure 9
Figure 9
Arteether (27) and artemisinin (28).
Figure 10
Figure 10
Grandisine A (29), Grandisine B (30), morphine (31), apomorphine (32) and tubocaurarine (33).
Figure 11
Figure 11
Plitidepsin (34), ET743, Spisulosine (36) and Cryptophycin (37).
Figure 12
Figure 12
Polycavernoside-A (38), 4-acetoxydictylolactone (39), Dictyolide A (40), Dictyolide B (41), Nordictyolide (42) and Crenuladial (43).
Figure 13
Figure 13
Compound (44), Compound (45), Compound (46), 1α-(2-E-chlorovinyl)-2α,4β,5α-trichloro-1β,5β-dimethylcyclohexane (47), 1β-(2-E-chlorovinyl)-2β,4α,5α-trichloro-1α,5β-dimethylcyclohexane (48), Laurepinnacin (49) and (Z)-laureatin (50).
Figure 14
Figure 14
Spongouridine (51) and Spongothymidine (52).
Figure 15
Figure 15
Compound (53), Bryostatin 1 (54) Halichondrin B (55) and Halichondrin E-7389 (56).
Figure 16
Figure 16
Sorafendib (57).
Figure 17
Figure 17
Myxoprincomide (58).
Figure 18
Figure 18
Ginsenoside Rf (59), 20(S)-pseudoginsenoside F11 (60), Malonyl gisenoside Rb1 (61), and gisenoside Rb2 (62).
Figure 19
Figure 19
Galphimine (63).
Figure 20
Figure 20
Dihydrocucurbitacin F-25-O-acetate (64).
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