Marine Anticancer Agents: An Overview with a Particular Focus on Their Chemical Classes

The marine environment is a rich source of biologically active molecules for the treatment of human diseases, especially cancer. The adaptation to unique environmental conditions led marine organisms to evolve different pathways than their terrestrial counterparts, thus producing unique chemicals with a broad diversity and complexity. So far, more than 36,000 compounds have been isolated from marine micro- and macro-organisms including but not limited to fungi, bacteria, microalgae, macroalgae, sponges, corals, mollusks and tunicates, with hundreds of new marine natural products (MNPs) being discovered every year. Marine-based pharmaceuticals have started to impact modern pharmacology and different anti-cancer drugs derived from marine compounds have been approved for clinical use, such as: cytarabine, vidarabine, nelarabine (prodrug of ara-G), fludarabine phosphate (pro-drug of ara-A), trabectedin, eribulin mesylate, brentuximab vedotin, polatuzumab vedotin, enfortumab vedotin, belantamab mafodotin, plitidepsin, and lurbinectedin. This review focuses on the bioactive molecules derived from the marine environment with anticancer activity, discussing their families, origin, structural features and therapeutic use.     

Bioactive Compounds in Wild Asteraceae Edible Plants Consumed in the Mediterranean Diet

Plant Foods for Human Nutrition - Three wild edible plant species belonging to the Asteraceae family, Crepis vesicaria L. (s.l.), Sonchus asper (L.) Hill s.l., and Sonchus oleraceus L., usually...     

Algal Phlorotannins as Novel Antibacterial Agents with Reference to the Antioxidant Modulation: Current Advances and Future Directions

The increasing drug resistance of infectious microorganisms is considered a primary concern of global health care. The screening and identification of natural compounds with antibacterial properties have gained immense popularity in recent times. It has previously been shown that several bioactive compounds derived from marine algae exhibit antibacterial activity. Similarly, polyphenolic compounds are generally known to possess promising antibacterial capacity, among other capacities. Phlorotannins (PTs), an important group of algae-derived polyphenolic compounds, have been considered potent antibacterial agents both as single drug entities and in combination with commercially available antibacterial drugs. In this context, this article reviews the antibacterial properties of polyphenols in brown algae, with particular reference to PTs. Cell death through various molecular modes of action and the specific inhibition of biofilm formation by PTs were the key discussion of this review. The synergy between drugs was also discussed in light of the potential use of PTs as adjuvants in the pharmacological antibacterial treatment.     

Correction of ADA-SCID by stem cell gene therapy combined with nonmyeloablative conditioning

Hematopoietic stem cell (HSC) gene therapy for adenosine deaminase (ADA)-deficient severe combined immunodeficiency (SCID) has shown limited clinical efficacy because of the small proportion of engrafted genetically corrected HSCs. We describe an improved protocol for gene transfer into HSCs associated with nonmyeloablative conditioning. This protocol was used in two patients for whom enzyme replacement therapy was not available, which allowed the effect of gene therapy alone to be evaluated. Sustained engraftment of engineered HSCs with differentiation into multiple lineages resulted in increased lymphocyte counts, improved immune functions (including antigen-specific responses), and lower toxic metabolites. Both patients are currently at home and clinically well, with normal growth and development. These results indicate the safety and efficacy of HSC gene therapy combined with nonmyeloablative conditioning for the treatment of SCID.     

Dissection of antioxidant activity of durum wheat (Triticum durum Desf.) grains as evaluated by the new LOX/RNO method

Antioxidant activity (AA) of durum wheat (Triticum durum Desf.) grains was studied using the innovative LOX/RNO method, able to simultaneously detect different antioxidant mechanisms, and the TEAC assay, one of the most widely used assays. Insoluble-bound and free-soluble phenols, hydrophilic and lipophilic compounds were extracted from eight different whole flour samples; extracts were analyzed for AA and their content in several antioxidants. The LOX/RNO method measured very high AA values, with the highest ones [850–1500 μmol Trolox eq./g whole flour (dry weight)] for insoluble-bound phenolic extracts, highly correlated to total phenolic (r = 0.761, P < 0.001) and ferulic acid (r = 0.816, P < 0.001) contents. Hydrophilic and lipophilic extracts showed lower AA [70-140 and 40–60 μmol Trolox eq./g (dry weight), respectively], highly correlated to flavonoid (r = 0.583, P < 0.01) and protein (r = 0.602, P < 0.01), as well as β-tocotrienol (r = 0.684, P < 0.05) contents, respectively. Interestingly, the LOX/RNO method suggests that insoluble-bound phenolic compounds may exert very strong synergistic interactions within the extract. Contrarily, the TEAC assay did not correlate to any antioxidant content, resulted unable to highlight differences among samples, measured much lower AA values and did not suggest synergism. The use of the LOX/RNO method is useful to unearth new properties of phytochemicals from durum wheat grains, potentially giving health benefits.     

Adverse Effect of Antifouling Compounds on the Reproductive Mechanisms of the Ascidian Ciona intestinalis

Fertilization and embryo development that occur in sea water are sensitive to xenobiotics from anthropogenic sources. In this work, we evaluated the influence of two antifouling biocides, tributyltin (TBT) and diuron, on the reproductive mechanisms of the marine invertebrate Ciona intestinalis. By using electrophysiological techniques, we examined the impact of these compounds on the electrical properties of the mature oocytes and of events occurring at fertilization. With different toxicity assays, we studied the effect of the two biocides on the gametes by evaluating fertilization rate and embryo development. Results show that sodium (Na⁺) currents were significantly reduced by either of the two biocides, whereas conductance was significantly increased. The fertilization current frequency and amplitude, fertilization rate and larval development were affected only by TBT. This study suggests that: (i) the two biocides affect either the electrical properties of the oocyte plasma membrane and the reproductive success representing a risk factor for the survival of the species exposed to environmental pollution; (ii) the ascidian Ciona intestinalis may represent a good model organism to test toxicity of marine pollutants. Possible mechanisms of action of the two biocides are discussed.     

Medium Light and Medium Roast Paper-Filtered Coffee Increased Antioxidant Capacity in Healthy Volunteers: Results of a Randomized Trial

We compared the effects of medium light roast (MLR) and medium roast (MR) paper-filtered coffee on antioxidant capacity and lipid peroxidation in healthy volunteers. In a randomized crossover study, 20 volunteers consumed 482?±?61?ml/day of MLR or MR for four weeks. Plasma total antioxidant status (TAS), oxygen radical absorbance capacity (ORAC), oxidized LDL and 8-epi-prostaglandin F2α, erythrocyte superoxide dismutase (SOD), glutathione peroxidase (GPx), and catalase (CAT) activity were measured at baseline and after the interventions. MLR had higher chlorogenic acids-(CGA; 334?mg/150?mL) and less caffeine (231?mg/150?ml) than MR had (210 and 244?mg/150?ml, respectively). MLR also had fewer Maillard reaction products (MRP) than MR had. Compared with baseline, subjects had an increase of 21 and 26?% in TAS, 13 and 13?% in CAT, 52 and 75?% in SOD, and 62 and 49?% in GPx after MLR and MR consumption (P?相似文献   

冰糖橙果实品质无损伤在线检测分级技术的建立与应用

【目的】冰糖橙果实外观分级与内部品质不一致极大地影响了其市场声誉,建立冰糖橙果实品质分级标准和果实快速规模化无损伤品质检测分级技术,并进行在线应用,为快速分选不同糖酸度冰糖橙产品提供技术支持。【方法】在利用常规果实品质分析方法对主产区的冰糖橙果实进行多年品质分析的基础上,找出果实外观和内在品质的相关性,确定不同果型横径与糖酸度含量的关系,形成冰糖橙果实分级标准。在此基础上,采集710-960 nm波段近红外透射光谱建立果实无损伤检测模型,利用常规品质分析数据对原始光谱反复进行校正并验证,确定无损伤检测的准确性,并在分级线上进行应用;调查统计应用无损伤检测生产线分级后各级冰糖橙的产量、销售单价和销售额。【结果】（1）根据果实横径大小进行初选分级,68-74 mm为大果型,62-67 mm为中果型,56-61 mm为小果型,再按果实的糖度（可溶性固形物Brix度）和酸度不同将冰糖橙划分为4个等级：糖度≥14、酸度≤0.4%为特级果;12≤糖度＜14、酸度≤0.4%为一等果;糖度≥14、0.6%≥酸度＞0.4%为二等果;糖度＜12、酸度≤0.4%为合格果。通过反复矫正,建立了冰糖橙果实品质分级标准。（2）通过多次进行单果糖度和酸度的分析矫正,建立了冰糖橙果实糖度和酸度的检验线。第1次建立的冰糖橙糖度检量线检测范围为10.1-14.9 Brix,再利用常规品质分析验证无损伤检测结果,合格率仅为26%。第2次建立的糖度检量线延长高糖检测范围,为10.1-16.2 Brix,经验证后合格率达90%。第3次建立的糖度检量线扩大低糖检测范围,为9.8-16.2 Brix,经验证后合格率为90%。第1次建立的冰糖橙酸度检量线检测范围为0.1%-1.26%,再利用常规品质分析验证无损伤检测结果,合格率仅为64%。第2次建立的酸度检量线延长高酸检测范围,为0.1%-1.37%,经验证后合格率达94%。第3次建立的酸度检量线继续扩大高酸检测范围,为0.1%-1.53%,经验证后合格率为92%。（3）新建立无损伤糖酸度校正和验证模型,糖度有效检测范围为8.7-15.1 Brix,酸度有效检测范围为0.14%-2.0%,经验证后糖度合格率达到98%,酸度合格率为98%。应用该分级技术,分选速度达到10个冰糖橙/秒,品质分级后最高单价48元/kg,年产量4 500 t,实现产值9 122万元。【结论】研究结果预测糖酸度准确,测量范围全面涵盖冰糖橙商品果的糖酸度,能大批量、快速、高质量和无损伤在线鉴别冰糖橙果实内在品质,结合外观品质分级标准,分选出内外品质均一的产品。