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101.
The naturally occurring yellow dietary diarylheptanoid curcumin (1) was converted by γ-ray to two new γ-lactones, curculactones A (2) and B (3), as well as four known transformates, erythro-1-(3-methoxy-4-hydroxy-phenyl)-propan-1,2-diol (4), threo-1-(3-methoxy-4-hydroxy-phenyl)-propan-1,2-diol (5), vanillic acid (6), and vanillin (7). The structures of the two new γ-lactone derivatives were elucidated on the basis of spectroscopic methods. The steroisomeric phenylpropanoids 4 and 5 exhibited significantly enhanced inhibitory activity against pancreatic lipase when compared to parent curcumin. 相似文献
102.
Glioblastoma is the most malignant human brain tumor that shows poor response to existing therapeutic agents. Search continues
for an effective therapy for controlling this deadliest brain tumor. Curcumin (CCM), a polyphenolic compound from Curcuma longa, possesses anti-cancer properties in both in vitro and in vivo. In the present investigation, we evaluated the therapeutic
efficacy of CCM against human malignant glioblastoma U87MG cells. Trypan blue dye exclusion test showed decreased viability
of U87MG cells with increasing dose of CCM. Wright staining and ApopTag assay, respectively, showed the morphological and
biochemical features of apoptosis in U87MG cells treated with 25 μM and 50 μM of CCM for 24 h. Western blotting showed activation
of caspase-8, cleavage of Bid to tBid, increase in Bax:Bcl-2 ratio, and release of cytochrome c from mitochondria followed by activation of caspase-9 and caspase-3 for apoptosis. Also, CCM treatments increased cytosolic
level of Smac/Diablo to suppress the inhibitor-of-apoptosis proteins and down regulated anti-apoptotic nuclear factor kappa
B (NFκB), favoring the apoptosis. Increased activities of calpain and caspase-3 cleaved 270 kDa α-spectrin at specific sites
generating 145 kDa spectrin break down product (SBDP) and 120 kDa SBDP, respectively, leading to apoptosis in U87MG cells.
Results show that CCM is an effective therapeutic agent for suppression of anti-apoptotic factors and activation of calpain
and caspase proteolytic cascades for apoptosis in human malignant glioblastoma cells.
Special issue in honor of Naren Banik. 相似文献
103.
Yamaguchi M Hamamoto R Uchiyama S Ishiyama K 《Molecular and cellular biochemistry》2007,303(1-2):83-88
The effect of various flavonoids, which are present in food and plants, on bone calcium content and osteoclastogenesis were
investigated to compare action of flavonoid on bone formation and bone resorption in vitro. Rat femoral-diaphyseal (cortical
bone) and -metaphyseal (trabecular bone) tissues were cultured for 48 h in Dulbecco’s modified Eagle’s medium (high glucose)
supplemented with antibiotics and bovine serum albumin. Amoung quercetin, myricetin, kaempferol, isorhamnetin, curcumin, hesperidin,
or astaxanthin in the range of 10−7–10−5 M, culture with quercetin (10−6 or 10−5 M) caused a significant increase in diaphyseal calcium content. Such an effect was not seen in other compounds. Mouse bone
marrow cells were cultured for 7 days in the presence of parathyroid hormone (PTH; 10−7 M), a bone-resorbing factor, in vitro. Culture with PTH caused a significant increase in osteoclast-like cell formation. This
increase was significantly inhibited in the presence of quercetin, myricetin, kaempferol, isorhamnetin, or curcumin in the
range of 10−8–10−6 M. Such an effect was not seen in the case of hesperidin or astaxanthin. In addition, culture with PTH (10−7 M) caused a significant decrease in diaphyseal calcium content. This decrease was completely prevented in the presence of
quercetin, myricetin, kaempferal, or isorhamnetin of 10−6 M. This study demonstrates that various flavonoids have a potent inhibitory effect on osteoclastogenesis and bone resorption
rather than bone formation in vitro. Among various flavonoids, quercetin had a stimulatory effect on bone formation and an
inhibitory effect on bone resorption in vitro. 相似文献
104.
105.
Gomez G Mansouraty G Gardea J Narayan M 《Biochemical and biophysical research communications》2007,364(3):561-566
Curcumin, the major constituent of turmeric is a known antioxidant. We have examined the oxidative folding of the model four-disulfide-bond-containing protein bovine pancreatic ribonuclease A (RNase A) in its presence; results indicate that RNase A regeneration rate increases in a curcumin-dependent manner. Examination of the native tendency of the fully-reduced polypeptide and the stability of key folding intermediates suggests that the increased oxidative folding rate can be attributed to native-like elements induced within the fully-reduced polypeptide and the stabilization of native-like species by this non-redox-active natural product. Our results provide a template for the design of curcuminoid-based synthetic small-molecule fold catalysts that accelerate the folding of ER-processed proteins; this assumes significance given that nitrosative stress and dysfunction of the ER-resident oxidoreductase protein disulfide isomerise due to S-nitrosylation are factors associated with the pathogenesis of Alzheimer’s and Parkinson’s diseases. 相似文献
106.
Gasem Mohammad Abu-Taweel 《Saudi Journal of Biological Sciences》2019,26(4):736-743
In the present investigation, the effects of mercuric chloride (HgCl2) on the neurobehavioural and neurochemical disruption in mice offspring was studied. A total of thirty pregnant mice were divided into six groups. Group II and III were received 150 and 300 ppm of curcumin respectively. Group IV was given 10 ppm of HgCl2. Group V and VI were given 10 ppm of HgCl2 with 150 and 300 ppm of curcumin respectively. In this study, treatment started from day one of pregnancy and continued until post-natal day 15 (PD 15). During weaning period, three pups in each experimental group were marked and were subjected to behavioral, physical and biochemical tests. The results revealed decreased body weight, delayed hair growth and eye opening. HgCl2 treated pups taken more time in righting, rotating reflexes to return to normal placement, cliff avoidance compared to that of control group. HgCl2 exposed pups showed memory and learning deficits. Anxiety behavior in treating pups was increased. Biochemical investigations showed decreased level of dopamine (DA), serotonin (5-HT) and acetylcholinesterase (AChE) in forebrain of treated pups compared to the control and curcumin groups. The protective effect of curcumin doses were significant compared to HgCl2 group. The results indicated that the administration of curcumin showed effective activity towards biochemical and behavioral disorders obtained with the HgCl2 treated animals. Overall, the curcumin administration revealed increased cognetion and anxiety behaviors in the treated animals. Conclusively, curcumin has a good benefits for health which can use to avoid toxicants such as Hg and other heavy metals. 相似文献
107.
目的:探究miR-21是否介导姜黄素(Cur)预处理抗多柔比星(DOX)心肌毒性作用。方法:体外分离培养大鼠原代心肌细胞,用DOX处理24 h建立心肌毒性离体模型。姜黄素于DOX处理前12 h加入心肌细胞培养液中。实验分组如下:Control组;Cur组;DOX组;Cur+DOX组;miR-21i(miR-21抑制剂)+Cur+DOX组;miR-21i+DOX组。DOX处理24 h后检测miR-21表达情况、细胞活力、凋亡和氧化应激相关指标。结果:与DOX组相比,姜黄素预处理可呈剂量依赖性地提高DOX处理后心肌细胞活力,且浓度为5μM时效果最佳。此外,姜黄素预处理可以明显提高Bcl-2和miR-21表达,降低心肌Bax和cleaved Caspase-3表达、凋亡率以及心肌细胞活性氧(ROS)产量和丙二醛(MDA)含量。而用miR-21i下调miR-21表达可明显削弱姜黄素预处理对DOX心肌损伤的上述保护作用(均P0.05)。结论:姜黄素预处理可通过上调miR-21表达,缓解心肌凋亡和氧化应激损伤,进而缓解DOX心肌毒性。 相似文献
108.
Can Xiao Lili Wang Lifang Zhu Chenping Zhang Jianhua Zhou 《Biochemical and biophysical research communications》2014
Curcumin, a phytochemical derived from the rhizome of Curcuma longa, has shown anticancer effects against a variety of tumors. In the present study, we investigated the effects of curcumin on the miR-9 expression in oral squamous cell carcinoma (OSCC) and explored the potential relationships between miR-9 and Wnt/β-catenin pathway in curcumin-mediated OSCC inhibition in vitro. As the results shown, the expression levels of miR-9 were significantly lower in clinical OSCC specimens than those in the adjacent non-tumor tissues. Furthermore, our results indicated that curcumin inhibited OSCC cells (SCC-9 cells) proliferation through up-regulating miR-9 expression, and suppressing Wnt/β-catenin signaling by increasing the expression levels of the GSK-3β, phosphorylated GSK-3β and β-catenin, and decreasing the cyclin D1 level. Additionally, the up-regulation of miR-9 by curcumin in SCC-9 cells was significantly inhibited by delivering anti-miR-9 but not control oligonucleotides. Downregulation of miR-9 by anti-miR-9 not only attenuated the growth-suppressive effects of curcumin on SCC-9 cells, but also re-activated Wnt/β-catenin signaling that was inhibited by curcumin. Therefore, our findings would provide a new insight into the use of curcumin against OSCC in future. 相似文献
109.
Zohreh Firouzi Parisa Lari Marzieh Rashedinia Mohammad Ramezani Mehrdad Iranshahi Khalil Abnous 《Life sciences》2014
Aims
Curcumin is one of the most important constituent of Curcuma longa L. with antioxidant, anti-inflammatory and anticancer effects. In this study, we investigated potential intracellular targets of curcumin by affinity chromatography based on target deconvolution. Identification of curcumin interacting proteins may help in evaluating biological and side effects of this natural compound.Main methods
Curcumin was immobilized through a linker to sepharose beads as solid matrix. Pull down assay was performed by passing tissue lysate of mouse brain through the column to enrich and purify curcumin interacting proteins. Then proteins were separated using two-dimensional gel electrophoresis and identified using MALDI/TOF/TOF mass spectrometry.Key findings
Our results show that curcumin physically binds to a wide range of cellular proteins including structural proteins, metabolic enzymes and proteins involved in apoptosis pathway.Significance
Finding curcumin interacting proteins may help in understanding a part of curcumin pharmacological effects. 相似文献110.
《Bioorganic & medicinal chemistry》2014,22(15):4151-4161
Arachidonic acid and its metabolites have generated high level of interest among researchers due to their vital role in inflammation. The inhibition of enzymes involved in arachidonic acid metabolism has been considered as synergistic anti-inflammatory effect. A series of novel α,β-unsaturated carbonyl based compounds were synthesized and evaluated for their inhibitory activity on secretory phospholipase A2 (sPLA2), cyclooxygenases (COX), soybean lipoxygenase (LOX) in addition to proinflammatory cytokines comprising IL-6 and TNF-α. Six α,β-unsaturated carbonyl based compounds (2, 3, 4, 12, 13 and 14) exhibited strong inhibition of sPLA2 activity, with IC50 values in the range of 2.19–8.76 μM. Nine compounds 1–4 and 10–14 displayed inhibition of COX-1 with IC50 values ranging from 0.37 to 1.77 μM (lower than that of reference compound), whereas compounds 2, 10, 13 and 14 strongly inhibited the COX-2. The compounds 10–14 exhibited strong inhibitory activity against LOX enzyme. All compounds were evaluated for the inhibitory activities against LPS-induced TNF-α and IL-6 release in the macrophages. On the basis of screening results, five active compounds 3, 4, 12, 13 and 14 were found strong inhibitors of TNF-α and IL-6 release in a dose-dependent manner. Molecular docking experiments were performed to clarify the molecular aspects of the observed COX and LOX inhibitory activities of the investigated compounds. Present findings increases the possibility that these α,β-unsaturated carbonyl based compounds might serve as beneficial starting point for the design and development of improved anti-inflammatory agents. 相似文献