Natural products frequently display a range of biological activities, yet many exhibit only moderate efficacy during initial evaluations. Often, these natural substances necessitate structural alterations to yield promising lead compounds. Chalcones, characterized by their β-unsaturated carbonyl aromatic ketone structure, are prevalent in plant life and serve as fundamental scaffolds for the biosynthetic precursors of flavonoids and isoflavones.
View Article and Find Full Text PDFPseudolaric Acid B (PAB), a natural product with remarkable anti-tumor activity, is a starting point for new anticancer therapeutics. We designed and synthesized 27 PAB derivatives and evaluated their anti-proliferative activities against four cancer cell lines: MCF-7, HCT-116, HepG2, and A549. Compared with unmodified PAB, the PAB derivatives showed stronger anti-proliferative activity.
View Article and Find Full Text PDFBackground: Cerebral blood flow and vascular structures serve as the fundamental components of brain metabolism and circulation. Acupuncture, an alternative and complementary medical approach, has demonstrated efficacy in treating cerebral ischemic stroke (CIS). Nevertheless, the mechanisms underlying the impact of acupuncture on vascular smooth muscle cell (VSMC) function remain uncertain.
View Article and Find Full Text PDFIndole is a heterocyclic compound formed by the fusion of a benzene ring and pyrrole ring, which has rich biological activity. Many indole-containing compounds have been sold on the market due to their excellent pharmacological activity. For example, vincristine and reserpine have been widely used in clinical practice.
View Article and Find Full Text PDFBioorg Med Chem Lett
December 2020
In light of the adequate sources for Hylotelephium erythrostictum, its active components have aroused research interest. 2-(3',4'-dihydroxyphenyl)-2,3-dihydro-4,6-dihydroxy-2-(methoxy)- 3-benzofuranone(1), apigenin(2), diosmetin(3), kaempferol(4), kaempferide(5), rhamnocitrin(6), quercetin(7), and gallic acid(8) were isolated from H. erythrostictum.
View Article and Find Full Text PDFIn an attempt to search for more potent positive inotropic agents, two series of [1,2,4]triazolo[4,3-] quinoxaline derivatives bearing substituted benzylpiperazine and benzoylpiperazine moieties were synthesized and their positive inotropic activities evaluated by measuring left atrial stroke volume in isolated rabbit heart preparations. Several compounds showed favorable activities compared with the standard drug, milrinone. Compound was the most potent agent, with an increased stroke volume of 12.
View Article and Find Full Text PDFSqualene synthase (SQS) is a key enzyme in plant terpenoid biosynthetic pathway. This study focused on cloning and analysis of Huperzia serrata SQS (HsSQS1) gene. After searching the transcriptome dataset of H serrata, one unique sequence encoding SQS was discovered.
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