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Lichens are a symbiotic association of algae and fungus, belonging to the family Parmeliaceae. Some lichen species are edible and used as an active ingredient for preparation of exotic spices as well as folklore medicine to cure different kinds of ailments. A specimen of lichen was collected from Munner in the Kerala State of South India for chemical profiling. Chemical analyses of the diethyl ether extract of the defatted lichen led to the isolation of six phenols 1-6 with variation of relative abundance. Amongst them, the relative abundance of compound 3 was the greatest (1 % of crude extract) and it was identified as atranorin. The structures of known compounds were confirmed by comparison of their 1 H-NMR, 13 C NMR, and mass data with published values available in the literature. In vitro bioassay for anti-proliferative activity of these compounds has been conducted against various human cancer cell lines in comparison with paclitaxel as control using SRB assay. Interestingly, a new compound 5 was found along with previously reported compounds from this lichen. This new compound was designated as fluoroatranorin 5 which was reported for the first time herein. The structural characterization of a new depside was determined by spectral methods such as 1 H-NMR, 13 C NMR, 19 F NMR, IR, LC-HRESI-MS, and LC-MS/MS study. Its structure was confirmed by single crystal X-ray diffraction study. This new compound was designated as fluoroatranorin 5 which was reported first time herein. Anti-proliferative activity of all these compounds was evaluated against six different cancer cell lines. The inhibitory activity, IC 50 value of compounds 1-3 and 5 exhibited at 99.64, 102.04, 109.20, 53.0 and 2.4 μM on cancer cell lines HT-29 (colon), Hela (cervical), HT-29, HPAC (pancreas) and A2780 (ovarian cancer cell line) respectively in comparison with paclitaxel as control. The new compound 5 exhibited significant activity with IC 50 value 2.4 μM on A2780 ovarian cancer cell line., (© 2024 Wiley-VHCA AG, Zurich, Switzerland.)

Covering up to early 2023The present review summarizes recent accomplishments made as part of a multidisciplinary, multi-institutional anticancer drug discovery project, wherein samples comprising higher plants were collected primarily from Southeast Asia, and also from Central America, and the West Indies. In the introductory paragraphs, a short perspective is provided on the current importance of plants in the discovery of cancer therapeutic agents, and the contributions of other groups working towards this objective are mentioned. For our own investigations, following their collection, tropical plants have been subjected to solvent extraction and biological evaluation for their antitumor potential. Several examples of purified plant lead bioactive compounds were obtained and characterized, and found to exhibit diverse structures, including those of the alkaloid, cardiac glycoside, coumarin, cucurbitacin, cyclobenzofuran (rocaglate), flavonoid, lignan, and terpenoid types. In order to maximize the efficiency of work on drug discovery from tropical plant species, strategies to optimize various research components have been developed, including those for the plant collections and taxonomic identification, in accordance with the requirements of contemporary international treaties and with a focus on species conservation. A major component of this aspect of the work is the development of collaborative research agreements with representatives of the source countries of tropical rainforest plants. The phytochemical aspects have included the preparation of plant extracts for initial screening and the selection of promising extracts for activity-guided fractionation. In an attempt to facilitate this process, a TOCSY-based NMR procedure has been applied for the determination of bioactive rocaglate derivatives in samples of Aglaia species (Meliaceae) collected for the project. Preliminary in vitro and in vivo mechanistic studies carried out by the authors are described for two tropical plant-derived bioactive lead compounds, corchorusoside C and (+)-betulin, including work conducted with a zebrafish ( Danio rerio ) model. In the concluding remarks, a number of lessons are summarized that our group has learned as a result of working on anticancer drug discovery using tropical plants, which we hope will be of interest to future workers.

Based on their current wide bioavailability, botanical dietary supplements have become an important component of the United States healthcare system, although most of these products have limited scientific evidence for their use. The most recent American Botanical Council Market Report estimated for 2020 a 17.3% increase in sales of these products when compared to 2019, for a total sales volume of $11,261 billion. The use of botanical dietary supplements products in the United States is guided by the Dietary Supplement Health and Education Act (DSHEA) from 1994, enacted by the U.S. Congress with the aim of providing more information to consumers and to facilitate access to a larger number of botanical dietary supplements available on the market than previously. Botanical dietary supplements may be formulated for and use only using crude plant samples (e.g., plant parts such as the bark, leaves, or roots) that can be processed by grinding into a dried powder. Plant parts can also be extracted with hot water to form an "herbal tea." Other preparations of botanical dietary supplements include capsules, essential oils, gummies, powders, tablets, and tinctures. Overall, botanical dietary supplements contain bioactive secondary metabolites with diverse chemotypes that typically are found at low concentration levels. These bioactive constituents usually occur in combination with inactive molecules that may induce synergy and potentiation of the effects observed when botanical dietary supplements are taken in their different forms. Most of the botanical dietary supplements available on the U.S. market have been used previously as herbal remedies or as part of traditional medicine systems from around the world. Their prior use in these systems also provides a certain level of assurance in regard to lower toxicity levels. This chapter will focus on the importance and diversity of the chemical features of bioactive secondary metabolites found in botanical dietary supplements that are responsible for their applications. Many of the active principles of botanical dietary substances are phenolics and isoprenoids, but glycosides and some alkaloids are also present. Biological studies on the active constituents of selected botanical dietary supplements will be discussed. Thus, the present chapter should be of interest for both members of the natural products scientific community, who may be performing development studies of the products available, as well as for healthcare professionals who are directly involved in the analysis of botanical interactions and evaluation of the suitability of botanical dietary supplements for human consumption., (© 2023. The Author(s), under exclusive license to Springer Nature Switzerland AG.)

The present study aims to continue the study of corchorusoside C ( 1 ), a cardenolide isolated from Streptocaulon juventas , as a potential anticancer agent. A mechanistic study was pursued in a zebrafish model and in DU-145 prostate cancer cells to investigate the selectivity of 1 towards NF-κB and PARP-1 pathway elements. Compound 1 was found to inhibit the expression of IKKα and NF-κB p65 in TNF-α induced zebrafish and inhibit the expression of NIK in vitro. The protein expression levels of XRCC-1 were increased and p53 decreased in DU-145 cells. XIAP protein expression was initially decreased after treatment with 1 , followed by an increase in expression at doses higher than the IC 50 value. The activity of caspase-1 and the protein expression levels of IL-18 were both decreased following treatment of 1 . The binding interactions for 1 to NIK, XRCC-1, p53, XIAP, and caspase-1 proteins were explored in molecular docking studies. Additionally, the toxicity profile of 1 in zebrafish was favorable in comparison to its analog digoxin and other anticancer drugs at the same MTD in zebrafish. Overall, 1 targets the noncanconical NF-κB pathway in vivo and in vitro, and is well tolerated in zebrafish supporting its potential in the treatment of prostate cancer., Competing Interests: The authors declare that there are no conflict of interest.