Drug Discovery: A Biodiversity Perspective

  • Kholis A. AudahEmail author


Conventional drug discovery is believed to be much slower than the emerging of diseases. It could also cost pharmaceutical companies hundreds of million of dollars with no guarantee that the process would be a successful one. Therefore, new alternatives for drug discovery methods are urgently required.

Nature has been known as long as human history as very rich sources for various types of human needs including as medicinal sources. By implementing the concept of antigen versus antibody, venom versus antidote somehow taught us that Mother Nature has provided us the cures for every disease. It is just a matter of how to find the right drug for particular disease which is already available in the nature. In the United States of America alone, approximately 50% of drugs recognized by the Food and Drug Administration from the year 1981 until the year 2010 were originated from natural product pure extracts or their derivatives.

This chapter briefly described the power of nature as the abundant sources to find drugs for different kinds of illnesses include the challenges associated with the drug discovery process. By virtue of biodiversity both on land and in oceans, researchers can collect as many as possible extracts (extract library) that can be utilized as medicines through screening process. Drug discovery through screening process utilizing natural products can become a solution of the slow and expensive drug discovery process using conventional way. By the advancement of screening technology such as high throughput screening, thousands of extracts and or bioactive compounds can be screened against different types of diseases only in one day. The availability of extract library allows the acceleration of drug discovery in a faster and cheaper way.

Indonesia as one of the richest country in the world in biodiversity has high potential in providing a large collection of extracts for drug discovery purposes. One of potential plants as medicinal sources is Mangrove. Mangroves and mangrove associates widely spread along roughly 90,000 km Indonesian coastline. Indonesia is home of about 20 family with about hundreds species of mangroves and their associates. Indonesia has the largest mangrove forest or about 23% of total world mangrove forests. Taken altogether, Indonesia offers invaluable medicinal sources. This opens up many opportunities for collaboration among researchers nationally and internationally.


Natural products Biodiversity Extract library Drug discovery Screening 


  1. Ahmed Y, Sohrab H, Al-Reza SM, Shahidulla Tareq F, Hasan CM, Sattar MA (2010) Antimicrobial and cytotoxic constituents from leaves of Sapium baccatum. Food Chem Toxicol 48:549–552CrossRefPubMedGoogle Scholar
  2. Arslanyolu M, Erdemgil FZ (2006) Evaluation of the antibacterial activity and toxicity of isolated arctiin from the seeds of Centaurea sclerolepis. J Fac Pharm 35:103–109Google Scholar
  3. Atanasov AG et al (2015) Discovery and resupply of pharmacologically active plant-derived natural products: A review. Biotechnol Adv 33(2015):1582–1614CrossRefPubMedPubMedCentralGoogle Scholar
  4. Audah KA (2015) Proceedings of the International conference on innovation, entrepreneurship and technology, 25–26 November, BSD City, Indonesia, ISSN: 2477-1538Google Scholar
  5. Audah KA, Amsyir J, Almasyhur F, Hapsari AM, Sutanto H (2018) Development of extract library from Indonesian biodiversity: exploration of antibacterial activity of mangrove Bruguiera cylindrica leaf extracts. IOP Conf Ser Earth Environ Sci 130(1):012025CrossRefGoogle Scholar
  6. Balouiri M, Sadiki M, Ibnsouda SK (2016) Methods for in vitro evaluating antimicrobial activity: a review. J Pharm Anal 6(2):71–79CrossRefPubMedGoogle Scholar
  7. Balunas MJ, Kinghorn AD (2005) Drug discovery from medicinal plants. Life Sci 78(2005):431–441CrossRefPubMedGoogle Scholar
  8. Bandaranayake WM (2002) Bioactive compounds and chemicals constituents of mangrove plants. Wet Ecol Manag 10:421–452CrossRefGoogle Scholar
  9. Batubara I, Mitsunaga T (2013) Use of Indonesian medicinal plant products against acne. Rev Agric Sci 1:11–30Google Scholar
  10. Batubara I, Darusman LK, Mitsunaga T, Rahminiwati M, Djauhari E (2010) Potency of Indonesian medicinal plants as tyrosinase inhibitor and antioxidant agent. J Biol Sci 10(2):138144Google Scholar
  11. Bindseil KU, Jakupovic J, Wolf D, Lavayre J, Leboul J, van der Pyl D (2001) Pure compound libraries: a new perspective for natural product based drug discovery. Drug Discov Today 6:840–847CrossRefPubMedGoogle Scholar
  12. Brenk R, Schipani A, James D, Krasowski A, Gilbert IH, Frearson J, Wyatt PG (2008) Lessons learnt from assembling screening libraries for drug discovery for neglected diseases. ChemMedChem 3(3):435–444CrossRefPubMedGoogle Scholar
  13. Butler MS (2004) The role of natural product chemistry in drug discovery. J Nat Prod 67(12):2141–2153CrossRefPubMedGoogle Scholar
  14. Butler MS (2005) Natural products to drugs: natural product derived compounds in clinical trials. Nat Prod Rep 2005(22):162CrossRefGoogle Scholar
  15. Butler, R.A., 2016. The top 10 most biodiverse countries: What are the world’s most biodiverse countries? Retreved from internet on April 30, 2018Google Scholar
  16. Cragg GM, Newman DJ (2004) A tale of two tumor targets: topoisomerase I and tubulin. The Wall and Wani contribution to cancer chemotherapy. J Nat Prod 67(2):232–244CrossRefPubMedGoogle Scholar
  17. Dandapani S, Rosse G, Southall N, Salvino JM, Thomas CJ (2012) Selecting, acquiring, and using small molecule libraries for high-throughput screening. Curr Protoc Chem Biol 4:177–191. Scholar
  18. Demain AL, Vaishnav P (2011) Natural products for cancer chemotherapy. J Microbial Biotechnol 4(6):687–699CrossRefGoogle Scholar
  19. Dickson M, Gagnon JP (2004) Key factors in the rising cost of new drug discovery and development. Nat Rev Drug Discov 3(5):417–429CrossRefPubMedGoogle Scholar
  20. Do QT, Bernard P (2004) Pharmacognosy and reverse pharmacognosy: a new concept for accelerating natural drug discovery. IDrugs 7(11):1017–1027PubMedGoogle Scholar
  21. de-Faria FM et al (2012) Mechanisms of action underlying the gastric antiulcer activity of the Rhizophora mangle L. J Ethnopharmacol 139(1):234–243CrossRefPubMedGoogle Scholar
  22. Farnsworth NR, Soejarto DD (2009) Global importance of medicinal plants. In: Akerele O, Heywood V, Synge H (eds) Conservation of medicinal plants, 1st edn. Cambridge University Press, Cambridge, pp 25–52Google Scholar
  23. Frantz S (2005) 2004 approvals: the demise of the blockbuster? Nat Rev Drug Discov 4(2):93–94CrossRefPubMedGoogle Scholar
  24. Frantz S, Smith A (2003) New drug approvals for 2002. Nat Rev Drug Discov 2(2):95–96CrossRefPubMedGoogle Scholar
  25. Ganesan A (2004) Natural products as a hunting ground for combinatorial chemistry. Curr Opin Biotechnol 15(6):584–590CrossRefPubMedGoogle Scholar
  26. Gaudêncio SP, Pereira F (2015) Dereplication: racing to speed up the natural products discovery process. Nat Prod Rep 32:779–810. Scholar
  27. Giri C et al (2011) Status and distribution of mangrove forests of the world using earth observation satellite data. Glob Ecol Biogeogr 20(1):154–159CrossRefGoogle Scholar
  28. Graul AI (2001) The year’s new drugs. Drug News Perspect 14(1):12–31PubMedGoogle Scholar
  29. Grynkiewicz G, Achmatowicz O, Pucko W (2000) Bioactive isoflavone—genistein; synthesis and prospective applications. Herba Polon 46:151–160Google Scholar
  30. Guo Z (2017) The modification of natural products for medical use. Acta Pharm Sin B 7(2):119–136CrossRefPubMedGoogle Scholar
  31. Gurudeeban S et al (2012) Antidiabetic effect of a black mangrove species Aegiceras corniculatum in alloxan-induced diabetic rats. J Adv Pharm Technol Res 3(1):52–56PubMedPubMedCentralGoogle Scholar
  32. Harvey AL (2008) Natural products in drug discovery. Drug Discov Today 13:894–901CrossRefPubMedGoogle Scholar
  33. Hassig CA et al (2014) Ultra-high-throughput screening of natural product extracts to identify proapoptotic inhibitors of Bcl-2 family proteins. J Biomol Screen 19(8):1201–1211CrossRefPubMedPubMedCentralGoogle Scholar
  34. Hughes JP, Rees S, Kalindjian SB, Philpott KL (2011) Principles of early drug discovery. Br J Pharmacol 162:1239–1249CrossRefPubMedPubMedCentralGoogle Scholar
  35. Islam MA et al (2012) Antinociceptive activity of methanolic extract of Acanthus ilicifolius Linn leaves. Turk J Pharm Sci 9(1):51–60Google Scholar
  36. Juyal D, Thawani V, Thaledi S, Joshi M (2014) Ethnomedical properties of Taxus wallichiana Zucc. (Himalayan Yew). J Tradit Complement Med 4(3):159–161CrossRefPubMedPubMedCentralGoogle Scholar
  37. Katiyar C, Gupta A, Kanjilal S, Katiyar S (2012) Drug discovery from plant sources: an integrated approach. Ayu 33(1):10–19CrossRefPubMedPubMedCentralGoogle Scholar
  38. Kazanietz MG (2005) Targeting protein kinase C and “non-kinase” phorbol ester receptors: emerging concepts and therapeutic implications. Biochim Biophys Acta 1754:296CrossRefPubMedGoogle Scholar
  39. Koehn FE, Carter GT (2005) The evolving role of natural products in drug discovery. Nat Rev Drug Discov 4(3):206–220CrossRefPubMedGoogle Scholar
  40. Kramer R, Cohen D (2004) Functional genomics to new drug targets. Nat Rev Drug Discov 3(11):965–972CrossRefPubMedGoogle Scholar
  41. Li JW, Vederas JC (2009) Drug discovery and natural products: end of an era or an endless frontier? Science 325(5937):161–165CrossRefPubMedGoogle Scholar
  42. Liem AF, Holle E, Gemnafle IY, Wakum DS (2013) Isolasi Senyawa Saponin dari Mangrove Tanjang (Bruguiera gymnorrhiza) dan Pemanfaatannya sebagai Pestisida Nabati pada Larva Nyamuk. Jurnal Biologi Papua 5(1):29–36Google Scholar
  43. Liu Z (2008) Preparation of botanical samples for biomedical research. Endocr Metab Immune Disord Drug Targets 8(2):112–121CrossRefPubMedPubMedCentralGoogle Scholar
  44. Lotsch J, Geisslinger G (2001) Morphine-6-glucuronide: an analgesic of the future? Clin Pharmacokinet 40(7):485–499CrossRefPubMedGoogle Scholar
  45. Mann J (2000) Murder, magic and medicine, 2nd edn. Oxford University Press, OxfordGoogle Scholar
  46. Mayorga P, Pérez KR, Cruz SM, Cáceres A (2010) Comparison of bioassays using the anostracean crustaceans Artemia salina and Thamnocephalus platyurus for plant extract toxicity screening. Rev Bras Farmacogn 20:897–903CrossRefGoogle Scholar
  47. Mittermeier RA, Gil PR, Hoffman M, Pilgrim J, Brooks T, Mittermeier CG, Lamoreux J, da Fonseca GAB, Seligmann PA, Ford H (2005) Hotspots revisited: earth’s biologically richest and most endangered terrestrial ecoregions. Conservation International, New YorkGoogle Scholar
  48. Mouafi FE et al (2014) Phytochemical analysis and antibacterial activity of mangrove leaves (Avicenna marina and Rhizophora stylosa) against some pathogens. World Appl Sci J 29(4):547–554Google Scholar
  49. Newman DJ, Cragg GM (2012) Natural products as sources of new drugs over the 30 years from 1981 to 2010. J Nat Prod 75(3):311–335CrossRefPubMedPubMedCentralGoogle Scholar
  50. Newman DJ, Cragg GM, Sneader KM (2000) The influence of natural products upon drug discovery. Nat Prod Rep 17(3):215–234CrossRefPubMedGoogle Scholar
  51. Newman DJ, Cragg GM, Snader KM (2003) Natural products as sources of new drugs over the period 1981–2002. J Nat Prod 66(7):1022–1037CrossRefPubMedGoogle Scholar
  52. Ochoa-Villarreal M, Howat S, Hong SM, Jang MO, Jin YW, Lee EK, Loake GJ (2016) Plant cell culture strategies for the production of natural products. BMB Rep 49(3):149–158CrossRefPubMedPubMedCentralGoogle Scholar
  53. Okouneva T, Hill BT, Wilson L, Jordan MA (2003) The effects of vinflunine, vinorelbine, and vinblastine on centromere dynamics. Mol Cancer Ther 2(5):427–436PubMedGoogle Scholar
  54. Pereira DA, Williams JA (2007) Origin and evolution of high throughput screening. Br J Pharmacol 152(1):53–61CrossRefPubMedPubMedCentralGoogle Scholar
  55. Pirttila T, Wilcock G, Truyen L, Damaraju CV (2004) Long-term efficacy and safety of galantamine in patients with mild-to-moderate Alzheimer’s disease: multicenter trial. Eur J Neurol 11(11):734–741CrossRefPubMedGoogle Scholar
  56. Quinn RJ (2012) Basics and principles for building natural product-based libraries for HTS. In: Haian F (ed) Chemical genomics. Cambridge University Press, CambridgeGoogle Scholar
  57. Rege AA, Chowdhary AS (2013) Evaluation of mangrove plants as putative HIV-protease inhibitors. Indian Drugs 50(7):41Google Scholar
  58. Rohaeti, E et al. (2010) Potensi Ekstrak Rhizophora sp. Sebagai inhibitor tirosinase. Prosiding Semnas Sains III. IPB, Bogor, 13 November, pp 196–201Google Scholar
  59. Roy A, McDonald PR, Sittampalam S, Chaguturu R (2010) Open access high throughput drug discovery in the public domain: a Mount Everest in the making. Curr Pharm Biotechnol 11(7):764–778CrossRefPubMedPubMedCentralGoogle Scholar
  60. Royal Botanical Garden Report (2017) State of the world’s plants. Royal Botanic Gardens, KewGoogle Scholar
  61. Safari VZ et al (2016) Antipyretic, antiinflammatory and antinociceptive activities of aqueous bark extract of Acacia nilotica (L.) Delile in albino mice. J Pain Manag Med 2:113Google Scholar
  62. Salim AA et al (2008) Drug discovery from plants. In: Ramawat KG, Mérillon JM (eds) Bioactive molecules and medicinal plants. Springer, Berlin. Scholar
  63. Samuelsson G (2004) Drugs of Natural Origin, 5th edn. Apotekarsocieteten, StockholmGoogle Scholar
  64. Schroeder FC, Gronquist M (2006) Extending the scope of NMR spectroscopy with microcoil probes. Angew Chem Int Ed 45(43):7122–7131CrossRefGoogle Scholar
  65. Singh CR, Kathiresan K (2015) Effect of cigarette smoking on human health and promising remedy by mangroves. Asian Pacific Journal of Tropical Biomedicine 5(2):162–167CrossRefGoogle Scholar
  66. Sneader W (2005) Drug discovery: a history. Wiley, ChichesterCrossRefGoogle Scholar
  67. Tambe VD, Bhambar RS (2016) Studies on diuretics and laxative activity of the Hibiscus tiliaceus Linn. bark extracts. Int J PharmTech Res 9(3):305–310Google Scholar
  68. Tan DS (2004) Current progress in natural product-like libraries for discovery screening. Comb Chem High Throughput Screen 7(7):631–643CrossRefPubMedGoogle Scholar
  69. Tanvira P, Seenivasan R (2014) Targeting mangrove species as an alternative for snake bite envenomation therapy with special reference to phospholipase A2 inhibitory activity: a mini review. Res J Pharm Biol Chem Sci 5(2):1724–1731Google Scholar
  70. Walters WP, Namchuk M (2003) Designing screens: how to make your hits a hit. Nat Rev Drug Discov 2:259–266CrossRefPubMedGoogle Scholar
  71. WHO (2005) WHO guidelines for sampling of pharmaceutical products and related materials. WHO Technical Report Series, No. 929Google Scholar
  72. World Health Organization (‎1996) The World health report : 1996 : fighting disease, fostering development / report of the Director-General.폘Geneva : World Health Organization.
  73. Yi XX et al (2015) Four new cyclohexylideneacetonitrile derivatives from the hypocotyl of mangrove (Bruguiera gymnorrhiza). Molecules 20(8):14565–14575CrossRefPubMedGoogle Scholar
  74. Yu D, Suzuki M, Xie L, Morris-Natschke SL, Lee KH (2003) Recent progress in the development of coumarin derivatives as potent anti-HIV agents. Med Res Rev 23(3):322–345CrossRefPubMedGoogle Scholar

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© Springer Nature Switzerland AG 2019

Authors and Affiliations

  1. 1.Department of Biomedical Engineering and Directorate of Academic Research and Community ServicesSwiss German UniversityTangerangIndonesia

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