A5001432282- Synthesis and biological activity
- Natural product bioactivities and synthesis
- Sesquiterpenes and Asteraceae Studies
- Plant Toxicity and Pharmacological Properties
- Bioactive natural compounds
- Cell death mechanisms and regulation
- Phytochemistry and Bioactive Compounds
- Plant biochemistry and biosynthesis
- Phytochemical Studies and Bioactivities
- Synthesis of Organic Compounds
- Biological Activity of Diterpenoids and Biflavonoids
- Phytochemistry and Biological Activities
- Protein Kinase Regulation and GTPase Signaling
- Marine Sponges and Natural Products
- Circadian rhythm and melatonin
- Fungal Biology and Applications
- Sphingolipid Metabolism and Signaling
- Bioactive Compounds and Antitumor Agents
- Synthesis and Characterization of Heterocyclic Compounds
- Cancer Treatment and Pharmacology
- Traditional and Medicinal Uses of Annonaceae
- Synthesis and Biological Evaluation
- Carbohydrate Chemistry and Synthesis
- Phytochemical compounds biological activities
- melanin and skin pigmentation
Universidad de Las Palmas de Gran Canaria
2014-2023
Consejo Superior de Investigaciones Científicas
1986-2022
Povisa Hospital
2015
Canary Institute of Cancer Research
2004-2013
FuelCell Energy (United States)
2010
Universidad de La Laguna
1983-2008
Instituto de Productos Naturales y Agrobiología
1984-2008
University of Ferrara
2005
Rega Institute for Medical Research
2004
Universidad de Alcalá
2002
1 Chloroquine was given in 300 mg single doses as an i.v. infusion, oral solution and tablets at intervals of least 56 days to 11 healthy volunteers. Concentrations chloroquine its metabolite desethylchloroquine were measured plasma, erythrocytes urine using h.p.l.c. 2 detectable all plasma samples up 23 occasionally 52 after dosage. Urinary concentrations monitored 119 days. The disposition pattern multiexponential reflecting extensive tissue binding the drug. 3 After dosing volume...
Melatonin is an indoleamine synthesized in the pineal gland, and after its release into blood, it has extensive repertoire of biological activities, including antitumoral properties. In this study, we found that melatonin reduced growth human melanoma cells SK-MEL-1. The antiproliferative effect was associated with alteration progression phases cell cycle also increase tyrosinase activity, key regulatory enzyme melanogenesis. Antagonists for membrane receptors (luzindole 4-P-PDOT) general...
Abstract: Melatonin is an indoleamine that synthesized in the pineal gland and has extensive repertoire of biological activities. In present study, we found melatonin reduced growth human myeloid leukemia cells HL‐60, inhibiting progression from G 1 to S phase cell cycle increasing apoptotic death. Furthermore, treatment elevated cytochrome c release mitochondria augmented caspase‐3 caspase‐9 Upregulation Bax downregulation Bcl‐2 was also observed upon treatment. The effects were not be...
In the present study, cytotoxicity of 30 diterpenoids with an abietane or a halimane skeleton was determined against five human tumor cell lines (HL-60, U937, Molt-3, SK-MEL-1, and MCF-7). Diterpenoids containing including taxodone (1) taxodione (2), as well semisynthetic derivatives 12, 14, 15, 17, 22, were most cytotoxic compounds for leukemia cells. Overexpression protective mitochondrial proteins Bcl-2 Bcl-xL did not confer resistance to diterpene-induced cytotoxicity. Studies performed...
Abstract Melatonin is a naturally occurring indoleamine synthesized in the pineal gland that exhibits an extensive repertoire of biological activities. An increasing number studies indicate melatonin protects normal cells, while it reducing cancer cell proliferation. In this study, we investigated effect on growth human leukemia cells and found efficiently reduced concentration‐ time‐dependent manner. Thus, incubation with increased percentage hypodiploid DNA content, augmented annexin...
We have synthesized and evaluated a series of hybrids polypyrrole minor groove binders structurally related to the natural antitumor agent distamycin A, alpha-methylene-gamma-butyrolactones with methyl, phenyl, 4-substituted phenyl groups at lactone C(gamma) position, denoted 5-17, for in vitro cytotoxic activity against variety cancer cell lines. The apoptotic activities several tumor lines are reported discussed terms their structural differences relation both number N-methylpyrrole rings...
Flavonoids are naturally occurring polyphenolic compounds which display a vast array of biological activities. In this study, we investigated the effects tamarixetin on viability human tumor cell lines and found that it was cytotoxic against leukemia cells in particular P-glycoprotein-overexpressing K562/ADR cells. This compound inhibited proliferation concentration- time-dependent manner, induced apoptosis blocked cycle progression at G2 -M phase. associated with accumulation cyclin B1,...
Melatonin is an endogenous indoleamine with a wide range of biological functions. In addition to modulating circadian rhythms, it plays important roles in the health as antioxidant. has also ability induce apoptosis cancer cells and enhance antitumoral activity chemotherapeutic agents. this study, effect melatonin on hyperthermia-induced was explored using human leukemia cells. The results demonstrate that greatly improved cytotoxicity hyperthermia U937 potentiation cell death achieved 1...
In granulosa cells labeled to isotopic steady-state with [3H]serine, addition of interleukin-1 beta (IL1 beta) or bacterial sphingomyelinase (SMase) induced a rapid decrease (approximately 60% by 10 min) in cellular [3H]Sphingomyelin content and prolonged generation (up 60 [3H]ceramide, the immediate lipid-moiety generated response sphingomyelin hydrolysis. FSH-treated cells, IL1 (0.3-30 ng/ml) inhibited progesterone biosynthesis dose-dependent manner, an effect that was also observed...
Stimulation of [3H]serine-labeled A431 cells with tumor necrosis factor-alpha (TNFalpha) or bacterial sphingomyelinase (SMase) resulted in a rapid decrease (approximately 50% by 15 min) cellular [3H]sphingomyelin content and generation the lipid moiety [3H]ceramide, which remained elevated 60 min later. Sphingomyelin hydrolysis response to TNFalpha SMase time-dependent phosphorylation state c-Jun protein, an effect that was also observed treated membrane-permeable ceramide analogue...
In [3H]serine-labelled granulosa cells treatment with TNF alpha (10 ng/ml) resulted in a transient decrease cellular [3H]sphingomyelin and generation of [3H]ceramide that remained elevated 60 min later. labelled [methyl-14C]choline, induced similar reduction [14C]sphingomyelin content was accompanied by sustained elevation [14C]phosphorylcholine levels. FSH-primed cells, inhibited P450-AROM activity dose-dependent manner, an effect also observed treated bacterial sphingomyelinase (SMase...
Flavonoids are polyphenolic compounds that ubiquitously in plants and display a vast array of biological activities. Here we have studied the effect phenylbenzo-γ-pyrone-derivative quercetin 3-methyl ether tetracetate (QD), obtained by acetylation natural product ether, on cell viability human leukemia HL-60 U937 lines. The results show QD was cytotoxic induced G 2 –M phase cycle arrest both lines it potent apoptotic inducer cells. QD-induced apoptosis is (i) mediated caspase activation,...
Eupatorin is a naturally occurring flavone that inhibits cell proliferation in human tumor cells. Here we demonstrate eupatorin arrests cells at the G2-M phase of cycle and induces apoptotic death involving activation multiple caspases, mitochondrial release cytochrome c poly(ADP-ribose) polymerase cleavage leukemia This flavonoid induced phosphorylation members mitogen-activated protein kinases was attenuated by inhibition c-jun N-terminal kinases/stress activated kinases. Eupatorin-induced...
Three new compounds, 5α-lanosta-7,9(11),24-triene-3β-hydroxy-26-al (1), 5α-lanosta-7,9(11),24-triene-15α-26-dihydroxy-3-one (2), and 8α,9α-epoxy-4,4,14α-trimethyl-3,7,11,15,20-pentaoxo-5α-pregnane (3), were isolated from Ganoderma concinna along with 12 known compounds. The structures of compounds 1 2 determined on the basis MS NMR studies. structure 3 was by MS, NMR, single-crystal X-ray diffraction. Compounds 1, 2, induce apoptosis in human promyelocytic leukemia HL-60 cells, as indicated...
From the stem bark of Dracaena draco, three new compounds, namely, draconins A−C (1−3), were isolated, along with 17 known compounds. The structures compounds isolated elucidated on basis spectroscopic data interpretation. Several showed potent cytotoxic activities measured human leukemia cell line HL-60 (IC50's from 2.0 to 9.7 μM at 72 h). mechanism by which 1 and 2 display their cytostatic properties is through induction death apoptosis, as evaluated fluorescence microscopy DNA fragmentation.
A new lanostanoid triterpene, 3-oxosulfurenic acid (1), together with three known triterpenes (3, 4, and 7) were isolated from the fruit bodies of Laetiporus sulphureus. Cytotoxicity these compounds their derivatives (2, 5, 6) was evaluated on HL-60 cells. Further studies revealed that acetyl eburicoic (5) most potent apoptosis inducer. Apoptosis accompanied by both activation caspase-3 fragmentation poly(ADP-ribose) polymerase-1 also associated an early release cytochrome c mitochondria.
6,7-dehydroroyleanone (DHR) is a cytotoxic abietane present in the essential oil of Plectranthus madagascariensis.Different extraction parameters were tested, and its optimization was accomplished with Clevenger apparatus-based hydrodistillation. After isolation, effect on microtubules, P-glycoprotein caspases assessed several cell lines compound coupled hybrid nanoparticles. The results show that DHR does not interfere microtubule formation, but evades resistance mechanisms P-glycoprotein....