Natural Products Chemistry
Natural Products Chemistry
Natural Products Chemistry
ABSTRACT: Long before the era of high through-put screening and genomics, drug discovery
relied heavily on natural products. Drug discovery involves the identification of New Chemical
Entities (NCEs) of potential therapeutic value, which can be obtained through isolation from
natural sources, through chemical synthesis or a combination of both. However, the success
stories for the discoveries Penicillin from penecilium rubens, Paclitaxel yew tree and marketed as
Taxol, Aspirin from Willow bark of Salix alba tree etc. have pave way for scholars in the field of
natural product and organic chemistry to focus their research work in drug-derived from plants
and microorganisms. Natural products derived from these sources are rich in bioactive compound,
which have been use over years throughout human history and evolution as remedies for various
ailments. This paper however, X-rayed the sources and classes of natural products,
pharmaceuticals derived from Natural product, and uses of natural products. The paper also
recommended among others that, government should fund research in the area of natural
products, pharmaceutical chemistry and pharmacognocy.
INTRODUCTION
Sand is a natural product, but we will not cover the chemistry of silica. Natural products of interest
are those organic compounds that contain at a minimum the element carbon. Carbon (chemical
symbol: C) has a valency of 4 and is bound to another carbon either as a single, double, or triple
bond. Carbon is also attached to other elements, such as carbons, hydrogen (H), oxygen (O), and
nitrogen (N); and also sulfurs (S) and phosphorous (P). The various combinations lead to the
bewildering array of natural products structures (Cooper and Nicola, 2015). Starting from the late
19th century there had been much account by scientists and physicians on the antibacterial
properties of the different types of moulds including the mould penicillium but they were unable
to discern what process causing the effect. The effect of mould penicillium was finally being
isolated in 1928 by Scottish scientist Alexander Fleming, in his work that seems to have been
independent of those earlier observations (Greenwood, 2008).
Similarly, recent literature also revealed how drugs were reportedly discovered through the natural
products process due to prevalence of many diseases without suitable medical products available.
Among the various pharmaceutical industrial processes used for drug discovery, the Research and
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Development process is one of the pioneer processes (Cutler, 2000). The meaning of natural
Products has been over the time defined as the naturally occurring compounds that are end products
of primary metabolites; often they are unique compounds for particular organisms (El-Olemyl et
al., 1994). Metabolites are intermediates in metabolic processes in nature and are usually small
molecules. A primary metabolite is directly involved in normal growth, development, and
reproduction, for example, fermentation products (ethanol, acetic acid, citric and lactic acid) and
cell constituents (lipids, vitamins, and polysaccharides). In contrast, secondary metabolite is not
directly involved in those processes and usually has a function but is not that important for the
organism (e.g., antibiotics, pigments, and carotenoids), (Cooper and Nicola, 2015).
Long before the era of high through-put screening and genomics, drug discovery relied heavily
on natural products (Bahl and Bahl, 2006). In fact, many of the drugs available today contain active
ingredients extracted from natural products. Since 1994, nearly half of all drugs were discovered
using natural products (Hamburger and Hostettman, 1991). Furthermore, there were thirteen (13)
new drugs based on natural products that entered the commercial market. These include
ixabepilone, retapamullin, trabectedin, and the peptides exenatide and ziconotide (Sofowora,
1984). Natural product drug discovery continues to play a significant role in the clinical
development of new therapies in the biopharmaceutical industry (Hamburger and Hostettman,
1991).
Natural Product is a chemical compound or substance produced by a living organism that is,
found in nature. In the broadest sense, natural products include any substance produced by life
(Hanson, 2003). Natural products remain the best sources of drugs and drug leads, and this remains
true today despite the fact that many pharmaceutical companies have deemphasized natural
products research in favor of HTP screening of combinatorial libraries during the past 2
decades. From 1940s to date, 131 (74.8%) out of 175 small molecule anticancer drugs are natural
product-based/inspired, with 85 (48.6%) being either natural products or derived there from. From
1981 to date, 79 (80%) out of 99 small molecule anticancer drugs are natural product-
based/inspired, with 53 (53%) being either natural products or derived there from. Among the 20
approved small molecule New Chemical Entities (NCEs) in 2010, a half of them are natural
products (Samuelson, 1999). Drug discovery involves the identification of New Chemical Entities
(NCEs) of potential therapeutic value, which can be obtained through isolation from natural
sources, through chemical synthesis or a combination of both. The field of natural products drug
discovery, despite the success stories of penicillin, paclitaxel, etc., also had aspects that made it
less attractive. In the traditional approach, drug targets were exposed to crude extracts, and in case
of evidence of pharmacological activity the extract was fractionated and the active compound
isolated and identified. This method was slow, labor intensive, inefficient, and provided no
guarantee that a lead from the screening process would be chemically workable or even patentable
(Williams et al., 2002). As natural products usually are molecules with more complex structures,
it was more difficult to extract, purify or synthesize sufficient quantities of a NCEs of interest for
discovery and development activities (Hunter et al., 2008).
Alkaloids (meaning alkali-like) are nitrogenous heterocyclic organic compounds mostly of plant
origin that show significant physiological or toxic effect on humans (El-Olemyl et al., 1994).
Alkaloids are classified based on prominent heterocyclic ring system present in the molecule.
These are:
• Pyridine alkaloids e.g. Nicotine
• Piperidine alkaloids e.g. coniine, piperine
• Quinoline alkaloids e.g. quinine
• Isoquinoline alkaloid e.g. papaverine, morphine
• Indole alkaloids e.g. gramine, strychnine.
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precipitating dietary proteins and digestive enzymes to form complexes not readily digestible
(Zaki, 2000). Other anti-nutritional effects include, damage to the gastrointestinal tract,
interference with the absorption of iron and possibly, a carcinogenic effect. Medicinally, they are
used in the treatment of diarrhea and skin burns (El-Olemyl et al., 1994). Tannins are classified as
hydrolysable tannins (i.e. a mixture of carbohydrates and polyphenols-gallic acid) and condensed
tannins (i.e. complex flavonoid polymers) (Sofowora, 1993).
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The larger structures are assembled from several isoprene units, usually by head-to-tail linked
isoprene units. Terpenes can be cyclic or acyclic, with a large range of structural.
Flavonoids: They are the most abundant polyphenols in human diet, representing about
2/3 of all those ones ingested. Like other phytochemicals, they are the products of secondary
metabolism of plants and, currently, it is not possible to determine precisely their number, even if
over 4000 have been identified. In fruits and vegetables, they are usually found in the form of
glycosides and sometimes as acylglycosides, while acylated, methylated and sulfate molecules are
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less frequent and in lower concentrations. They are water-soluble and accumulate in cell vacuoles
(El-Olemyl et al.,1994: Abdulmuhit et al.,2010:Adzu et al.,2001).
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Natural Product-derived Pharmaceuticals
Natural products constitute a key source of pharmacologically active ingredients in a variety of
novel agents with therapeutic potential in a wide range of diseases. Pharmaceuticals containing
natural products or compounds derived from natural product scaffolds or templates have to
undergo the same stringent approval process as drugs obtained from purely synthetic origin.
Drug: Drug has been define in a myriad ways, Okeye, (2001) define drug as a substance
that could bring about a change in the biological functions through its chemical actions. It is also
considered as a chemical that modifiers of the living tissues that could bring about psychological
and behavioral changes (Olalekan et al, 2014). Moreover, drug is defined as a substance that
modifies perceptions, cognition mood, behavior and general body function (Balogun, 2006).
Comprehensively, drug is any chemical substance, natural or man-made (usually excluding
nutrients, water, or oxygen), that by its chemical nature alters biological structure or functioning
when administered and absorbed (Dewick, 2009). Pharmacology is the discipline that studies drug
effects on living systems (Dewick, 2009).
Classification of Drug
Drugs can be categorized in a number of ways. In the world of medicine and pharmacology, a drug
can be classified by its chemical activity or by the condition that it treats.
Narcotics
Depressants
Stimulants
Hallucinogens
Anabolic steroids
Depressants. Drugs that suppress or slow the activity of the brain and nerves, acting
directly on the central nervous system to create a calming or sedating effect. This category includes
barbiturates (phenobarbital, thiopental, butalbital), benzodiazepines
(alprazolam, diazepam, clonazepam, lorazepam, midazolam), alcohol, and gamma
hydroxybutyrate (GHB). Depressants are taken to relieve anxiety, promote sleep and manage
seizure activity (Dewick, 2009).
Stimulants. Drugs that accelerate the activity of the central nervous system. Stimulants
can make you feel energetic, focused, and alert. This class of drugs can also make you feel edgy,
angry, or paranoid. Stimulants include drugs such as cocaine, crack cocaine, amphetamine,
and methamphetamine. According to the recent World Drug Report published by the United
Nations Office on Drugs and Crime, amphetamine-derived stimulants like ecstasy and
methamphetamine are the most commonly abused drugs around the world
after marijuana (Strobel, 2003).
Hallucinogens. Also known as psychedelics, these drugs act on the central nervous system
to alter your perception of reality, time, and space. Hallucinogens may cause you to hear or see
things that don’t exist or imagine situations that aren’t real. Hallucinogenic drugs include
psilocybin (found in magic mushrooms), lysergic acid diethylamide (LSD), peyote, and
dimethyltryptamine (DMT) (Zaffiri et al., 2012).
Inhalants. These are a broad class of drugs with the shared trait of being
primarily consumed through inhalation. Most of the substances in this class can exist in vapor form
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at room temperature. As many of these substances can be found as household items, inhalants are
frequently abused by children and adolescents. These include substances such as paint, glue, paint
thinners, gasoline, marker or pen ink, and others. Though ultimately all of these substances cross
through the lungs into the bloodstream, their precise method of abuse may vary but can include
sniffing, spraying, huffing, bagging, and inhaling, among other delivery routes (Zaffiri et al.,
2012).
Cannabis. Cannabis is a plant-derived drug that is the most commonly used illicit drug
worldwide. It acts through the cannabinoid receptors in the brain. Cannabis is abused in various
forms including bhang, ganja, charas, and hashish oil. (Strobel, 2003).
CONCLUSION/RECOMMENDATION
Compounds isolated from nature have long been known to possess biological profiles and
pharmaceutical potential far greater than anything made by man. However, natural products are
notoriously cumbersome to isolate and very challenging to synthesize. Natural products have
played a central role in advancing synthetic and biosynthetic chemistry, medicine, and our
understanding of nature. The training of chemists and pharmacognocists in the area of microscale
chromatographic purification and spectroscopy is ever increasing to tackle the challenging
questions in bioorganic chemistry and molecular biology. To this end the authors recommended
that, federal and state government should fund research in the area of natural products chemistry,
organic chemistry and biochemistry. Similarly, Nigerian universities in collaboration Non-
governmental Organizations NGOs such as WHO to open centre for research in drugs derived
from natural products.
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