Publications by authors named "A Douglas Kinghorn"

448 Publications

Spermidine alkaloid and glycosidic constituents of Vietnamese .

Phytochem Lett 2021 Jun 15;43:154-162. Epub 2021 Apr 15.

Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.

Phytochemical investigation of the aerial parts of led to the isolation of secondary metabolites belonging to the spermidine alkaloid, glycoside, depsidone and phenol classes. Of the eleven secondary metabolites isolated in this study, two spermidine alkaloids, dovyalicins H () and I (), which belong to a rare group among this class, and six glycosides () are previously undescribed. The structures of all new isolates were determined by interpretation of spectroscopic and spectrometric data. In this report, the structural elucidation of these unprecedented secondary metabolites () is described.
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http://dx.doi.org/10.1016/j.phytol.2021.04.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8078847PMC
June 2021

Update on Phytochemical and Biological Studies on Rocaglate Derivatives from Aglaia Species.

Planta Med 2021 Mar 30. Epub 2021 Mar 30.

Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio, United States.

With about 120 species, is one of the largest genera of the plant family Meliaceae (the mahogany plants). It is native to the tropical rainforests of the Indo-Australian region, ranging from India and Sri Lanka eastward to Polynesia and Micronesia. Various species have been investigated since the 1960s for their phytochemical constituents and biological properties, with the cyclopenta[]benzofurans (rocaglates or flavaglines) being of particular interest. Phytochemists, medicinal chemists, and biologists have conducted extensive research in establishing these secondary metabolites as potential lead compounds with antineoplastic and antiviral effects, among others. The varied biological properties of rocaglates can be attributed to their unusual structures and their ability to act as inhibitors of the eukaryotic translation initiation factor 4A (eIF4A), affecting protein translation. The present review provides an update on the recently reported phytochemical constituents of species, focusing on rocaglate derivatives. Furthermore, laboratory work performed on investigating the biological activities of these chemical constituents is also covered.
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http://dx.doi.org/10.1055/a-1401-9562DOI Listing
March 2021

Is it safe yet? Patient readiness and perceptions about returning to hospital for planned orthopaedic care.

Ann R Coll Surg Engl 2021 May 8;103(5):332-336. Epub 2021 Mar 8.

Cardiff and Vale University Health Board, Cardiff, UK.

Introduction: COVID-19 has necessitated significant changes to healthcare delivery but little is known regarding patient opinions of risks compared with benefits. This study investigates patient perceptions concerning attendance for planned orthopaedic surgery during the COVID-19 pandemic.

Materials And Methods: A total of 250 adult patients from the elective orthopaedic waiting list at Cardiff and Vale University Health Board were telephoned during lockdown. They were risk stratified for COVID-19 based on British Orthopaedic Association guidance and a discussion was held to determine patient willingness to proceed with surgery. The primary outcome measure was patients' willingness to proceed.

Results: Of the total number telephoned, 196 patients were included in the study, with a mean age of 57.4 years; 129 patients were willing to attend for surgery, leaving over one-third wishing to cancel or defer. The most frequent reason given for not wishing to attend was fear of contracting COVID-19. There was a statistically significant difference in the willingness to proceed observed with increasing clinical risk (χ(3) = 50.073,  = .000) with almost double the expected count of unwilling to proceed in the high and very high risk groups, equalled by half the expected count in the low risk group.

Discussion: This study illustrates the variable and personal decisions that patients are making about orthopaedic care because of COVID-19. It highlights the need for change to departmental processes regarding recommencement of planned surgical lists. It also reconfirms the importance of regular communication and shared decision making between a well-informed patient and a holistic orthopaedic team.
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http://dx.doi.org/10.1308/rcsann.2020.7025DOI Listing
May 2021

Antitumor potential of the protein phosphatase inhibitor, cantharidin, and selected derivatives.

Bioorg Med Chem 2021 Feb 9;32:116012. Epub 2021 Jan 9.

Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, United States. Electronic address:

Cantharidin is a potent natural protein phosphatase monoterpene anhydride inhibitor secreted by several species of blister beetle, with its demethylated anhydride analogue, (S)-palasonin, occurring as a constituent of the higher plant Butea frondosa. Cantharidin shows both potent protein phosphatase inhibitory and cancer cell cytotoxic activities, but possible preclinical development of this anhydride has been limited thus far by its toxicity. Thus, several synthetic derivatives of cantharidin have been prepared, of which some compounds exhibit improved antitumor potential and may have use as lead compounds. In the present review, the potential antitumor activity, structure-activity relationships, and development of cantharidin-based anticancer drug conjugates are summarized, with protein phosphatase-related and other types of mechanisms of action discussed. Protein phosphatases play a key role in the tumor microenvironment, and thus described herein is also the potential for developing new tumor microenvironment-targeted cancer chemotherapeutic agents, based on cantharidin and its naturally occurring analogues and synthetic derivatives.
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http://dx.doi.org/10.1016/j.bmc.2021.116012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7854516PMC
February 2021

Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.

J Med Chem 2020 12 8;63(24):15410-15448. Epub 2020 Dec 8.

Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States.

Naturally occurring terpenoid lactones and their synthetic derivatives have attracted increasing interest for their promising antitumor activity and potential utilization in the discovery and design of new antitumor agents. In the present perspective article, selected plant-derived five-membered γ-lactones and six-membered δ-lactones that occur with terpenoid scaffolds are reviewed, with their structures, cancer cell line cytotoxicity and in vivo antitumor activity, structure-activity relationships, mechanism of action, and the potential for developing cancer chemotherapeutic agents discussed in each case. The compounds presented include artemisinin (ART, ), parthenolide (PTL, ), thapsigargin (TPG, ), andrographolide (AGL, ), ginkgolide B (GKL B, ), jolkinolide B (JKL B, ), nagilactone E (NGL E, ), triptolide (TPL, ), bruceantin (BRC, ), dichapetalin A (DCT A, ), and limonin (LMN, ), and their naturally occurring analogues and synthetic derivatives. It is hoped that this contribution will be supportive of the future development of additional efficacious anticancer agents derived from natural products.
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http://dx.doi.org/10.1021/acs.jmedchem.0c01449DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7812702PMC
December 2020