Flavone acetic acid (LM-975; NSC-347512) activation to cytotoxic species in vivo and in vitro

1989 ◽  
Vol 24 (5) ◽  
pp. 273-276 ◽  
Author(s):  
Guy G. Chabot ◽  
Marie-Christine Bissery ◽  
Alain Gouyette
Author(s):  
Thriveni Vasanth Kumar ◽  
Manjunatha H. ◽  
Rajesh Kp

Objective: Dietary curcumin and capsaicin are well known for their health beneficial potencies. The current study was done to assess the anti-inflammatory activity of curcumin, capsaicin and their combination by employing in vitro and in vivo models.Methods: We investigated the protective effect of curcumin, capsaicin and their combination using in vitro heat induced human red blood cell (HRBC) membrane stabilisation, in vivo 3% agar induced leukocyte mobilisation and acetic acid induced vascular permeability assay.Results: Curcumin, capsaicin and their combination exhibited concentration dependent protective effect against heat-induced HRBC membrane destabilisation, while combined curcumin and capsaicin restored 87.0±0.64 % membrane stability and it is found to be better than curcumin, capsaicin and diclofenac sodium (75.0±0.25. 72±0.9 and 80.0±0.31 %) protective effect. In agar suspension induced leukocyte mobilization assay, the combined curcumin and capsaicin had shown 39.5±1.58 % of inhibition compared to individual curcumin and capsaicin, which showed moderate inhibition of 16.0±3.14 and 21.6±2.17 % respectively. Besides, the combined curcumin and capsaicin had shown highly significant inhibition of acetic acid-induced vascular permeability in rats (62.0±3.14 %), whereas individual curcumin and capsaicin showed moderate inhibition of vascular permeability with 36.0±2.41 and 43.0±1.92 % respectively.Conclusion: This study demonstrates the significant anti-inflammatory property of combined curcumin and capsaicin at half of the individual concentration of curcumin and capsaicin.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Shanghui Jin ◽  
Bingkai Hou ◽  
Guizhi Zhang

AbstractLeaf angle is an important agronomic trait affecting photosynthesis efficiency and crop yield. Although the mechanisms involved in the leaf angle control are intensively studied in monocots, factors contribute to the leaf angle in dicots are largely unknown. In this article, we explored the physiological roles of an Arabidopsis glucosyltransferase, UGT74D1, which have been proved to be indole-3-acetic acid (IAA) glucosyltransferase in vitro. We found that UGT74D1 possessed the enzymatic activity toward IAA glucosylation in vivo and its expression was induced by auxins. The ectopically expressed UGT74D1 obviously reduced the leaf angle with an altered IAA level, auxin distribution and cell size in leaf tissues. The expression of several key genes involved in the leaf shaping and leaf positioning, including PHYTOCHROME KINASE SUBSTRATE (PKS) genes and TEOSINTE BRANCHED1, CYCLOIDEA, and PCF (TCP) genes, were dramatically changed by ectopic expression of UGT74D1. In addition, clear transcription changes of YUCCA genes and other auxin related genes can be observed in overexpression lines. Taken together, our data indicate that glucosyltransferase UGT74D1 could affect leaf positioning through modulating auxin homeostasis and regulating transcription of PKS and TCP genes, suggesting a potential new role of UGT74D1 in regulation of leaf angle in dicot Arabidopsis.


2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Tamires Rocha Falcão ◽  
Aurigena Antunes de Araújo ◽  
Luiz Alberto Lira Soares ◽  
Iuri Brilhante de Farias ◽  
Wliana Alves Viturino da Silva ◽  
...  

Background.Libidibia ferrea(L. ferrea)is found throughout the northeastern region of Brazil, where it has been used in folk medicine with beneficial effects on many inflammatory disorders.Purpose. This study investigated the phytochemical composition of the crude extract and fractions ofL. ferreafruit and evaluated its anti-inflammatory and antinociceptive activitiesin vivoand effect on cell viabilityin vitro.Methods. Characterization of polyphenols present in crude extract (CE), hydroalcoholic fractions of 20-80% ethanol (CE20, CE40, CE60, and CE80), aqueous fraction (AqF), and ethyl acetate (EAF) fractions ofL. ferreafruit was performed by chromatographic analysis.Anti-inflammatory activity was evaluated by using a carrageenan-induced peritonitis model submitted to a leukocyte migration assay and myeloperoxidase activity (MPO) analysis. Total glutathione and malondialdehyde (MDA) levels were assessed to evaluate the oxidative stress level. Antinociceptive activity was evaluated by acetic acid-induced abdominal writhing and hot plate test.In vitrocell viability was determined by using MTT assay in a mouse embryonic fibroblast cell line (3T3 cells).Results. Chromatography revealed the presence of ellagic acid content in EAF (3.06), CE (2.96), and CE40 (2.89). Gallic acid was found in EAF (12.03), CE 20 (4.43), and CE (3.99).L. ferreacrude extract and all fractions significantly reduced leukocyte migration and MPO activity (p<0.001).L. ferreaantioxidant effect was observed through high levels of total glutathione and reduction of MDA levels (p<0.001). Acetic acid-induced nociception was significantly inhibited after administration ofL. ferreacrude extract and all fractions (p<0.001). Crude extract and all fractions significantly increased the viability of the 3T3 cell line (p<0.05).Conclusions. The appropriate extraction procedure preserves the chemical components ofL. ferreafruit, such as gallic acid and ellargic acid. Crude extract and fractions ofL. ferreafruit exhibited anti-inflammatory, antioxidant, antinociceptive activitiesin vivoand enhanced cell viabilityin vitro.


2004 ◽  
Vol 15 (4) ◽  
pp. 864-871 ◽  
Author(s):  
E. von Guggenberg ◽  
M. Behe ◽  
T. M. Behr ◽  
M. Saurer ◽  
T. Seppi ◽  
...  

2009 ◽  
Vol 99 (3) ◽  
pp. 258-264 ◽  
Author(s):  
Ting Yu ◽  
Jishuang Chen ◽  
Huangping Lu ◽  
Xiaodong Zheng

Cryptococcus laurentii is a well-known postharvest biocontrol yeast; however, it cannot provide satisfactory levels of decay control when used alone. Here, we evaluated the effects of indole-3-acetic acid (IAA), a plant growth regulator, on the biocontrol efficacy of the yeast antagonist C. laurentii against blue mold rot caused by Penicillium expansum in apple fruit. Results showed that the addition of IAA at 20 μg/ml to suspensions of C. laurentii greatly enhanced inhibition of mold rot in apple wounds compared with that observed with C. laurentii alone. The addition of IAA at 20 μg/ml or lower did not influence the population growth of C. laurentii in wounds, but adverse effects were seen on C. laurentii when the concentration of IAA was increased to 200 μg/ml or above in vitro and in vivo. P. expansum infection in apple wounds was not inhibited when the pathogen was inoculated into the fruit wounds within 2 h after application of IAA; however, infection was reduced when inoculated more than 12 h after IAA application. Treatment of wounds with IAA at 20 μg/ml 24 h before pathogen inoculation resulted in significant inhibition of P. expansum spore germination and host infection. Application of IAA at 20 μg/ml also reduced P. expansum infection when it was applied 48 h before pathogen inoculation in the intact fruit. Thus, IAA could reinforce the biocontrol efficacy of C. laurentii in inhibiting blue mold of apple fruit by induction of the natural resistance of the fruit.


2010 ◽  
Vol 89 (3) ◽  
pp. 351-357 ◽  
Author(s):  
Kari Ann Shirey ◽  
Quan M. Nhu ◽  
Kevin C. Yim ◽  
Zachary J. Roberts ◽  
John R. Teijaro ◽  
...  

1996 ◽  
Vol 10 (2) ◽  
pp. 159-169 ◽  
Author(s):  
C.E. Smith ◽  
M. Issid ◽  
H.C. Margolis ◽  
E.C. Moreno

The objectives of this study were to measure pH in developing enamel at progressively older (more mature) stages of amelogenesis in vivo, and then to formulate synthetic enamel fluid mixtures that approximated these pH values for in vitro studies. The ultimate goal was to characterize the molecular weights of proteinases visualized by enzymograms incubated in synthetic enamel fluid using gelatin and casein as substrates. For most experiments. the proteinases were extracted en masse from small freeze-dried enamel strips directly into a non-reducing sample preparation buffer. In some experiments, we pre-treated the enamel strips with acetic acid to determine if this common method for demineralization and protein extraction caused any changes in the activity levels of the enamel proteinases. In other experiments, we first soaked enamel strips in synthetic enamel fluid to determine solubility of the proteinases within an aqueous phase. The results indicated that the pH of developing enamel remained fairly constant near pH 7.23 across the secretory stage, but it was generally more acidic (6.93) and fluctuated in focal areas between mildly acidic (6.2-6.8) and near-neutral (7.2) conditions across the maturation stage. The pH then slowly rose to near 7.35 when the enamel was almost mature (hard). The acidic conditions were generally inhibitory to most enamel proteinases, but there were some caseinase activities in mid-maturation-stage enamel near 23-30 kDa which appeared to be activated by weakly acidic conditions (pH 6.28). Pre-treatment of enamel samples with 0.5 M acetic acid markedly altered the overall profile of enamel proteinases, causing activation of some latent proteinase activities and permanent inhibition of other activities. Most proteinases in whole homogenates were insoluble in synthetic enamel fluid. This suggests that they may be tightly bound, directly or indirectly, to matrix proteins or mineral components in situ.


2017 ◽  
Author(s):  
Xiaodan Xu ◽  
Wei Zheng

This study aimed to establish a simple and efficient in vivo multiplication protocol by leaf cutting to satisfy the supply of young succulent ornamentals Pachyveria pachytoides and Sedum morganianum. The regenerability of leaves injected with 6-benzylaminopurine (BAP) and α-naphthalene acetic acid (NAA) in vivo were tested with common leaf cutting as control. Results showed a 100% shoot induction frequency using hormone-injeceted methods for the two species. The number of shoots per leaf of 4.0 or 6.0 mg l −1 BAP and 0.1 mg l −1 NAA injected in vivo (5.08-5.14 in P. pachytoides, and 6.22-6.74 for S. morganianum) were significantly greater than that of the other treatments. Since the h ormone-injected leaf cutting needs no aseptic operation which is necessary for in vitro multiplication, it is simple for the commercial production of the two species. The new in vivo propagation method would be of great interest for growers and breeders of succulent plants.


2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Syeda Rubaiya Afrin ◽  
Mohammad Rashedul Islam ◽  
Bibi Humayra Khanam ◽  
Nawreen Monir Proma ◽  
Sayeda Saima Didari ◽  
...  

Abstract Background Macropanax dispermus is traditionally used to treat various diseases by ethnic people. The present research reports the pharmacological properties with phytochemical profiling of the crude extracts of M. dispermus leaves (MDML), its n-hexane (MDHL), carbon tetrachloride (MDTL), chloroform (MDCL), ethyl acetate (MDEL), and aqueous (MDAL) fractions, and crude methanol extracts of its stem barks (MDMS). The in vitro thrombolytic activity was done on human erythrocytes whereas the cytotoxic activity was done by brine shrimp lethality assay. The in vivo analgesic activity was examined by acetic acid-induced writhing, tail immersion, and formalin-induced paw licking method. In contrast, antipyretic activity was done by the brewer’s yeast-induced pyrexia method. Results MDHL and MDMS showed 37.05% and 42.21% of significant (p < 0.01) thrombolytic activity, respectively. MDCL and MDMS showed the lower LC50 values of 23.15 and 37.11 µg/ml during cytotoxicity test, respectively. In acetic acid writhing method, MDTL and MDEL showed significant (p < 0.001) inhibition of writhing by 79.34% and 80.17%, respectively. MDMS showed significant (p < 0.001) maximal possible effect (%MPE) of 45.95%, 62.26%, 65.79%, 89.69% and elongation of time in pain reaction of 48.53%, 60.28%, 58.76%, and 70.14% at 30, 60, 90, and 120 min intervals, respectively. MDML at 400 mg/kg exhibited significant (p < 0.001) 82.72% of inhibition of pain at the late phases. MDEL at 400 mg/kg of dose exhibited significant (p < 0.001) reduction of rectal temperature by 36.31%, 62.42%, 89.81%,, and 96.82% at 1, 2, 3, and 4 h intervals, respectively. Conclusion The current research suggests that the plant extracts possess potential thrombolytic, cytotoxic, analgesic, and antipyretic activities.


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