Rapeepat Sangsuwan, Jasper H.N. Yik, Matthew Owen, Gang-YuLiu, Dominik R. Haudenschild, and Jamal S. Lewis* September 2022 Shortened author list: Rapeepat Sangsuwan, … and Jamal S. Lewis*
The attained natural products and their analogs have been evaluated for their anticancer, antioxidant, antimicrobial, and anti-inflammatory activities, among others. With an emphasis on anticancer activity, more mechanistic understanding at the molecular level such as antiproliferation, cell cycle arrest, apoptotic induction, and cancer-related inflammation, more efficacious drug candidates can be designed and evaluated. For example, vernodalin, vernolepin, and vernolide, the natural sesquiterpene lactones from Gymnanthemum extensum or Pim Pailin, as well as uvamicranin B and uvarigrin from Uvaria micrantha induce apoptosis by inhibiting mitosis of HepG2 at the G2/M phase; this has led to further development of other sesquiterpene lactones and acetogenins as efficacious anticancer agents. While direct biological evaluations provide the needed information on the potential utility of natural products, low natural abundance has been a severe limiting factor for a more comprehensive evaluation and medicinal applications. The advent of computational software has enabled virtual visualization of interactions between the biomolecular protein targets and the natural products. Through molecular docking, the process of biological studies has become more cost-effective; cost of high-throughput screening of otherwise greater number of compounds can be significantly lowered. More importantly, compound specificity against target of interest can be realized. To this end, libraries of over 1,000 structurally diverse natural products and their analogs available from CRI laboratories have been accumulated...
By employing appropriate modern organic methods, some natural products isolable in sufficiently large quantity have served as starting materials for subsequent direct structural modifications to attain higher bioactivity. Alternatively, they can provide access to other natural products with low natural abundance; this may be natural congeners or some other natural products which can undergo sequences of transformations to the desired compounds. As a result, this value-added approach facilitates the use of one natural product to gain access to others which are less accessible naturally or even serve as starting materials for total synthesis of otherwise structurally complex molecules more efficiently. Using this approach, semi-synthetic analogs of lycopodium alkaloids, flavonoids, and triterpenoids from ferns and lycophytes have been successfully prepared. Similarly, anticopalic acid from Kaempferia elegans, or Prao Pah, pterocarpan along with isoflavone from Butea superba Roxb., or Kwaw Kreu Daeng, and malabaricol from Ailanthus triphysa, or Ma Yom Pah, have also been structurally modified successfully. Anticopalic acid, in particular, which is more naturally abundant, has served as a starting material for the preparation of other naturally-occurring structurally diverse natural terpenoids with more potent biological activities such as habiterpenol.
Plants have served as major sources of structurally diverse and complex natural products unmatched even by the most imaginative minds. While many have received attention for their medicinal use, chemotaxonomic research on a plethora of genera and species remain largely quiescent; that is, a still relatively vast number of natural products await discovery. Thailand, with its tropical location and climate, has been endowed with a wealth of natural resources and abundant biodiversity. On the basis of folk medicinal wisdom, which has utilized local herbs as medicine for centuries, our laboratory has embarked on systematic chemotaxonomic approach for chemical constituents of these herbs spanning from GPS-recorded sample collection, modern and greener isolation process, bioassay-guided fractionation, compound identification, and biological evaluations. Such approach has led to natural products with unprecedented framework while also linking the folk wisdom and the chemical knowledge of bioactive constituents from locally used medicinal plant extracts. Some herbal plants have also been investigated following their bioassay-guided fractionation to yield pure compounds. Triterpenes from Drypetes hoaensis, known locally as Lhong-Lai, exhibit potent cytotoxicity against hepatocarcinoma HepG2.Cardinane sesquiterpenes fromAlangium salviifolium, also known asProoh, and prenylated acridones fromAtalantia monophylla, or Manow Peeh, are aromatase inhibitors which can lower estrogen in some breast cancer patients. Anti-oxidant and cytotoxic flavonoidtrans-stilbenes were isolated and characterized fromMacaranga siamensis, or Tao Siam. Currently, our laboratory...
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