Insect Growth Regulatory Activity of Some Extracts and Compounds from Parthenium argentatum on Fall Armyworm Spodoptera frugiperda

2001 ◽  
Vol 56 (1-2) ◽  
pp. 95-105 ◽  
Author(s):  
Carlos L. Céspedes ◽  
Mariano Martinez-Vázquez ◽  
Jose S. Calderón ◽  
Juan R. Salazar ◽  
Eduardo Aranda
Keyword(s):  
Spodoptera Frugiperda ◽  
Inhibitory Activity ◽  
Fall Armyworm ◽  
Acetylcholinesterase Inhibition ◽  
Melia Azedarach ◽  
Dependent Manner ◽  
Parthenium Argentatum ◽  
Meoh Extract ◽  
Concentration Dependent Manner ◽  
Insect Growth

Abstract Argentatins, Insect Growth Regulators, Acetylcholinesterase The methanolic extract from aerial parts of Parthenium argentatum, afforded argentatin A and B. These compounds were evaluated for their effect on the fall armyworm (Spodoptera frugiperda). Toosendanin, a commercial insecticide derived from Melia azedarach was used as positive control. When tested for activity, using neonate larvae into the no-choice artificial diet bioassays, argentatin A, argentatin B and methanol extract caused significant growth inhibitory activity with GC50 of 17.8, 36.1 and 6.4 ppm at 7 days, respectively, and increased the development time of surviving larvae in a concentration-dependent manner with RGI values of 0.40, 0.60 and 0.26, at 25.0, 25.0 and 5.0 ppm. respectively. In addition, it was possible to observe in most of the treated groups a significant delay in the time of pupation, adult emergence and deformities. Acute toxicity against adults of S. frugiperda was also found, MeOH extract had the most potent activity with LD50 value of 3.10 ppm. In addition, MeOH extract and argentatin A caused acetylcholinesterase inhibition of 93.7% and 90.0%, at 5.0 and 50.0 ppm, respectively; whereas argentatin B had only slight inhibitory activity. Therefore, the MeOH extract was identified as insecticidal extract from P. argentatum with activity at concentrations above 15.0 ppm.

Acetylcholinesterase and Insect Growth Inhibitory Activities of Gutierrezia microcephala on Fall Army worm Spodoptera frugiperda J. E. Smith

2001 ◽  
Vol 56 (5-6) ◽  
pp. 382-394 ◽  
Author(s):  
José S. Calderón ◽  
Carlos L. Céspedes ◽  
Rosaura Rosas ◽  
Federico Gómez-Garibay ◽  
Juan R. Salazar ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Spodoptera Frugiperda ◽  
Inhibitory Activity ◽  
Larval Mortality ◽  
Insect Growth Regulator ◽  
Acetylcholinesterase Inhibition ◽  
Insect Growth ◽  
Growth Inhibitory ◽  
Hexane Extracts ◽  
Inhibitory Activities

From the aerial parts of Gutierrezia microcephala (Asteraceae), four oxyflavones were isolated, namely 5,7,2′-trihydroxy-3,6,8,4′,5′-pentamethoxyflavone (1); 5,7,4′-trihydroxy-3,6,8-trimethoxyflavone (2); 5,7,2′,4′-tetrahydroxy-3,6,8,5′-tetramethoxyflavone (3); 5,2′-dihydroxy- 3,6,7,8,4′,5′-hexamethoxyflavone (4), and an ent-clerodane, bacchabolivic acid (5). Compounds 1-5, the synthetic methyl ester (6 ), n-hexane and MeOH extracts were evaluated against the fall armyworm (Spodoptera frugiperda). Gedunin, a known insect growth regulator isolated from Cedrela spp. was used as a positive control. When tested for activity on neonate larvae into the no-choice artificial diet bioassay, flavone (1), clerodane (5), its methyl ester (6), MeOH and n-hexane extracts caused significant larval mortality with MC50 of 3.9, 10.7, 3.46. 7.95 and 7.5 ppm at 7 days, respectively, as well as growth reduction. They also increased the development time of surviving larvae and a significant delay in time to pupation and adult emergence. Acute toxicity against adults of S. frugiperda was also found, 5, 6 , gedunin and n-hexane extract had the most potent activity with LD50 value of 6.59, 15.05, 10.78, and 12.79 ppm, respectively. In addition, MeOH, n-hexane extracts, 5, 6 and gedunin caused acetylcholinesterase inhibition with 93.7,100,90.2,62.0 and 100% at 50.0 ppm, respectively; whereas 1-4 exhibited only moderate inhibitory activity. Compounds 1,5 and 6 showed inhibitory activities comparable with gedunin. These compounds could be responsible of the insect growth inhibitory activity of this plant.

Effects of supercritical CO2 extracts of Melia azedarach L. on the control of fall armyworm (Spodoptera frugiperda)

2014 ◽  
Vol 93 ◽  
pp. 20-26 ◽  
Author(s):  
Jaqueline Scapinello ◽  
J. Vladimir Oliveira ◽  
Marcelo Lucas Ribeiros ◽  
Osmar Tomazelli ◽  
Luís Antonio Chiaradia ◽  
...  
Keyword(s):  
Spodoptera Frugiperda ◽  
Supercritical Co2 ◽  
Fall Armyworm ◽  
Melia Azedarach

scholarly journals Betulinic Acid Suppresses Ovarian Cancer Cell Proliferation through Induction of Apoptosis

Biomolecules ◽  
2019 ◽  
Vol 9 (7) ◽  
pp. 257 ◽  
Author(s):  
Dahae Lee ◽  
Seoung Rak Lee ◽  
Ki Sung Kang ◽  
Yuri Ko ◽  
Changhyun Pang ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Cancer Cell ◽  
Betulinic Acid ◽  
Molecular Mechanisms ◽  
Underlying Mechanism ◽  
Nuclear Staining ◽  
Dependent Manner ◽  
Meoh Extract ◽  
Concentration Dependent Manner ◽  
Induction Of Apoptosis

Ovarian cancer is one of the leading causes of cancer deaths worldwide in women, and the most malignant cancer among the different gynecological cancers. In this study, we explored potentially anticancer compounds from Cornus walteri (Cornaceae), the MeOH extract of which has been reported to show considerable cytotoxicity against several cancer cell lines. Phytochemical investigations of the MeOH extract of the stem and stem bark of C. walteri by extensive application of chromatographic techniques resulted in the isolation of 14 compounds (1–14). The isolated compounds were evaluated for inhibitory effects on the viability of A2780 human ovarian carcinoma cells and the underlying molecular mechanisms were investigated. An 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was employed to assess the anticancer effects of compounds 1–14 on A2780 cells, which showed that compound 11 (betulinic acid) reduced the viability of these cells in a concentration-dependent manner and had an half maximal (50%) inhibitory concentration (IC50) of 44.47 μM at 24 h. Nuclear staining and image-based cytometric assay were carried out to detect the induction of apoptosis by betulinic acid. Betulinic acid significantly increased the condensation of nuclei and the percentage of apoptotic cells in a concentration-dependent manner in A2780 cells. Western blot analysis was performed to investigate the underlying mechanism of apoptosis. The results indicated that the expression levels of cleaved caspase-8, -3, -9, and Bax were increased in A2780 cells treated with betulinic acid, whereas those of Bcl-2 were decreased. Thus, we provide the experimental evidence that betulinic acid can induce apoptosis in A2780 cells through both mitochondria-dependent and -independent pathways and suggest the potential use of betulinic acid in the development of novel chemotherapeutics for ovarian cancer therapy.

Fire Ant Venom Alkaloid, Isosolenopsin A, a Potent and Selective Inhibitor of Neuronal Nitric Oxide Synthase

2003 ◽  
Vol 22 (2) ◽  
pp. 81-86 ◽  
Author(s):  
G. B. Yi ◽  
D. Mc Clendon ◽  
D. Desaiah ◽  
J. Goddard ◽  
A. Lister ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Inhibitory Activity ◽  
Systemic Toxicity ◽  
Fire Ant ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Nos Inhibitors ◽  
Oxide Synthase ◽  
Nos Isoforms

Massive, multiple fire ant, Solenopsis invicta, stings are often treated aggressively, particularly in the elderly, despite limited evidence of systemic toxicity due to the venom. Over 95% of the S. invicta venom is composed of piperidine alkaloid components, whose toxicity, if any, is unknown. To assess a possible pharmacological basis for systemic toxicity, an alkaloid-rich, protein-free methanol extract of the venom from whole ants was assayed for inhibitory activity on the following nitric oxide synthase (NOS) isoforms, rat cerebellar neuronal (n NOS), bovine recombinant endothelial (e NOS), and murine recombinant immunologic (i NOS). Cytosolic NOS activity was determined by measuring the conversion of [3H]arginine to [3H]citrulline in vitro. Rat n NOS activity was inhibited significantly and in a concentration-dependent manner by the alkaloid-rich venom extract. For n NOS, enzyme activity was inhibited by approximately 50% with 0.33 ± 0.06 μgg of this venom extract, and over 95% inhibition of the three isoforms, n NOS, e NOS, and i NOS, was found with doses of 60 μg in 60-μl reaction mixture. These results indicate that the alkaloid components of S. invicta venom can produce potent inhibition of all three major NOS isoforms. Isosolenopsin A ( cis-2-methyl-6-undecylpiperidine), a naturally occurring fire ant piperidine alkaloid, was synthesized and tested for inhibitory activity against the three NOS isoforms. Enzyme activities for n NOS and e NOS were over 95% inhibited with 1000 μM of isosolenopsin A, whereas the activity of i NOS was inhibited by only about 20% at the same concentration. The IC50 for each of three NOS isoforms was approximately 18 ± 3.9 μM for n NOS, 156 ± 10 μM for e NOS, and >1000 μM for i NOS, respectively. Kinetic studies showed isosolenopsin A inhibition to be noncompetitive with L-arginine ( Ki = 19 ± 2 μM). The potency of isosolenopsin A as an inhibitor of n NOS compares favorably with the inhibitory potency of widely used n NOS inhibitors. Inhibition of NOS isoforms by isosolenopsin A and structurally similar compounds may have toxicological significance with respect to adverse reactions to fire ant stings.

scholarly journals Chemical Constituents of the Bulbs of Scilla peruviana and Their Pancreatic Lipase Inhibitory Activity

2021 ◽  
Vol 22 (3) ◽  
pp. 1262
Author(s):  
Yukiko Matsuo ◽  
Asuka Yamashiro ◽  
Kanae Ootomo ◽  
Mika Nakagawa ◽  
Hiroko Tsuchihashi ◽  
...  
Keyword(s):  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Serum Triglyceride ◽  
2D Nmr ◽  
Triterpene Glycosides ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Phytochemical Investigation

Scilla species are used as medicinal plants and contain lanosterol-type triterpene glycosides. The phytochemical investigation of the bulbs of Scilla peruviana led to the isolation of 17 compounds, including three new rearranged pentacyclic-lanosterol glycosides (1–3) and two new homoisoflavanone glycosides (12 and 13). The structures of the undescribed compounds were determined by extensive spectroscopic analyses, including two-dimensional (2D) NMR. Among the triterpene glycosides, 2, 3, and 6 showed significant pancreatic lipase inhibitory activity in a concentration-dependent manner in vitro. The oral administration of scillascilloside D-2 (6) reduced serum triglyceride levels in a dose-dependent manner in soybean oil-loaded mice.

scholarly journals Collagenase inhibition by water-pepper (Polygonum hydropiper L.) sprout extract

2019 ◽  
Vol 8 (2) ◽  
pp. 114-119 ◽  
Author(s):  
Tomoaki Kawaguchi ◽  
Kaori Nagata
Keyword(s):  
Column Chromatography ◽  
Inhibitory Activity ◽  
High Performance ◽  
Inhibitory Effect ◽  
Skin Aging ◽  
Dependent Manner ◽  
Dermal Matrix ◽  
Polygonum Hydropiper ◽  
Concentration Dependent Manner ◽  
Hplc Fraction

Introduction: Collagenase plays an important role in the degradation of dermal matrix proteins leading to wrinkle formation. The objectives of this study were to evaluate the inhibitory effect of water-pepper (Polygonum hydropiper L.) sprout extract on the activity of collagenase and to identify the inhibitory compounds.Methods: Collagenase inhibitory activity was measured by spectrophotometric assay. Activity-guided fractionation was performed using liquid-liquid extraction of water and n-butanol and Diaion HP-20 column chromatography, followed by high-performance liquid chromatography (HPLC) fraction collection.Results: A methanolic extract of water-pepper sprout inhibited collagenase activity in a concentration-dependent manner with an IC50 value of 156.7 μg/mL. Collagenase inhibitory activity (IC50 = 23.5 μg/mL) was found in 50% methanol eluate from the HP-20 column chromatography of the n-butanol soluble fraction. The active compound (IC50 = 1.9 μg/mL) in the eluate was isolated by HPLC and identified as quercetin-3-O-galactoside (hyperoside) from comparing retention time, UV-Vis absorption, and mass spectra with those of the standard. Lineweaver-Burk plots revealed that hyperoside was an uncompetitive inhibitor against collagenase. Hyperoside was also the most abundant flavonoid present in the methanolic extract.Conclusion: These results suggest that water-pepper sprouts could be beneficial as a natural source of collagenase inhibitor which might be used for the treatment of skin aging.

scholarly journals Uridine Triphosphate Thio-analogues Inhibit Platelet P2Y12 Receptors and Aggregation

2016 ◽  
Author(s):  
Dursun Guenduez ◽  
Christian Tanislav ◽  
Daniel Sedding ◽  
Mariana Parahuleva ◽  
Sentot Santoso ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Inhibitory Activity ◽  
Platelet Rich Plasma ◽  
P2y12 Receptor ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Uridine Triphosphate ◽  
Ic50 Value ◽  
Adp Receptor ◽  
First Time

Platelet P2Y12 is an important ADP receptor that is involved in agonist-induced platelet aggregation and is a valuable target for the development of anti-platelet drugs. Here we characterise the effects of thio-analogues of uridine triphosphate (UTP) on ADP-induced platelet aggregation. Using human platelet-rich plasma we demonstrate that UTP inhibits P2Y12 but not P2Y1 receptors and antagonises 10 μM ADP-induced platelet aggregation in a concentration-dependent manner with an IC50 value of ~250 μM. An 8-fold higher platelet inhibitory activity was observed with a 2-thio analogue of UTP (2S-UTP), with an IC50 of 30 μM. The 4-thio analogue (4S-UTP) with an IC50 of 7.5 μM was 33-fold more effective. A 3-fold decrease in inhibitory activity, however, was observed by introducing an isobutyl group at the 4S- position. A complete loss of inhibition was observed with thio-modification of the γ phosphate of the sugar moiety, which yields an enzymatically stable analogue. The interaction of UTP analogues with P2Y12 receptors was verified by P2Y12 receptor binding and cAMP assays. These novel data demonstrate for the first time that 2- and 4-thio analogues of UTP are potent P2Y12 receptor antagonists that may be useful for therapeutic intervention.

Bilirubin Directly Inhibits Proteolytic Cleavage of a Fluorogenic VWF73 Peptide and Plasma Von Willebrand Factor

Blood ◽  
2014 ◽  
Vol 124 (21) ◽  
pp. 2882-2882
Author(s):  
Ruinan Lu ◽  
X. Long Zheng
Keyword(s):  
Differential Diagnosis ◽  
Thrombotic Microangiopathy ◽  
Inhibitory Activity ◽  
Conflicts Of Interest ◽  
Proteolytic Cleavage ◽  
Unconjugated Bilirubin ◽  
Breakdown Product ◽  
Dependent Manner ◽  
Adamts13 Activity ◽  
Concentration Dependent Manner

Abstract Bilirubin is a yellow breakdown product of heme catabolism. Increased levels of plasma bilirubin are a condition commonly seen in neonates and adults with hemolysis. The unconjugated bilirubin consists of an open chain of four pyrrole-like rings. Previous studies have shown that bilirubin decreases the cleavage of a commercially available FRETS­­­­­-VWF73 assay, resulting in falsely low plasma ADAMTS13 activity. However, the mechanism underlying such a reduction of ­­­­ADAMTS13 activity is not fully understood. Plasma ADAMTS13 activity is critical for differential diagnosis of thrombotic microangiopathy in which low ADAMTS13 activity (less than 5-10%) is more consistent with thrombotic thrombocytopenic purpura (TTP), while normal to mildly reduced ADAMTS13 activity (greater than 10-20%) is the common findings of hemolytic uremic syndrome (HUS). Here, we show that bilirubin directly inhibits the proteolytic cleavage of a fluorogenic VWF73 peptides labeled with fluorescein-5-maleimide (FL485-VWF73) (ext. 485nm/emi.530nm) or DyLight-633-maleimide (DL633-VWF73) (ext.638nm/emi.658 nm) in a concentration-dependent manner (Fig. 1). The IC50 for inhibiting the cleavage of FL485-VWF73 and DL633-VWF73 was estimated to be 13 micro mol/L and 70 micro mol/L, respectively. To confirm the direct inhibitory activity, bilirubin at various concentrations was incubated with plasma-derived multimeric VWF and recombinant ADAMTS13 in the presence of 1.5 M urea, 5 mM Tris-HCl, pH 8.0 for four hours. The cleavage of multimeric VWF was determined by 1% agarose and SDS-polyacrylamide gel electrophoreses, followed by Western blotting with rabbit anti-VWF IgG. The results demonstrated that bilirubin also inhibited recombinant ADAMTS13-mediated cleavage of VWF in a concentration-dependent manner with an IC50 ~0.43 milli mol/L (Fig. 2). The inhibitory activity of bilirubin on the cleavage of a fluorogenic peptide or a multimeric VWF substrate was largely eliminated by addition of bilirubin oxidase that converts bilirubin to biliverdin (not shown). Our results demonstrate for the first time that unconjugated bilirubin directly inhibits plasma and recombinant ADAMTS13 activity in addition to its known interference with certain fluorogenic assays for ADAMTS13 activity. These findings are clinically important concerning diagnosis and differential diagnosis of thrombotic microangiopathy. Additionally, our findings may shed new light on the mechanism of thrombotic complications pertinent to acute hemolysis and liver diseases. Figure 1 Figure 1. Figure 2 Figure 2. Disclosures No relevant conflicts of interest to declare.

scholarly journals In Vivo and In Vitro α-Glucosidase Inhibitory Activity of Perfoliatin a from Melampodium Perfoliatum

2019 ◽  
Vol 14 (1) ◽  
pp. 1934578X1901400 ◽  
Author(s):  
Laura Flores-Bocanegra ◽  
Rafael Torres-Colín ◽  
Martin González-Andrade ◽  
José S. Calderón ◽  
Rachel Mata
Keyword(s):  
Inhibitory Activity ◽  
Sesquiterpene Lactones ◽  
Tolerance Test ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Glucosidase Inhibitors ◽  
In Vivo Testing ◽  
Oral Sucrose

As part of our effort to discover new α-glucosidase inhibitors from natural sources, it was found that an aqueous extract from Melampodium perfoliatum (Cavanilles) Kunth (Asteraceae) inhibited the activity of rat-intestinal α-glucosidases in a concentration dependent manner (IC50= 958 μg/mL). Fractionation of the active extract led to the isolation of perfoliatin A (1), which was active against the mammal α-glucosidases and a recombinant α-glucosidase with maltase-glucoamylase activity obtained from Ruminococcus obeum. Kinetic analysis revealed that the interaction of 1 with R. obeum-α-glucosidase was noncompetitive. The calculated Ki was 0.68 ± 0.034 mM. In vivo testing using an oral sucrose tolerance test, in healthy and hyperglycemic mice, revealed that perfoliatin A (1) reduced significantly the postprandial peak, consistent with its α-glucosidase inhibitory activity. The effect was comparable or better to that of acarbose, a therapeutically used α-glucosidase inhibitor. Altogether, these findings clearly supported the α-glucosidase inhibitory activity of melampolide-type of sesquiterpene lactones.

scholarly journals Antiausterity Activity of Arctigenin Enantiomers: Importance of (2R,3R)-Absolute Configuration

2014 ◽  
Vol 9 (1) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Suresh Awale ◽  
Mamoru Kato ◽  
Dya Fita Dibwe ◽  
Feng Li ◽  
Chika Miyoshi ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Absolute Configuration ◽  
The Other ◽  
Dependent Manner ◽  
Meoh Extract ◽  
Concentration Dependent Manner ◽  
Akt Activation ◽  
Other Hand

From a MeOH extract of powdered roots of Wikstroema indica, six dibenzyl-γ-butyrolactone-type lignans with (2 S,3 S)-absolute configuration [(+)-arctigenin (1), (+)-matairesinol (2), (+)-trachelogenin (3), (+)-nortrachelogenin (4), (+)-hinokinin (5), and (+)-kusunokinin (6)] were isolated, whereas three dibenzyl-γ-butyrolactone-type lignans with (2 R,3 R)-absolute configuration [(-)-arctigenin (1), (-)-matairesinol (2), (-)-trachelogenin (3)] were isolated from Trachelospermum asiaticum. The in vitro preferential cytotoxic activity of the nine compounds was evaluated against human pancreatic PANC-1 cancer cells in nutrient-deprived medium (NDM), but none of the six lignans (1–6) with (2 S,3 S)-absolute configuration showed preferential cytotoxicity. On the other hand, three lignans (1*–3*) with (2 R,3 R)-absolute configuration exhibited preferential cytotoxicity in a concentration-dependent manner with PC50 values of 0.54, 6.82, and 5.85 μM, respectively. Furthermore, the effect of (-)- and (+)-arctigenin was evaluated against the activation of Akt, which is a key process in the tolerance to nutrition starvation. Interestingly, only (-)-arctigenin (1*) strongly suppressed the activation of Akt. These results indicate that the (2 R,3 R)-absolute configuration of (-)-enantiomers should be required for the preferential cytotoxicity through the inhibition of Akt activation.

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