Biodiversity and natural product drug discovery

Mahidol, Chulabhom; Ruchirawat, Somsak; Prawat, Hunsa; Pisutjaroenpong, S.; Engprasert, Surang; Chumsri, Phannipha; Tengchaisri, T; Sirisinha, Stitaya; Picha, P.

doi:10.1351/pac199870112065

Cited by 43 publications

(19 citation statements)

References 2 publications

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“…Natural products have a long history of medicinal use in both traditional and modern societies, and have been utilized as herbal remedies, purified compounds, and as starting materials for combinatorial chemistry. Terrestrial flora and fauna, marine organisms, bacteria, fungi, and other microbes, provide a chemically diverse array of compounds not available through current synthetic chemistry techniques [e.g., [91][92][93][94][95][96][97][98][99][100]. Natural products that have been used traditionally for nutritional or medicinal purposes (for example, botanical dietary supplements and ethnobotanically utilized species) may also provide AIs with reduced side effects.…”

Section: Natural Products As Aromatase Inhibitorsmentioning

confidence: 99%

Natural Products as Aromatase Inhibitors

Balunas¹,

Su²,

Brueggemeier³

et al. 2008

ACAMC

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With the clinical success of several synthetic aromatase inhibitors (AIs) in the treatment of postmenopausal estrogen receptor-positive breast cancer, researchers have also been investigating also the potential of natural products as AIs. Natural products from terrestrial and marine organisms provide a chemically diverse array of compounds not always available through current synthetic chemistry techniques. Natural products that have been used traditionally for nutritional or medicinal purposes (e.g., botanical dietary supplements) may also afford AIs with reduced side effects. A thorough review of the literature regarding natural product extracts and secondary metabolites of plant, microbial, and marine origin that have been shown to exhibit aromatase inhibitory activity is presented herein. Keywordsaromatase inhibitors; natural products; breast cancer; botanical dietary supplements BREAST CANCERWorldwide breast cancer estimates included over one million incident cases and almost 400,000 deaths in the year 2000 [1,2]. In the United States, over 178,000 women were expected to be diagnosed with breast cancer in 2007 with over 40,000 deaths occurring from the disease [3]. In developed countries, mortality from breast cancer has recently begun to decline, primarily due to earlier detection and improved treatments [4,5]. Breast cancer is thought to be a result of inherited genetic predisposition (e.g., mutations in genes such as BRCA-1, p53, PTEN/MMAC1, and/or ATM) and/or environmental factors (e.g., radiation exposure, dietary factors, alcohol consumption, hormonal exposure) [2,6,7]. Numerous genetic mutations are necessary for breast cancer development and progression including the acquisition of the capabilities for self-sufficiency in growth signals, insensitivity to anti-growth signals, evasion of apoptosis, limitless replicative potential, sustained angiogenesis, and tissue invasion and metastasis, known collectively as the "hallmarks of cancer" [8].Numerous molecular targets have been identified as playing a significant role in breast cancer development and progression. Estrogens and the estrogen receptors (ERs) are widely NIH Public Access Author ManuscriptAnticancer Agents Med Chem. Author manuscript; available in PMC 2011 April 12.Published in final edited form as:Anticancer Agents Med Chem. 2008 August ; 8(6): 646-682. NIH-PA Author ManuscriptNIH-PA Author Manuscript NIH-PA Author Manuscript recognized to play an important role in the development and progression of breast cancer, making estrogens and the ERs widely studied molecular targets [9][10][11][12]. Two of the endogenous estrogens found in humans include estradiol and estrone. In pre-menopausal women, estrogens are produced primarily through conversion of androgens in the ovaries while estrogen production in postmenopausal women occurs in only peripheral tissues [13,14]. Estrogens have various effects throughout the body, including positive effects on the brain, bone, heart, liver, and vagina, with negative effects such as increased risk...

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Section: Natural Products As Aromatase Inhibitorsmentioning

confidence: 99%

Natural Products as Aromatase Inhibitors

Balunas¹,

Su²,

Brueggemeier³

et al. 2008

ACAMC

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“…For certain therapy areas, such as antimicrobials, anticancer antihypertensive and anti-inflammatory drugs, the number was even higher the most of all approved small molecule new chemical entities were derived from nature. The latter is also recognized as important source of biodiversity [8].…”

Section: Nature As Source Of New Drug Compoundsmentioning

confidence: 99%

“…It is considered that because of the structural and biological diversity of their constituents, terrestrial plants offer a unique and renewable resource for the discovering of potential new drugs and biological entities [1,8].…”

Section: The Successful Of Natural Products In Drug Discoverymentioning

confidence: 99%

The Success of Natural Products in Drug Discovery

Lahlou¹

2013

460

262

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Drug discovery leading to robust and viable lead candidates' remains a challenging scientific task, which is the transition from a screening hit to a drug candidate, requires expertise and experience. Natural products and their derivatives have been recognized for many years as a source of therapeutic agents and of structural diversity. However, in addition to their chemical structure diversity and their biodiversity, the development of new technologies has revolutionized the screening of natural products in discovering new drugs. Applying these technologies compensates for the inherent limitations of natural products and offers a unique opportunity to re-establish natural products as a major source for drug discovery. The present article attempts to describe the utilization of compounds derived from natural resources as drug candidates, with a focus on the success of these resources in the process of finding and discovering new and effective drug compounds, an approach commonly referred to as "natural product drug discovery".

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“…Given that nearly 50% of known drugs are metabolites or derivatives of metabolites [4], it is likely that our expanded knowledge of metabolites and protein-metabolite interactions will lead to the discovery of many new drug leads -either through computational methods or standard metabolite screening approaches [19].…”

Section: What Does the Future Hold?mentioning

confidence: 99%

“…• Over 95% of all diagnostic clinical assays test for small molecules [3] • 89% of known drugs are small molecules [102] • 50% of all drugs are derived from pre-existing metabolites [4] • 30% of identified genetic disorders involve diseases of small-molecule metabolism [5] Furthermore, almost all of the leading (and most costly) causes of chronic disease and morbidity arise from adverse interaction of small molecules with our genome or proteome [6][7][8]. These include obesity (dietary sugars or fats), diabetes (dietary sugars), heart disease (dietary fats and cholesterol), cancer (pollutants or mutagens) and adverse drug reactions (drugs or drug metabolites).…”

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confidence: 99%