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of abietic acid induces PPARQ target gene expression in RAW264.7 macrophages and
3T3-L1 adipocytes. These data indicate that abietic acid is a PPARQ ligand and that
its anti-inflammatory effect is partly due to the activation of PPARQ in stimulated
macrophages. The results suggested a novel possibility that abietic acid, a naturally
occurring compound, can be used not only as an anti-inflammatory agant but also
for regulating lipid metabolism and atherosclerosis.
6.5 Development Trends in Biological Research
Despite the rise of combinatorial chemistry as an integral part of the lead discovery
process, natural products still play a major role as starting materials for drug
discovery [68]. A report published in 2007, covering the years 1981-2006, details
the contribution of naturally occurring chemicals in drug development. According
to this report, of the 974 small molecule new chemical entities, 63% were natural
product-derived or semisynthetic derivatives of natural products [2]. Although much
attention has been paid to the biological activity of rosin derivatives, not a single
rosin-based drug is available on the market. Thorough investigation of the biological
activities of rosin derivatives is required.
Terpenoids constitute one of the largest families of natural products, accounting for
more than 40,000 individual compounds. In particular, terpenoids are constituents of
many herbal plants, and several terpenoids are used for pharmaceutical applications,
for example, artemisinin and taxol as malaria and cancer medicines, respectively.
Although there are many advantages to the design and synthesis of drugs from
natural products, there are perceived disadvantages, which include difficulties in
access and supply, complexities of natural product chemistry and the slow progress
of working with natural products. However, many kinds of pure rosin acids can
now be easily separated from rosin or modified rosin, and they can be purified to
the standards required for drug development. Thus, using rosin as a raw material
for drug development is of great advantage because of the large quantity available
and the special stereostructures.
Most biologically active compounds contain heteroatoms. Oxygen and nitrogen
atoms are often present in natural products, and synthetic compounds often contain
sulfur and halogen atoms. Biologically active compounds usually contain a level
of nonaromatic unsaturation. The rigidity and chirality of chemical structures are
both well-established factors in medicinal chemistry which are known to enhance
the specificity of action of compounds and their efficacy as drugs [69]. Rosin acids
have both of these two natural advantages because their structures contain tricyclic
hydrophenanthrene and several chiral centres. Rosin acids have only carbon, hydrogen
and oxygen atoms, and so it has been suggested that active atoms, such as fluorine,
