Nutritional Sources and Anticancer Potential of Phenethyl Isothiocyanate: Molecular Mechanisms and Therapeutic Insights

Phenethyl isothiocyanate (PEITC), a compound derived from cruciferous vegetables, has garnered attention for its anticancer properties. This review synthesizes existing research on PEITC, focusing on its mechanisms of action in combatting cancer. PEITC has been found to be effective against various cancer types, such as breast, prostate, lung, colon, and pancreatic cancers. Its anticancer activities are mediated through several mechanisms, including the induction of apoptosis (programmed cell death), inhibition of cell proliferation, suppression of angiogenesis (formation of new blood vessels that feed tumors), and reduction of metastasis (spread of cancer cells to new areas). PEITC targets crucial cellular signaling pathways involved in cancer progression, notably the Nuclear Factor kappa-light-chain-enhancer of activated B cells (NF-κB), Protein Kinase B (Akt), and Mitogen-Activated Protein Kinase (MAPK) pathways. These findings suggest PEITC's potential as a therapeutic agent against cancer. However, further research is necessary to determine the optimal dosage, understand its bioavailability, and assess potential side effects. This will be crucial for developing PEITC-based treatments that are both effective and safe for clinical use in cancer therapy.     

Conjugation with Phospholipids as a Modification Increasing Anticancer Activity of Phenolic Acids in Metastatic Melanoma—In Vitro and In Silico Studies

Phenolic acids possess many beneficial biological activities, including antioxidant and anti-inflammatory properties. Unfortunately, their low bioavailability restricts their potential medical uses, as it limits the concentration of phenolic acids achievable in the organism. The conjugation with phospholipids constitutes one of the most effective strategies to enhance compounds bioavailability in biological systems. In the present study, the conjugates of anisic (ANISA) and veratric acid (VA) with phosphatidylcholine (PC) were investigated. Since both ANISA and VA are inhibitors of tyrosinase, a melanocyte enzyme, the expression of which increases during tumorigenesis, anticancer potential of the conjugates was tested in several metastatic melanoma cell lines. The conjugates proved to be antiproliferative, apoptosis-inducing and cell-cycle-affecting agents, selective for cancerous cells and not affecting normal fibroblasts. The conjugates substituted by ANISA and VA, respectively, at both the sn-1 and sn-2 positions of PC, appeared the most promising, since they were effective against the vast majority of metastatic melanoma cell lines. Additionally, the conjugation of phenolic acids to PC increased their antioxidant activity. Molecular modeling was employed for the first time to estimate the features of the investigated conjugates relevant to their anticancer properties and membrane permeation. Again, the conjugates substituted by phenolic acid at both the sn-1 and sn-2 positions of PC seemed to be presumably most bioavailable.     

Synthesis, structure, and in vitro antitumor activity of some glycoside derivatives of ferrocenyl-chalcones and ferrocenyl-pyrazolines

Some new glycosides of 3-ferrocenyl-1-(4'-hydroxyphenyl)-prop-2-en-1-one were prepared and transformed into the corresponding pyrazoline and pyrazole derivatives. Using methyl-hydrazine, formation of regioisomers was observed. DDQ was found to be a mild and efficient reagent for the pyrazoline-pyrazole dehydroaromatization process. The structure of the new compounds was proved by IR and NMR spectroscopy. The in vitro antitumor activity of the substances was investigated against human leukemia (HL-60) cells by the MTT method. Among these new compounds some chalcone derivatives (3 a, 3 b, 5 a, and 5 b) showed attractive in vitro antitumor effects on human leukemia cells. These molecules contained ferrocenyl moieties and a p-hydroxy-phenolic ring or a size-independent apolar substitution of that.     

细香葱提取物对人胃癌细胞SGC7901抑制作用

通过四甲基偶氮唑蓝比色法和流式细胞术研究不同细香葱提取物对人胃癌细胞SGC7901增殖的抑制作用及其对细胞周期、凋亡率的影响。结果显示,细香葱抗胃癌活性成分主要集中在75%乙醇提取部位,同一区域不同品种细香葱抑制胃癌细胞增殖作用存在显著性差异(P0.05),其中3号细香葱75%乙醇提取物的抑制作用最强,其24、48、72 h时IC50值分别为(0.88±0.07)、(0.45±0.08)、(0.21±0.03)mg/m L;SGC7901细胞经1.0、2.0 mg/m L的细香葱75%乙醇提取物处理48 h后,S期细胞所占比例显著增多(P0.05),细香葱75%乙醇提取物阻碍人胃癌细胞SGC7901由S期向G2期的转化,将细胞周期阻滞于S期;同时,实验组细胞相比对照组凋亡率显著上升(P0.05),存在量效关系。综上,细香葱75%乙醇提取物能够阻滞人胃癌细胞SGC7901由S期向G2期转化、促进其凋亡并抑制细胞增殖,细香葱具有开发成为抗胃癌功能食品的潜力。     

红阳猕猴桃多糖组分的分离纯化、单糖组成及其抑制癌细胞活性

研究红阳猕猴桃果实多糖组分的分离纯化、单糖组成及其对癌细胞增殖的抑制作用。用水提取总多糖,层析法分离纯化多糖组分;高效凝胶渗透色谱测定组分的纯度和分子质量;高效液相色谱法测定多糖纯组分的单糖组成;傅里叶变换红外(Fourier transform-infrared,FT-IR)光谱鉴定多糖纯组分的特征官能团;用3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐法测定多糖纯组分对肺癌、乳腺癌、肝癌、胃癌和结肠癌这5种癌细胞的体外抑制活性。总多糖分离出ACP-1、ACP-2、ACP-3、ACP-4这4种单组分多糖;其中ACP-3纯度最高,分子质量为2 663 k D,主要含有L-鼠李糖(17.78%,物质的量分数,后同)、D-半乳糖醛酸(25.25%)、D-半乳糖(25.45%)、L-阿拉伯糖(20.51%)、D-葡萄糖(6.14%)、D-甘露糖(2.13%)、D-木糖(1.03%)、D-葡萄糖醛酸(0.97%)及少量D-岩藻糖(0.74%);其FT-IR光谱图有多糖特征官能团的吸收峰。ACP-3对5种癌细胞增殖的半数最大抑制浓度依次为0.646、0.310、0.642、0.281、0.575μmol/L,对癌细胞增殖有抑制活性。     

榛花粉不同提取物组分抗癌症活性研究

以榛花粉为原材料,首先利用乙醇浸泡榛花粉得到乙醇提取物,然后分别利用不同溶剂对榛花粉乙醇提取物进行萃取得到不同组分,利用MTT比色法测量榛花粉各提取组分对胃癌细胞(AGS)和肝癌细胞(SK-Hep1)生长的体外抑制作用.实验结果表明:榛花粉各提取组分对胃癌细胞均具有很好的抑制作用,对肝癌细胞的抑制活性较低,其中二氯甲烷组分对癌症细胞的抑制活性均高于其他各组分.     

Novel lysosome-targeted anticancer fluorescent agents used in zebrafish and nude mouse tumour imaging

The design of three novel fatty nitrogen mustard-based anticancer agents with fluorophores incorporated into the alkene structure(CXL 118,CXL121,and CXL122)is described in this report.The results indicated that these compounds are selectively located in lysosomes and exhibit effective antitumour activity.Notably,these compounds can directly serve as both reporting and imaging agents in vitro and in vivo without the need to add other fluorescent tagging agents.     

Allene as an alternative functional group for drug design: effect of C--C multiple bonds conjugated with quinazolines on the inhibition of EGFR tyrosine kinase

A series of allenic quinazolines were synthesized as receptor tyrosine kinase inhibitors by using a simple protocol for palladium-catalyzed allene transformation. Among the compounds synthesized, two allenic 4-anilinoquinazolines selectively suppressed epidermal growth factor receptor (EGFR) tyrosine kinase activity in vitro. According to immunoblot analysis, the allenic quinazolines inhibited the EGF-mediated phosphorylation of EGFR and its downstream kinases in A431 cells. Furthermore, one of these allenic quinazolines decreased the proliferation of A431 cells through the induction of cell-cycle arrest and apoptosis.