The cytotoxicity of three alkaloids from the roots of Aconitum yesoense var. macroyesoense as well as 36 semi-synthetic C(20)-diterpenoid atisine-type alkaloid derivatives against A549 human lung carcinoma cells was examined. Ten acylated alkaloid derivatives, pseudokobusine 11-veratroate (9), 11-anisoate (12), 6,11-dianisoate (14), 11-p-nitrobenzoate (18), 11,15-di-p-nitrobenzoate (22), 11-cinnamate (25) and 11-m-trifluoromethylbenzoate (27), and kobusine 11-p-trifluoromethylbenzoate (35), 11-m-trifluoromethylbenzoate (36) and 11,15-di-p-nitrobenzoate (39), exhibited cytotoxic activity, and 11,15-dianisoylpseudokobusine (16) was found to be the most potent cytotoxic agent. Their IC(50) values against A549 cells ranged from 1.72 to 5.44 μM. In the occurrence of cytotoxic effects of atisine-type alkaloids, replacement by an acyl group at both C-11 and C-15 resulted in the enhancement of activity of the parent alkaloids compared to that from having hydroxy groups at this position, and the presence of a hydroxy group at the C-6 position was required for the cytotoxic effects. These acylated alkaloid derivatives inhibit cell growth through G1 arrest.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2999725 | PMC |
| http://dx.doi.org/10.1007/s11418-010-0452-3 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Optimization of the extraction methods and evaluation of the hypoglycemic effect of extracts on artificially induced diabetic mice.
Heliyon
January 2025
Department of Chemical Engineering, Bangladesh University of Engineering and Technology, Dhaka, 1000, Bangladesh.
Synthetic antidiabetic drugs are often associated with various adverse side effects, including hypoglycemia, nausea, gastrointestinal disturbances, headaches, and even liver damage. In contrast, plant-derived natural antidiabetic bioactive compounds typically exhibit lower toxicity and fewer side effects and have been reported to aid effectively in diabetes management. These plant extracts regulate diabetes by restoring pancreatic function, enhancing insulin secretion, inhibiting intestinal glucose absorption, and facilitating insulin dependent metabolism.
View Article and Find Full Text PDFStrawberry plant growth enhancement: Effects of artificial light and methyl jasmonate-salicylic acid treatments on physiology and metabolism.
Heliyon
January 2025
Department of Agronomy and Horticulture, Faculty of Agriculture, IPB University, Bogor, Indonesia.
Strawberries, known for their antioxidant properties, exhibit changes in physiology and metabolite profiles based on cultivation techniques. In Indonesia, strawberries are typically grown in highland regions, but climate change has necessitated adjustments in cultivation practices to enhance production and quality. This study investigates the adaptation of strawberry plants in lowland environments using light-emitting diodes (LEDs) and the exogenous application of methyl jasmonate (MeJA) and methyl salicylic acid (MeSA).
View Article and Find Full Text PDFOptical assessment of heroin using laser-induced fluorescence spectroscopy based on modified Beer-Lambert formalism.
Spectrochim Acta A Mol Biomol Spectrosc
January 2025
Department of Chemistry, Isfahan University of Technology P. O. Box 84156-833111 Isfahan, Iran.
Heroin as a derivative of morphine contains the alkaloids and flavonoids with plenty of three to five aromatic rings. The latter is known as the main source of fluorescence emission after laser excitation. Here, laser induced fluorescence (LIF) spectroscopy at excitation line of 405 nm with the solvent densitometry method is introduced based on modified Beer-Lambert (MBL), for the rapid and reliable identification of street heroin samples.
View Article and Find Full Text PDFPharmacological Characterization of the Novel Selective Kappa Opioid Receptor Agonists 10-Iodo-Akuammicine and 10-Bromo-Akuammicine in Mice.
Neuropharmacology
January 2025
Center for Substance Abuse Research, Lewis Katz School of Medicine, Temple University, Philadelphia, PA, USA. Electronic address:
Akuammicine (AKC), an indole alkaloid, is a kappa opioid receptor (KOR) full agonist with a moderate affinity. 10-Iodo-akuammicine (I-AKC) and 10-Bromo-akuammicine (Br-AKC) showed higher affinities for the KOR with K values of 2.4 and 5.
View Article and Find Full Text PDFManzamine A: A Promising Marine-Derived Cancer Therapeutic for Multi-targeted Interactions with E2F8, SIX1, AR, GSK-3β, and V-ATPase - A Systematic Review.
Eur J Pharmacol
January 2025
Department of Urology, Brown Cancer Center, 505 S Hancock Street, Louisville, KY, USA. Electronic address:
Manzamine A, a natural compound derived from various sponge genera, features a β-carboline structure and exhibits a range of biological activities, including anti-inflammatory and antimalarial effects. Its potential as an anticancer agent has been explored in several tumor models, both in vitro and in vivo, showing effects through mechanisms such as cytotoxicity, regulation of the cell cycle, inhibition of cell migration, epithelial-to-mesenchymal transition (EMT), autophagy, and apoptosis through multi-target interactions of E2F transcriptional factors, ribosomal S6 kinases, androgen receptor (AR), SIX1, GSK-3β, V-ATPase, and p53/p21/p27 cascades. This systematic review evaluates existing literature on the potential application of this marine alkaloid as a novel cancer therapy, highlighting its promising ability to inhibit cancer cell growth while causing minimal side effects.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!