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Harnessing the power of Arctium lappa root: a review of its pharmacological properties and therapeutic applications 利用牛蒡根的力量:药理特性和治疗应用综述。
IF 4.8 3区 化学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-08-20 DOI: 10.1007/s13659-024-00466-8
Mukul Shyam, Evan Prince Sabina

Arctium lappa, widely recognized as burdock, is a perennial plant that is employed in the realm of traditional Chinese medicine for a wide range of medicinal applications. The herb is rich in bioactive metabolites with therapeutic potential, encompassing polyphenolic antioxidants in its leaves, and flavonoids and fructo-oligosaccharides in its underground parts. Nutraceuticals originating from botanical sources such as Arctium lappa provide supplementary health advantages alongside their nutritional content and have demonstrated effectiveness in the prevention and management of specific ailments. The utilization of Arctium lappa root extract has exhibited encouraging outcomes in addressing hepatotoxicity induced by cadmium, lead, chromium, and acetaminophen, ameliorating liver damage and oxidative stress. Additionally, the root extract displays properties such as antidiabetic, hypolipidemic, aphrodisiac, anti-rheumatic, anti-Alzheimer, and various other pharmacological actions.

Graphical abstract

牛蒡(Arctium lappa)被广泛认为是牛蒡,是一种多年生植物,在传统中药领域具有广泛的药用价值。牛蒡富含具有治疗潜力的生物活性代谢物,叶片中含有多酚抗氧化剂,地下部分含有类黄酮和果寡糖。源自牛蒡等植物资源的保健食品除营养成分外,还具有补充保健的优势,在预防和治疗特定疾病方面已证明十分有效。在解决镉、铅、铬和对乙酰氨基酚引起的肝毒性方面,使用牛蒡根提取物已取得令人鼓舞的成果,可改善肝损伤和氧化应激。此外,牛蒡根提取物还具有抗糖尿病、降血脂、壮阳、抗风湿、抗老年痴呆等多种药理作用。
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引用次数: 0
Biotransformation of selected secondary metabolites by Alternaria species and the pharmaceutical, food and agricultural application of biotransformation products Alternaria 物种对某些次级代谢物的生物转化以及生物转化产物在制药、食品和农业方面的应用。
IF 4.8 3区 化学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-08-19 DOI: 10.1007/s13659-024-00469-5
Babalwa Tembeni, Olusola Emmanuel Idowu, Rachid Benrkia, Salima Boutahiri, Opeyemi Joshua Olatunji

Biotransformation is a process in which molecules are modified in the presence of a biocatalyst or enzymes, as well as the metabolic alterations that occur in organisms from exposure to the molecules. Microbial biotransformation is an important process in natural product drug discovery as novel compounds are biosynthesised. Additionally, biotransformation products offer compounds with improved efficacy, solubility, reduced cytotoxic and allows for the understanding of structure activity relationships. One of the driving forces for these impeccable findings are associated with the presence of cytochrome P450 monooxygenases that is present in all organisms such as mammals, bacteria, and fungi. Numerous fungal strains have been used and reported for their ability to biotransform different compounds. This review focused on studies using Alternaria species as biocatalysts in the biotransformation of natural product compounds. Alternaria species facilitates reactions that favour stereoselectivity, regioselectivity under mild conditions. Additionally, microbial biotransformation products, their application in food, pharmaceutical and agricultural sector is discussed in this review.

Graphical Abstract

生物转化是分子在生物催化剂或酶的作用下发生改变的过程,也是生物体因接触分子而发生新陈代谢改变的过程。微生物生物转化是天然产物药物发现的一个重要过程,因为新型化合物是通过生物合成产生的。此外,生物转化产物还能提高化合物的药效、溶解性,降低细胞毒性,并有助于了解结构与活性的关系。这些无懈可击的发现的推动力之一与细胞色素 P450 单氧化酶的存在有关,这种酶存在于哺乳动物、细菌和真菌等所有生物体内。许多真菌菌株都被用于生物转化不同化合物,并有相关报道。本综述重点介绍利用交链孢属真菌作为生物催化剂对天然产物化合物进行生物转化的研究。在温和的条件下,Alternaria 菌可促进有利于立体选择性和区域选择性的反应。此外,本综述还讨论了微生物生物转化产品及其在食品、制药和农业领域的应用。
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引用次数: 0
Polysaccharide fraction from Triplostegia glandulifera Wall and its renoprotective effect in streptozotocin-induced diabetic mice by attenuating oxidative stress 从三叶一枝花壁中提取的多糖成分及其通过减轻氧化应激对链脲佐菌素诱导的糖尿病小鼠的肾保护作用。
IF 4.8 3区 化学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-08-19 DOI: 10.1007/s13659-024-00467-7
Hai-Hui Guo, Lei Wu, Dan Mi, Xing-Yu Zhang, Fu-Mei He, Ting Lei, Fu-Sheng Wang

Triplostegia glandulifera Wall (T. glandulifera) is an ethnomedicine commonly used by ethnic minorities in Yunnan, China, to treat kidney disease. However, there are few reports on the renoprotective effects of this substance, and the active ingredients remain unclear. In this study, we extracted the polysaccharide fractions TGB and TGC using the water extraction-alcohol precipitation method and determined their molecular weight (Mw) and monosaccharide composition. The study investigated the protective effects of TGB and TGC fractions against diabetic nephropathy (DN) using an in vitro high glucose-induced HRMCs model and an in vivo STZ-induced diabetic mouse model. HPLC analysis revealed that TGB contained D-galacturonic acid, D-glucose, D-galactose, and D-arabinose, and had a lower Mw than TGC. In vitro, TGB showed concentration-dependent antioxidant activity and effectively reduced abnormal proliferation and while attenuating oxidative stress in HRMCs. In mice with diabetes, TGB corrected the dysregulation of glucose-lipid metabolism and alleviated oxidative stress in the kidneys. Additionally, it improved renal function and reduced renal tissue damage. The study suggests that the low Mw polysaccharides (TGB) have better activity against DN through the antioxidative stress mechanism.

Graphical Abstract

滇贝母(Triplostegia glandulifera Wall,T. glandulifera)是中国云南少数民族常用来治疗肾病的一种民族药。然而,有关这种物质的肾脏保护作用的报道很少,其有效成分也不清楚。本研究采用水提取-酒精沉淀法提取了多糖组分 TGB 和 TGC,并测定了它们的分子量(Mw)和单糖组成。研究采用体外高糖诱导 HRMCs 模型和体内 STZ 诱导的糖尿病小鼠模型,考察了 TGB 和 TGC 部分对糖尿病肾病(DN)的保护作用。HPLC 分析表明,TGB 含有 D-半乳糖醛酸、D-葡萄糖、D-半乳糖和 D-阿拉伯糖,其 Mw 低于 TGC。在体外,TGB 具有浓度依赖性抗氧化活性,能有效减少 HRMC 的异常增殖,同时减轻其氧化应激。在糖尿病小鼠体内,TGB 能纠正糖脂代谢失调,减轻肾脏的氧化应激。此外,它还能改善肾功能,减少肾组织损伤。该研究表明,低 Mw 多糖(TGB)通过抗氧化应激机制具有更好的抗 DN 活性。
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引用次数: 0
Natural and revolutionary tumor-specific T-cell therapy 天然、革命性的肿瘤特异性 T 细胞疗法。
IF 4.8 3区 化学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-08-19 DOI: 10.1007/s13659-024-00472-w
Zhi Dai, Xue-Meng Liu, Yun-li Zhao, Li-Xing Zhao, Xiao-Dong Luo

Recently the FDA conducted a risk investigation and labeled the Boxed Warning for all BCMA- and CD19-directed CAR-T cell therapy, so does it mean that the public must take risk of secondary cancer to receive cell therapy? Here, without lentivirus and professional antigen presenting cell application, a novel tumor-specific T-cell therapy was successfully developed only by co-culturing MHC+ cancer cells and Naïve-T cells under the CD28 co-stimulatory signals. These tumor-specific T-cells could be separated through cell size and abundantly produced from peripheral blood, and would spontaneously attack target cells that carrying the same tumor antigen while avoiding others in vitro test. Moreover, it markedly decreased 90% tumor nodules companying with greatly improving overall survival (76 days vs 30 days) after twice infusion back to mice. This work maximally avoided the risks of secondary cancer and non-specific killing, and might open a revolutionary beginning of natural tumor-specific T-cell therapy.

Graphical Abstract

最近,美国食品药品管理局(FDA)对所有BCMA和CD19导向的CAR-T细胞疗法进行了风险调查并标注了 "警示框",这是否意味着公众接受细胞疗法必须承担继发性癌症的风险呢?在这里,在没有慢病毒和专业抗原提呈细胞应用的情况下,仅通过在CD28共刺激信号下将MHC+癌细胞和Naïve-T细胞共培养,就成功开发出了一种新型的肿瘤特异性T细胞疗法。这些肿瘤特异性 T 细胞可通过细胞大小进行分离,并从外周血中大量产生,在体外试验中会自发攻击携带相同肿瘤抗原的靶细胞,而不攻击其他细胞。此外,它还显著减少了 90% 的肿瘤结节,并大大提高了小鼠两次输注后的总生存期(76 天对 30 天)。这项工作最大限度地避免了继发性癌症和非特异性杀伤的风险,可能会为肿瘤特异性 T 细胞自然疗法开创一个革命性的开端。
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引用次数: 0
Silvaticusins A–D: ent-kaurane diterpenoids and a cyclobutane-containing ent-kaurane dimer from Isodon silvaticus Silvaticusins A-D:Isodon silvaticus 中的ent-kaurane diterpenoids 和一种含环丁烷的 ent-kaurane dimer。
IF 4.8 3区 化学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-08-15 DOI: 10.1007/s13659-024-00465-9
Qi-Xiu Hai, Kun Hu, Su-Ping Chen, Yang-Yang Fu, Xiao-Nian Li, Han-Dong Sun, Hong-Ping He, Pema-Tenzin Puno

Three new ent-kaurane diterpenoids, silvaticusins A–C (13), along with a new ent-kaurane dimer silvaticusin D (4) were isolated from the aerial parts of Isodon silvaticus. The structures of these new compounds were established mainly by comprehensive analysis of their NMR and MS data. The absolute configuration of compounds 1 and 4 were determined using a single-crystal X-ray diffraction and computational methods, respectively. Compounds 2 and 3 were found to exhibit remarkable cytotoxic effects against five human tumor cell lines (HL-60, A-549, SMMC-7721, MDA-MB-231, and SW-480), with IC50 values spanning from 1.27 ± 0.08 to 7.52 ± 0.33 μM.

Graphical Abstract

从 Isodon silvaticus 的气生部分分离出了三种新的ent-kaurane 二萜类化合物 silvaticusins A-C (1-3),以及一种新的ent-kaurane 二聚体 silvaticusin D (4)。这些新化合物的结构主要是通过对其核磁共振和质谱数据的综合分析而确定的。利用单晶 X 射线衍射和计算方法分别确定了化合物 1 和 4 的绝对构型。研究发现,化合物 2 和 3 对五种人类肿瘤细胞系(HL-60、A-549、SMMC-7721、MDA-MB-231 和 SW-480)具有显著的细胞毒性作用,IC50 值从 1.27 ± 0.08 到 7.52 ± 0.33 μM。
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引用次数: 0
Xiaoyankangjun tablet alleviates dextran sulfate sodium-induced colitis in mice by regulating gut microbiota and JAK2/STAT3 pathway 小安康君片通过调节肠道微生物群和JAK2/STAT3通路缓解右旋糖酐硫酸钠诱导的小鼠结肠炎
IF 4.8 3区 化学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-08-12 DOI: 10.1007/s13659-024-00468-6
Suqin Yang, Jingtao Huang, Wenjing Tan, Xiankun Xia, Dali Gan, Yalei Ren, Hanwen Su, Meixian Xiang

Xiaoyankangjun tablet (XYKJP) is a traditional Chinese medicine formulation used to treat intestinal disorders in clinical practice. However, the specific therapeutic mechanism of action of XYKJP in colitis has not yet been elucidated. This study aimed to reveal the multifaceted mechanisms of action of XYKJP in treating colitis. The model established based on DSS-induced colitis in C57BL/6 mice was employed to estimate the effect of XYKJP on colitis, which was then followed by histological assessment, 16S rRNA sequencing, RT-qPCR, ELISA, and Western blot. XYKJP alleviated the symptoms of DSS-induced colitis mainly by reducing oxidative stress, inflammatory responses, and intestinal mucosal repair in colitis tissues. In addition, XYKJP regulated the intestinal flora by increasing the relative abundance of Akkermansia and Bifidobacterium and reducing the relative abundance of Coriobacteriaceae_UCG-002. Mechanistically, XYKJP increased the content of short-chain fatty acids (SCFAs) in the feces, particularly propanoic acid and butyric acid, activated their specific receptor GPR43/41, furthermore activated the Nrf2/HO-1 pathway, and suppressed the JAK2/STAT3 pathway. XYKJP significantly alleviated the symptoms of experimental colitis and functioned synergistically by regulating the intestinal flora, increasing the production of SCFAs, and activating their specific receptors, thereby repressing oxidative stress and inflammation.

Graphical Abstract

小阳康君片(XYKJP)是一种传统中药配方,临床上用于治疗肠道疾病。然而,XYKJP 对结肠炎的具体治疗作用机制尚未阐明。本研究旨在揭示 XYKJP 治疗结肠炎的多重作用机制。本研究以 DSS 诱导的 C57BL/6 小鼠结肠炎为模型,通过组织学评估、16S rRNA 测序、RT-qPCR、ELISA 和 Western blot 等方法评估 XYKJP 对结肠炎的影响。XYKJP主要通过减少氧化应激、炎症反应和结肠炎组织的肠粘膜修复来缓解DSS诱导的结肠炎症状。此外,XYKJP 还通过增加 Akkermansia 和 Bifidobacterium 的相对丰度以及降低 Coriobacteriaceae_UCG-002 的相对丰度来调节肠道菌群。从机理上讲,XYKJP 增加了粪便中短链脂肪酸(SCFAs)的含量,尤其是丙酸和丁酸,激活了它们的特异性受体 GPR43/41,进一步激活了 Nrf2/HO-1 通路,抑制了 JAK2/STAT3 通路。XYKJP 能明显缓解实验性结肠炎的症状,并通过调节肠道菌群、增加 SCFAs 的产生和激活其特异性受体发挥协同作用,从而抑制氧化应激和炎症。
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引用次数: 0
Correction: Metabolism characterization and toxicity of N-hydap, a marine candidate drug for lung cancer therapy by LC–MS method 更正:用 LC-MS 方法分析肺癌治疗海洋候选药物 N-hydap 的代谢特征和毒性。
IF 4.8 3区 化学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-08-02 DOI: 10.1007/s13659-024-00464-w
Jindi Lu, Weimin Liang, Yiwei Hu, Xi Zhang, Ping Yu, Meiqun Cai, Danni Xie, Qiong Zhou, Xuefeng Zhou, Yonghong Liu, Junfeng Wang, Jiayin Guo, Lan Tang
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引用次数: 0
Natural approaches for the management of ulcerative colitis: evidence of preclinical and clinical investigations 治疗溃疡性结肠炎的自然方法:临床前和临床研究的证据。
IF 4.8 3区 化学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-07-30 DOI: 10.1007/s13659-024-00463-x
Rudra Narayan Subudhi, Neelam Poonia, Dilpreet Singh, Vimal Arora

Ulcerative colitis (UC) is a recurring autoimmune disorder characterized by persistent inflammation in the mucosal lining of the lower part of the large intestine. Conventional treatment options such as salicylates, corticosteroids, and immunosuppressants often come with severe side effects, limited bioavailability, and the development of drug resistance, which hampers their therapeutic effectiveness. Therefore, it is imperative to explore natural strategies as safe and alternative treatments for UC. Currently, around 40% of UC patients find relief through natural constituents, which can help reduce toxic side effects and maintain clinical remission. This review aims to provide a summary of both preclinical and clinical evidence supporting the efficacy of various natural substances in the prophylaxis of UC. These natural options include plant extracts, essential oils, nutraceuticals, and phytochemicals. Furthermore, we will delve into the potential mechanisms that underlie the protective and curative actions of these novel herbal agents. In summary, this review will explore the effectiveness of natural remedies for UC, shedding light on their preclinical and clinical findings and the mechanisms behind their therapeutic actions. These alternatives offer hope for improved treatment outcomes and reduced side effects for individuals suffering from this challenging autoimmune condition.

Graphical Abstract

溃疡性结肠炎(UC)是一种反复发作的自身免疫性疾病,其特点是大肠下部粘膜持续发炎。水杨酸盐、皮质类固醇激素和免疫抑制剂等传统治疗方法往往具有严重的副作用、有限的生物利用度以及耐药性的产生,从而影响了其治疗效果。因此,当务之急是探索自然疗法,作为治疗多发性硬化症的安全替代疗法。目前,约有 40% 的 UC 患者通过天然成分获得缓解,这有助于减少毒副作用并维持临床缓解。本综述旨在总结临床前和临床证据,证明各种天然物质在预防 UC 方面的功效。这些天然物质包括植物提取物、精油、营养保健品和植物化学物质。此外,我们还将深入研究这些新型草药的保护和治疗作用的潜在机制。总之,本综述将探讨治疗 UC 的天然疗法的有效性,揭示其临床前和临床研究结果及其治疗作用背后的机制。这些替代疗法为改善治疗效果和减少副作用带来了希望,使人们摆脱这种具有挑战性的自身免疫疾病的困扰。
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引用次数: 0
Revealing the effect of sea buckthorn oil, fish oil and structured lipid on intestinal microbiota, colonic short chain fatty acid composition and serum lipid profiles in vivo 揭示沙棘油、鱼油和结构脂对体内肠道微生物群、结肠短链脂肪酸组成和血清脂质的影响。
IF 4.8 3区 化学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-07-03 DOI: 10.1007/s13659-024-00461-z
Ankang Song, Yanbo Li, Wei Wang, Yueqi Hu, Junjie Xu, Zhixin Xu, Li Zhou, Jikai Liu

In this study, the effects of sea buckthorn oil (SBO), fish oil (FO) and an enzymatically synthesized structured lipid (SL) on serum, short-chain fatty acids (SCFAs) and intestinal microbiota in Sprague–Dawley (SD) rats were investigated. The results demonstrated that FO, SBO, and SL effectively reduced the levels of high-density lipoprotein cholesterol and low-density lipoprotein cholesterol in the serum of SD rats. SBO increased serum triglyceride levels, while FO elevated total cholesterol levels. Furthermore, all three dietary lipids decreased short-chain fatty acid production and enhanced intestinal microbiota diversity. FO increased the abundance of intestinal microbiota including Romboutsia, Lactobacillus, Escherichia-Shigella, and Lachnospiraceae_NK4A136_group. Conversely, all three dietary lipids reduced the abundance of Klebsiella and Blautia. These findings provide a foundation for understanding the functionality of SBO and FO as well as their potential application in synthesizing novel SLs to regulate intestinal microbiota.

Graphical Abstract

本研究调查了沙棘油(SBO)、鱼油(FO)和酶法合成的结构脂(SL)对斯布拉格-道利(SD)大鼠血清、短链脂肪酸(SCFAs)和肠道微生物群的影响。结果表明,FO、SBO 和 SL 能有效降低 SD 大鼠血清中高密度脂蛋白胆固醇和低密度脂蛋白胆固醇的水平。SBO 增加了血清甘油三酯水平,而 FO 则增加了总胆固醇水平。此外,这三种膳食脂质都减少了短链脂肪酸的产生,并提高了肠道微生物群的多样性。膳食脂增加了肠道微生物群的丰度,包括伦博氏菌、乳酸杆菌、志贺氏杆菌和拉赫诺斯弧菌_NK4A136_组。相反,所有三种膳食脂质都会减少克雷伯氏菌和布劳氏菌的数量。这些发现为了解 SBO 和 FO 的功能以及它们在合成新型 SLs 以调节肠道微生物群方面的潜在应用奠定了基础。
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引用次数: 0
Hibiscus acid and hydroxycitric acid dimethyl esters from Hibiscus flowers induce production of dithiolopyrrolone antibiotics by Streptomyces Strain MBN2-2 木槿花中的木槿酸和羟基柠檬酸二甲酯可诱导链霉菌 MBN2-2 株产生二硫代吡咯酮类抗生素。
IF 4.8 3区 化学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-07-03 DOI: 10.1007/s13659-024-00460-0
Felaine Anne Sumang, Alan Ward, Jeff Errington, Yousef Dashti

Plants and microbes are closely associated with each other in their ecological niches. Much has been studied about plant–microbe interactions, but little is known about the effect of phytochemicals on microbes at the molecular level. To access the products of cryptic biosynthetic gene clusters in bacteria, we incorporated an organic extract of hibiscus flowers into the culture media of different Actinobacteria isolated from plant rhizospheres. This approach led to the production of broad-spectrum dithiolopyrrolone (DTP) antibiotics, thiolutin (1) and aureothricin (2), by Streptomyces sp. MBN2-2. The compounds from the hibiscus extract responsible for triggering the production of these two DTPs were found to be hibiscus acid dimethyl ester (3) and hydroxycitric acid 1,3-dimethyl ester (4). It was subsequently found that the addition of either Fe2+ or Fe3+ to culture media induced the production of 1 and 2. The Chrome Azurol S (CAS) assay revealed that 3 and 4 can chelate iron, and therefore, the mechanism leading to the production of thiolutin and aureothricin appears to be related to changes in iron concentration levels. This work supports the idea that phytochemicals can be used to activate the production of cryptic microbial biosynthetic gene clusters and further understand plant–microbe interactions.

Graphical Abstract

植物和微生物在其生态位中密切相关。关于植物与微生物之间相互作用的研究很多,但关于植物化学物质在分子水平上对微生物的影响却知之甚少。为了获取细菌中隐秘生物合成基因簇的产物,我们将木槿花的有机提取物加入从植物根瘤中分离出来的不同放线菌的培养基中。通过这种方法,链霉菌 MBN2-2 生产出了广谱二硫代吡咯烷酮(DTP)抗生素--硫柳丁(1)和金霉素(2)。从木槿提取物中发现,引发这两种 DTP 生成的化合物是木槿酸二甲酯(3)和羟基柠檬酸 1,3 二甲基酯(4)。随后发现,在培养基中加入 Fe2+ 或 Fe3+ 可诱导产生 1 和 2。Chrome Azurol S(CAS)测定显示,3 和 4 可以螯合铁,因此,导致硫醇素和金霉素产生的机制似乎与铁浓度水平的变化有关。这项工作支持了植物化学物质可用于激活隐性微生物生物合成基因簇的产生并进一步了解植物与微生物相互作用的观点。
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引用次数: 0
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