Journal ArticleDOI
Aphadilactones A–D, Four Diterpenoid Dimers with DGAT Inhibitory and Antimalarial Activities from a Meliaceae Plant
Jia Liu,Xiu-Feng He,Gaihong Wang,Emilio F. Merino,Sheng-Ping Yang,Rongxiu Zhu,Li-She Gan,Hua Zhang,Maria B. Cassera,He-Yao Wang,David G. I. Kingston,Jian-Min Yue +11 more
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TLDR
Aphadilactones A-D (1-4), four diastereoisomers possessing an unprecedented carbon skeleton, were isolated from the Meliaceae plant Aphanamixis grandifolia and showed significant antimalarial activities and the strongest natural DGAT-1 inhibitor discovered to date.Abstract:
Aphadilactones A-D (1-4), four diastereoisomers possessing an unprecedented carbon skeleton, were isolated from the Meliaceae plant Aphanamixis grandifolia. Their challenging structures and absolute configurations were determined by a combination of spectroscopic data, chemical degradation, fragment synthesis, experimental CD spectra, and ECD calculations. Aphadilactone C (3) with the 5S,11S,5'S,11'S configuration showed potent and selective inhibition against the diacylglycerol O-acyltransferase-1 (DGAT-1) enzyme (IC50 = 0.46 ± 0.09 μM, selectivity index > 217) and is the strongest natural DGAT-1 inhibitor discovered to date. In addition, compounds 1-4 showed significant antimalarial activities with IC50 values of 190 ± 60, 1350 ± 150, 170 ± 10, and 120 ± 50 nM, respectively.read more
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Recent applications of the hetero Diels–Alder reaction in the total synthesis of natural products
TL;DR: In this article, the scope and preparative synthetic applications of the hetero Diels-Alder (HDA) reaction are discussed, as a key step in the total synthesis of natural products.
Journal ArticleDOI
Antiplasmodial natural products: an update
TL;DR: Several natural products with potential for blocking the transmission of malaria have the potential to be developed into viable anti-malarial drugs and could play a role in malaria eradication by targeting gametocytes.
Journal ArticleDOI
Nanomolar Antimalarial Agents against Chloroquine-Resistant Plasmodium falciparum from Medicinal Plants and Their Structure-Activity Relationships.
Bin Zhou,Yan Wu,Seema Dalal,Emilio F. Merino,Qun-Fang Liu,Cheng-Hui Xu,Tao Yuan,Jian Ding,David G. I. Kingston,Maria B. Cassera,Jian-Min Yue +10 more
TL;DR: A comprehensive structure-activity relationship study indicated that three functional groups are essential and two motifs can be modified in sesquiterpenoids, which is comparable to the potency of artemisinin.
Journal ArticleDOI
Fortunoids A–C, Three Sesquiterpenoid Dimers with Different Carbon Skeletons from Chloranthus fortunei
TL;DR: Three dimeric sesquiterpenoids (1-3), fortunoid A possessing a new carbon skeleton of rearranged lindenane dimer and fortunoids B (2) and C (3) representing the first example of the dimers of a lINDenane and a eudesmane sesQUiterpene, were isolated from Chloranthus fortunei.
Journal ArticleDOI
Euphorbesulins A-P, Structurally Diverse Diterpenoids from Euphorbia esula.
TL;DR: Aqueous ethanol extracts of powdered twigs of Euphorbia esula afforded 16 new diterpenoids, named euphorbesulins A-P, which represent a rare type of presegetane diter penoid and low nanomolar antimalarial activity.
References
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Catalytic Asymmetric Dihydroxylation
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Identification of a gene encoding an acyl CoA:diacylglycerol acyltransferase, a key enzyme in triacylglycerol synthesis
Sylvaine Cases,Steven J. Smith,Yaowu Zheng,Heather M. Myers,Steven R. Lear,Eric Sande,Sabine Novak,Colin Collins,Carrie B. Welch,Aldons J. Lusis,Sandra K. Erickson,Robert V. Farese +11 more
TL;DR: An expressed sequence tag clone that shared regions of similarity with acyl CoA:cholesterol acyltransferase, an enzyme that also uses fatty acyl coA as a substrate was identified, which will greatly facilitate studies of cellular glycerolipid metabolism and its regulation.
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Simple and Inexpensive Fluorescence-Based Technique for High-Throughput Antimalarial Drug Screening
TL;DR: A side-by-side comparison of this new fluorescence assay and a standard radioisotopic method suggest that it may be an ideal method for high-throughput antimalarial drug screening.
Journal ArticleDOI
Thematic review series: glycerolipids. DGAT enzymes and triacylglycerol biosynthesis.
TL;DR: The genes encoding two DGAT enzymes, DGAT1 and DGAT2, were identified in the past decade, and the use of molecular tools, including mice deficient in either enzyme, has shed light on their functions.
Journal ArticleDOI
Cloning of DGAT2, a Second Mammalian Diacylglycerol Acyltransferase, and Related Family Members
Sylvaine Cases,S. Stone,Ping Zhou,Eric Yen,Bryan Tow,Kathryn D. Lardizabal,Toni Voelker,Robert V. Farese +7 more
TL;DR: A second mammalian DGAT, DGAT2, is cloned and characterized, which was identified by its homology to a DGAT in the fungus Mortierella rammaniana, suggesting that it may play a significant role in mammalian triglyceride metabolism.