海洋动物功能蛋白及活性肽研究进展

海洋动物中含有丰富的蛋白质、多糖、多肽、脂肪酸等活性物质，具有来源丰富、功能多样、活性显著、毒副作用小等优点，已经成为当前医药卫生和功能食品研究的热点。本文主要对海洋动物来源的抗氧化、抗菌、抗肿瘤和免疫调节等活性的功能蛋白和多肽进行综述，介绍其可能的作用机制，并就海洋生物功能蛋白及活性肽开发利用前景作出展望。     

缩酚酸肽类化合物的研究进展

缩酚酸肽(depsipeptide)是一类天然产物活性物质,包含酯键的一类多肽,具有抗菌、抗肿瘤、抗病毒、抗疟和抗血栓等生物活性。本文综述了缩酚酸肽类化合物的来源、生物活性、作用机制以及临床研究等信息,并展望缩酚酸肽类药物研究开发的前景。     

抗肿瘤活性多肽的研究现状

由于发病率和死亡率的逐年攀升,恶性肿瘤目前成为威胁人类健康的重大疾病,对于恶性肿瘤的高效治疗已成为医学领域的研究热点。随着小分子化学药物开发难度的增大,具有高效低毒等诸多优点的活性多肽开始受到重视,相关药物市场也不断扩大。本文通过对抗肿瘤活性多肽的特点与来源、制备技术、结构修饰、作用机制及研发现状等方面进行综述,为后续的研究工作提供参考。     

海洋天然抗肿瘤活性产物的临床研究现状

海洋特殊的生态系统是天然抗肿瘤活性物质的重要来源之一,许多源于海洋生物的抗肿瘤活性化合物已经进入临床研究阶段。简要介绍海洋天然抗肿瘤活性产物的作用机制,综述新近发现的海洋天然抗肿瘤活性化合物的最新临床研究进展。     

多肽抗肿瘤化合物的研究进展

恶性肿瘤是目前严重威胁人类生命健康的疾病之一。化疗作为肿瘤治疗的传统手段,存在有选择性低、毒副作用大、多药耐药等缺陷。然而,多肽作为抗肿瘤化合物具有高选择性、低毒性、不产生耐药性的优点。这使得多肽有希望成为新型的抗肿瘤药物之一。本文综述了各种具有抗肿瘤活性的肽类化合物,并简要阐述其作用机制。     

五环三萜羽扇豆烷型天然产物抗肿瘤活性研究进展

天然产物是抗肿瘤药物的重要来源。三萜化合物是植物体内重要的次生代谢产物,具有广泛的生物活性,其中五环三萜羽扇豆烷型天然产物对多种肿瘤细胞生长均表现出很强地抑制活性,同时由于毒性较低且作用机制独特,使其成为优秀的抗肿瘤先导化合物。近年来,针对羽扇豆烷型天然产物的抗肿瘤机制研究越发深入,对其结构进行衍生化从而提升活性、改善成药性的研究也越来越多。本文综述了五环三萜中白桦酸、23-羟基白桦酸、桦木醇和羽扇豆醇4个天然活性化合物的来源、抗肿瘤活性、作用机制及结构衍生化等方面国内外的研究进展。     

抗肿瘤多肽研究进展

抗肿瘤活性多肽由于具有相对分子质量小、活性高、毒性低等特点,在肿瘤的临床治疗上有重要的价值。此文按照多肽的来源综述了目前国内外对于一些新的具有抗肿瘤活性的多肽的研究现状。     

异戊烯基口占吨酮类天然产物的抗肿瘤活性研究进展

近年来有研究显示,含有异戊烯基结构的天然咕吨酮类化合物对多种肿瘤具有显著抑制活性,故而从此类化合物中寻找具有开发价值的抗肿瘤先导化合物,已成为一个研究热点。按来源分别介绍异戊烯基咕吨酮类天然化合物及其抗肿瘤活性研究新进展,并对其中部分化合物的作用机制及构效关系进行了初步探讨。     

白术抗肿瘤活性成分及其抗肿瘤机制研究进展

白术,来源于菊科植物白术(Atractylodes macrocephala Koidz)的干燥根茎。白术活性成分对胃癌、肝癌、肺癌、食管癌、卵巢癌、结直肠癌、宫颈癌等肿瘤细胞显示出广泛的抗肿瘤活性,其主要作用机制涉及以下几个方面:诱导肿瘤细胞凋亡,抑制肿瘤细胞增殖,抑制肿瘤细胞迁移、侵袭和转移,调节肿瘤微环境和调控机体免疫功能等。对白术的研究一直是天然药物和药理学领域的热点之一,随着研究的深入,对白术抗肿瘤活性成分及其抗肿瘤作用机制的研究也不断地丰富,因此,该综述对白术抗肿瘤有效活性成分及其作用机制进行归纳总结,以期为白术抗肿瘤作用的深入研究提供夯实的理论基础和科学依据。     

膜活性多肽(MAPs)的抗菌活性及其作用机制的研究进展

膜活性多肽(MAPs)是一类具有较好抗菌活性的抗菌肽。作为先天宿主防御分子,广泛的分布于细菌、植物、无脊椎动物、脊椎动物中。膜活性多肽具有抗菌肽的结构特征,肽链通常较短,带正电荷,具有两亲性的α-螺旋或β-折叠结构,通过破坏膜的通透性杀死细菌、真菌和部分肿瘤细胞。膜活性多肽在细胞膜或细胞内部存在特定的分子靶点,并因其独特的作用机制而成为一种新型的肽类抗生素。本文主要对膜活性多肽的抗菌活性及其作用机制的研究现状和发展情况做一综述。     

丹皮酚抗肿瘤作用机制的研究进展

丹皮酚是牡丹皮的主要活性成分,其抗肿瘤作用的研究已经受到广泛关注。研究报道了丹皮酚对肝癌、胃癌、乳腺癌、卵巢癌等多种肿瘤均具有抗癌作用。丹皮酚主要通过抑制肿瘤细胞增殖,影响肿瘤细胞周期,调控凋亡相关因子及相关通路,抑制肿瘤细胞转移,逆转化疗药物耐药性及放疗增敏发挥抗肿瘤作用。主要综述了丹皮酚抗肿瘤作用机制的最新研究进展。目前丹皮酚抗肿瘤的研究仍处在初步阶段,还需进一步加强对信号转导通路、调控靶点、抑癌基因、联合用药及体内实验等方面的研究。     

Antitumor activity of extracts and compounds from the skin of the toad Bufo bufo gargarizans Cantor

The skin of the toad Bufo bufo gargarizans Cantor is known to be rich in bufadienolides, peptides and alkaloids. It has been found to be a source of some extracts and biologically active compounds with antitumor activity. Cinobufacini (Huachansu), a Chinese medicine prepared from the dried toad skin, has been widely used in clinical therapy for various cancers in China. Bufadienolides, such as bufalin, cinobufagin, resibufogenin, and telocinobufagin, are the major active compounds derived from the toad skin. They are the maker biologically active compounds of cinobufagin while the antitumor activity of cinobufagin may be due to this kind of components. Experimental research has suggested that cinobufacini and its active compounds (e.g. bufalin and cinobufagin) exhibit significant antitumor activity, including inhibition of cell proliferation, induction of cell differentiation, induction of apoptosis, disruption of the cell cycle, inhibition of cancer angiogenesis, reversal of multi-drug resistance, and regulation of the immune response. Clinical data have indicated that cinobufacini may have effective anticancer activity with low toxicity and few side effects. Data to date suggest it may also enhance quality of life for patients with cancer. Thus, this review briefly summarizes recent studies on the anticancer activity of cinobufacini and some of its active compounds from the skin of the toad Bufo bufo gargarizans Cantor. This might provide additional evidence for further study of the extracts and active compounds from the toad skin in cancer treatment.     

Application of reproductive hormone peptides for tumor targeting

Targeted therapy may be a promising approach against cancer because its focus of attention is to enhance the efficacy and to reduce the side effects of antitumor agents through high selectivity. One of targeted strategies is to use tumor-specific ligands as targeting moieties to carry drugs into tumor cells, and use the receptors that expressed on tumor cells as target sites to bind with peptide ligands. The fact that the distributions of reproductive hormone receptors are relatively limited in normal tissues makes it possible to use them as targeted sites and use hormone peptides as targeting moieties for cancer treatment. Until now many tumor targeting approaches with reproductive hormone peptides have been developed, and some of them have been introduced into clinical trials. Here a review is given to discuss the targeted antitumor therapeutic strategies based on gonadotropin-releasing hormone, follicle-stimulating hormones, luteinizing hormone, human chorionic gonadotropin and their receptors.     

Recent developments in taxane drug delivery

Paclitaxel (taxol, 1a) and docetaxel (taxotere, 1b) have established themselves as an important class of antitumor drugs currently available to the oncologist. While the great contribution of these drugs to the management of the disease and their effect on the improvement of the patient quality of life could not be overemphasized, a great deal of research has been ongoing to improve two key pharmacologic factors, antitumor activity and systemic toxicity. Both physical and chemical means have been employed towards the enhancement of antitumor activity and at the same time, lowering the inherent toxicity and side effects of these drugs. This mini-review compiles the recent reported works on the design and development of taxane delivery systems through tumor cell surface receptor-targeted delivery mechanisms such as small-molecule peptides and monoclonal antibodies, as well as those on non-targeted procedures such as liposomes, nanostructures, and natural and synthetic polymers.     

多靶点抗肿瘤天然产物研究进展

天然产物及其衍生物是抗肿瘤药物的重要组成部分.目前在临床上应用的天然产物来源的抗肿瘤药物以传统细胞毒类药物或靶向某一特定靶点的分子靶向药物为主,其应用受限于药物相关不良反应和肿瘤耐药.近年的研究表明,抗肿瘤活性天然产物往往能够靶向肿瘤细胞的多个靶点,影响肿瘤发生发展中的多个过程.由于肿瘤是一种多因素诱发的系统性疾病,多...     

烯二炔类抗肿瘤抗生素及其靶向药物研究近况

烯二炔类抗生素是一种结构新颖、作用机制独烯二炔结构是其活性中心。该类抗生素具有极强的抗肿瘤活性却因毒性较大难以直接用于临床。近年来,研究人员展开了烯二炔类抗生素靶向药物的研发工作,以提高其肿瘤靶向性并减少药物毒副作用。归纳总结了已报道的天然来源的烯二炔类抗肿瘤抗生素及其活性代谢物,并重点介绍烯二炔类抗生素相关靶向药物的研究进展,旨在为其深度开发提供参考。     

Induction of apoptosis in human leukemia K-562 and gastric carcinoma SGC-7901 cells by salvicine, a novel anticancer compound

Salvicine (a novel diterpenoid quinone compound) exhibited a marked antitumor activity on human solid tumor cell lines and BALB/c-nu human carcinoma xenografts in our earlier studies, and it has been chosen as a candidate anticarcinogenic compound in the preclinical research stage. The present study was undertaken in order to observe whether or not the antitumor effect of salvicine is associated with its ability to induce apoptosis. Our results show that salvicine is capable of inhibiting cell proliferation and inducing characteristic changes of apoptosis in both human leukemia K-562 and gastric carcinoma SGC-7901 cells. These effects are dose and time dependent. The results of this study strongly suggest that the antitumor effect of salvicine is associated with its ability to induce apoptosis. Meanwhile, this study also shows that the activity of salvicine against K-562 and SGC-7901 cells is similar with regards to both growth inhibition and apoptosis induction, further indicating that salvicine causes these particular effects on solid tumor cells.     

白藜芦醇抗肿瘤药理作用机制研究进展

白藜芦醇是一种天然单体化合物,属于非黄酮类的多酚化合物,存在于多种植物中。现代药理研究发现,白藜芦醇具有抗炎、抗氧化、抗肿瘤、调节代谢与机体免疫等药理活性。白藜芦醇对结肠癌、胰腺癌、卵巢癌、乳腺癌等多种肿瘤细胞均有抑制作用,其抗肿瘤作用逐渐成为研究热点。白藜芦醇可以通过抑制肿瘤细胞的增殖、诱导肿瘤细胞凋亡、抑制肿瘤细胞侵袭和转移、调节机体免疫功能、直接作用于相关靶点等发挥抗肿瘤活性。就白藜芦醇在不同肿瘤细胞中发挥的抗肿瘤作用及其机制进行综述,以期为抗肿瘤新药的研发提供参考依据。     

射干抗肿瘤的研究现状

射干是鸢尾科射干属植物射干Belamcanda chinensis(L.)DC.的干燥根茎,是一种具有免疫调节作用及抑制肿瘤生长的传统中药.基础研究与临床应用已证实其抗癌效果.本文就射干单体化合物、粗提物以及复方药剂3个方面的抗肿瘤活性以及减轻药物不良反应的研究进展进行综述,其抗肿瘤的主要机制可能是通过对细胞周期、免疫...