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Phytosome-based drug delivery systems: an updated patent review 基于磷脂酶体的给药系统:最新的专利审查
IF 6.3 2区 生物学 Q1 PLANT SCIENCES Pub Date : 2026-08-07 DOI: 10.1007/s11101-026-10295-x
Shibangi Mukhopadhyay, Nidhi Agrawal, Jaishree Biswas, Vaishali Bharat, S. K. Lanjhiyana, Sanjay Kumar Bharti, Meenakshi Jaiswal

Plant-derived compounds known as phytochemicals have various therapeutic benefits in terms of human health. Despite the wide range of therapeutic uses of phytochemicals, they are encountered with many challenges, viz., poor solubility, instability, and reduced bioavailability in a few instances. Many researchers have recently used phytosomes to overcome these technical difficulties and achieve better outcomes. A phytosome is a matrix-carrier system composed of active phytochemical(s) and phospholipids that enhances the absorption and bioavailability of phytochemicals while facilitating the transport of medication to the target site of action. Globally, the increase in patent registrations over the last two decades has demonstrated a significant growing interest in utilizing phytosomes for developing medicines and nutraceuticals. This report presents a thorough investigation of patents registered regarding phytosomes from the years 2000 to 2024, aiming to detail technological advancements, methodological developments, applications for specific diseases, therapeutic domains, and nutraceuticals in a coherent sequence. The expanding patent landscape on phytosome-based formulations underscores their promise in enhancing bioavailability, targeted delivery, and therapeutic efficacy of natural compounds in comparison to synthetic active compounds. However, future success will rely on bridging preclinical innovation with robust clinical validation and addressing regulatory challenges for translational acceptance.

Graphical abstract

被称为植物化学物质的植物衍生化合物在人类健康方面具有各种治疗益处。尽管植物化学物质的治疗用途广泛,但它们遇到了许多挑战,即溶解度差,不稳定,在少数情况下生物利用度降低。许多研究人员最近使用磷脂体来克服这些技术困难并取得更好的结果。植物体是一种由活性植物化学物质和磷脂组成的基质载体系统,可增强植物化学物质的吸收和生物利用度,同时促进药物转运到作用靶点。在全球范围内,过去二十年来专利注册的增加表明,人们对利用磷脂体开发药物和营养保健品的兴趣日益浓厚。本报告对2000年至2024年期间有关磷脂体的专利注册进行了全面调查,旨在以连贯的顺序详细介绍技术进步,方法发展,特定疾病,治疗领域和营养保健品的应用。与合成活性化合物相比,基于植物复合物的配方在提高生物利用度、靶向递送和天然化合物的治疗功效方面的前景越来越大。然而,未来的成功将依赖于将临床前创新与强大的临床验证联系起来,并解决转化接受的监管挑战。图形抽象
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引用次数: 0
Cyclotides as sustainable biopesticides: structure, function and agricultural potential 环聚糖作为可持续生物农药:结构、功能和农业潜力
IF 6.3 2区 生物学 Q1 PLANT SCIENCES Pub Date : 2026-07-28 DOI: 10.1007/s11101-026-10289-9
Shambhawi, Mengbai Zhang, Lai Yue Chan, David J. Craik

The ever-growing world population has escalated pressure on food production, leading to a dramatic rise in the use of chemical pesticides. Reliance on synthetic chemicals is not only hazardous to humans but also to the environment, highlighting the urgent need for eco-friendly alternatives. Biopesticides have emerged as a promising solution, with the global market for biostimulants and biopesticides projected to reach $30 billion within the next decade. Among these product classes, peptide-based biopesticides have gained considerable attention due to their high specificity, environmental compatibility, and efficacy. Several natural peptide families possess potency against plant pathogens. One such family is cyclotides, which are cyclic plant peptides that are involved in plant defence and have been extensively studied over the last few decades for their agricultural and pharmaceutical properties. Their exceptional stability, conferred by a head-to-tail cyclic backbone and cystine knot motif, enhances their resilience to formulation and storage and broadens their potential applications in agriculture. This review presents a comprehensive overview of cyclotides in the context of other biopesticide classes, highlighting their broad bioactivities, consensus sequence features linked to function, applications in agriculture, and their involvement in plant stress responses. We highlight key advances in the field over the past decade.

Graphical Abstract

不断增长的世界人口给粮食生产带来了更大的压力,导致化学农药的使用急剧增加。对合成化学品的依赖不仅对人类有害,而且对环境有害,因此迫切需要环保替代品。生物农药已经成为一种很有前途的解决方案,生物刺激剂和生物农药的全球市场预计将在未来十年内达到300亿美元。在这些产品类别中,肽基生物农药因其高特异性、环境相容性和有效性而受到广泛关注。几种天然肽家族具有抗植物病原体的效力。其中一个家族是环肽,这是一种参与植物防御的环状植物肽,在过去的几十年里,由于其农业和制药特性而被广泛研究。由首尾相连的环状骨架和胱氨酸结基序所赋予的特殊稳定性,增强了它们对配方和储存的弹性,拓宽了它们在农业中的潜在应用。本文综述了环肽在其他生物农药类别中的研究概况,重点介绍了其广泛的生物活性、与功能相关的一致序列特征、在农业中的应用以及它们在植物胁迫反应中的作用。我们重点介绍了过去十年该领域的主要进展。图形抽象
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引用次数: 0
Bioactive metabolites and antibacterial activity of Copaifera species: evidence from a systematic review Copaifera种的生物活性代谢物和抗菌活性:来自系统综述的证据
IF 6.3 2区 生物学 Q1 PLANT SCIENCES Pub Date : 2026-07-20 DOI: 10.1007/s11101-026-10288-w
Maria da Conceição Alves da Costa, Maria de Jesus Pereira Gomes, Alessandra Souza dos Santos, Fátima de Cássia Evangelista de Oliveira, Luan Ramalho Pinheiro, Maria Francilene Souza Silva, Ivanilza Moreira de Andrade

The Copaifera genus (Fabaceae) is widely used in traditional medicine, especially in the form of oleoresin, for the treatment of inflammatory and infectious disorders. However, other plant parts, particularly the leaves, remain comparatively underexplored despite their considerable pharmacological potential. Therefore, this study aimed to systematically review the available literature regarding the chemical composition and antibacterial activity of leaf extracts from Copaifera species. Literature searches were conducted in Google Scholar, EMBASE, LILACS, PubMed, SciELO, and Scopus databases, including original articles published in Portuguese and English. The search strategy included combinations of descriptors related to Copaifera species, chemical composition, and antibacterial activity. Of the 983 studies initially identified, 11 met the inclusion criteria. The included studies revealed that Copaifera leaf extracts contain a wide variety of secondary metabolites, particularly diterpenes, sesquiterpenes, flavonoids, and pentacyclic triterpenes, which were associated with antibacterial, antioxidant, and anti-inflammatory activities against Gram-positive and Gram-negative bacteria. Non-polar extracts were predominantly associated with terpenoid-rich profiles and antibacterial activity against clinically relevant pathogens. The findings indicate that Copaifera leaf extracts represent a promising and sustainable source of antibacterial bioactive compounds with potential applications in phytotherapeutic and anti-infective formulations. However, the available evidence remains limited by methodological heterogeneity, inconsistent antibacterial assays, limited in vivo validation, and scarce translational studies. Future investigations should prioritize standardized extraction protocols, integrated pharmacological approaches, and in vivo validation to support the therapeutic development of Copaifera-derived compounds.

豆花属(豆科)在传统医学中被广泛使用,特别是以油树脂的形式,用于治疗炎症和感染性疾病。然而,其他植物部分,特别是叶子,尽管具有相当大的药理潜力,但仍相对未被充分开发。因此,本研究旨在系统地综述国内外文献中有关黄芪叶提取物的化学成分及抑菌活性的研究进展。在谷歌Scholar、EMBASE、LILACS、PubMed、SciELO和Scopus数据库中进行文献检索,包括以葡萄牙语和英语发表的原创文章。搜索策略包括与Copaifera物种相关的描述符、化学成分和抗菌活性的组合。在最初确定的983项研究中,有11项符合纳入标准。这些研究表明,铜叶提取物含有多种次生代谢产物,特别是二萜、倍半萜、类黄酮和五环三萜,它们具有抗菌、抗氧化和抗炎作用,可抑制革兰氏阳性和革兰氏阴性菌。非极性提取物主要与萜类化合物丰富的特征和对临床相关病原体的抗菌活性有关。研究结果表明,铜叶提取物是一种有前景的、可持续的抗菌生物活性化合物来源,在植物治疗和抗感染制剂中具有潜在的应用前景。然而,可用的证据仍然受到方法学异质性、不一致的抗菌测定、有限的体内验证和缺乏转化研究的限制。未来的研究应优先考虑标准化的提取方案、综合药理学方法和体内验证,以支持copaifera衍生化合物的治疗开发。
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引用次数: 0
From traditional use to modern phytochemistry – chemical composition and biological activity of cosmopolitan weed species: Stellaria media, Galium aparine and Galinsoga parviflora 从传统植物化学到现代植物化学——世界性杂草:星形草、天冬草和小花草的化学成分和生物活性
IF 6.3 2区 生物学 Q1 PLANT SCIENCES Pub Date : 2026-07-15 DOI: 10.1007/s11101-026-10287-x
Bartosz Rył, Izabela Jasicka-Misiak

Stellaria media (L.) Vill., Galium aparine L., and Galinsoga parviflora Cav. are cosmopolitan species widely used in traditional medicine and as food sources. All three plants have been traditionally applied as anti-inflammatory agents and for the treatment of wounds and skin disorders. S. media has also been used as anti-arthritic remedy, while G. parviflora has been employed for protection against solar radiation. This review evaluates whether the traditional medicinal uses of these species are supported by contemporary phytochemical and pharmacological evidence and provides an updated overview of their chemical composition and biological activity. A comprehensive literature survey was conducted using major scientific databases, including Google Scholar, PubMed, ScienceDirect, Web of Science, SpringerLink, and Wiley Online Library. Phytochemical studies revealed high chemical diversity in all three species, including phenolic acids, flavonoids, iridoids, terpenoids, and phytosterols. Polar fractions were rich in phenolic compounds, whereas non-polar fractions were dominated by fatty acids, hydrocarbons, and terpenoids. Reported biological activities include antimicrobial, anti-inflammatory, enzyme inhibitory, and antidiabetic effects. S. media additionally demonstrated anti-obesity, neuroprotective, and wound-healing activities, while G. aparine showed immunomodulatory and anticancer potential. Extracts of G. parviflora exhibited anti-biofilm, larvicidal, anti-arthritic, and photoprotective effects and inhibited enzymes such as α-amylase, α-glucosidase, urease, and hyaluronidase. Current evidence partially supports the traditional uses of these species. However, further studies employing standardized extraction procedures, bioactivity-guided fractionation, and detailed phytochemical characterization are necessary to clarify structure–activity relationships and support the development of evidence-based phytotherapy.

紫菀(L.)斯德。(3)小檗属植物,小檗属植物。是广泛用于传统医学和食物来源的世界性物种。传统上,这三种植物都被用作抗炎剂,用于治疗伤口和皮肤疾病。美国媒体也被用来作为抗关节炎的补救措施,而细小植物被用来防止太阳辐射。本综述评估了这些物种的传统药用是否得到当代植物化学和药理学证据的支持,并提供了其化学成分和生物活性的最新概述。利用谷歌Scholar、PubMed、ScienceDirect、Web of Science、SpringerLink和Wiley Online Library等主要科学数据库进行了全面的文献调查。植物化学研究表明,这三个物种的化学多样性很高,包括酚酸、类黄酮、环烯醚萜、萜类和植物甾醇。极性馏分富含酚类化合物,而非极性馏分以脂肪酸、碳氢化合物和萜类化合物为主。已报道的生物活性包括抗菌、抗炎、酶抑制和降糖作用。培养基还显示出抗肥胖、神经保护和伤口愈合活性,而G. aparine显示出免疫调节和抗癌潜力。其提取物具有抗生物膜、杀幼虫、抗关节炎和光保护作用,并能抑制α-淀粉酶、α-葡萄糖苷酶、脲酶和透明质酸酶等酶的活性。目前的证据部分支持这些物种的传统用途。然而,进一步的研究采用标准化的提取程序,生物活性引导的分离和详细的植物化学表征是必要的,以澄清结构-活性关系和支持基于证据的植物疗法的发展。
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引用次数: 0
Progress in plant-derived terpenoid: biosynthetic pathways, therapeutic roles, and sustainable production strategies 植物源萜类化合物的研究进展:生物合成途径、治疗作用和可持续生产策略
IF 6.3 2区 生物学 Q1 PLANT SCIENCES Pub Date : 2026-07-14 DOI: 10.1007/s11101-026-10281-3
Abdul Fatah A. Samad, Nazrin Abd-Aziz, Joazaizulfazli Jamalis, Mohd Bakri Bakar, Azman Abd Samad, Raihana Ridzuan, Siti Ernieyanti Hashim, Alina Wagiran, Mira Panadi, Mohd Ridzuan Mohd Abd Razak

Plant-derived terpenoids constitute one of the most structurally diverse and biologically active classes of natural products, offering substantial potential for therapeutic and industrial applications. This review provides a comprehensive synthesis of current advances in plant derived terpenoid medicines, beginning with the fundamental principles of terpene chemistry and extending to the complexity of plant specific biosynthetic pathways. We critically examine the therapeutic roles of terpenoids, with particular emphasis on their antioxidant, anticancer, antiallergic, and antimicrobial activities. Furthermore, the review highlights recent developments in biotechnological approaches, including genetic transformation, CRISPR genome editing, microRNA (miRNA) mediated regulation, and plant tissue culture, aimed at enhancing terpenoid biosynthesis and yield. Emerging chemical and green synthesis strategies are also discussed as sustainable alternatives to conventional plant extraction. By integrating perspectives from pharmacology, plant molecular biology, and synthetic chemistry, this review underscores the versatility of plant derived terpenoids as promising candidates for drug discovery and industrial innovation, while identifying key challenges and outlining future research directions.

Graphical abstract

植物源性萜类化合物是结构最多样、生物活性最高的一类天然产物,具有巨大的治疗和工业应用潜力。本文综述了植物萜类药物的最新进展,从萜类化学的基本原理开始,延伸到植物特异性生物合成途径的复杂性。我们严格检查萜类化合物的治疗作用,特别强调其抗氧化,抗癌,抗过敏和抗菌活性。此外,本文还重点介绍了生物技术方法的最新进展,包括遗传转化、CRISPR基因组编辑、microRNA (miRNA)介导的调控和植物组织培养,旨在提高萜类化合物的生物合成和产量。新兴的化学和绿色合成策略也讨论了作为传统植物提取的可持续替代品。本文综合了药理学、植物分子生物学和合成化学的观点,强调了植物衍生萜类化合物在药物发现和工业创新方面的多功能性,同时确定了关键挑战并概述了未来的研究方向。图形抽象
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引用次数: 0
Prescription principle, phytochemistry, pharmacological activities and clinical applications of Huangqin decoction: a comprehensive review 黄芩汤的处方原理、植物化学、药理活性及临床应用综述
IF 6.3 2区 生物学 Q1 PLANT SCIENCES Pub Date : 2026-07-14 DOI: 10.1007/s11101-026-10277-z
Yan Fang, Haizhen Liang, Linlin Lu, Xijie Tian, Yuting Zhang, Junyu Zhang, Zhifeng Dai, Xiaojuan Chen, Juan Song, Tao Su, Zhongqiu Liu, Baiping Ma

Huangqin decoction (HQD), a traditional Chinese prescription composed of Scutellariae Radix (Huang-Qin in Chinese), Paeonia Lactiflora (Shao-Yao), Glycyrrhizae Radix et Rhizoma (Gan-Cao), and Jujubae Fructus (Da-Zao), has been used for heat-induced diarrhea (Re-Xie) for over 1800 years. Its modern modified pharmaceutical formulation, YIV906, was currently the first traditional Chinese prescriptions botanical medicine to enter the Food and Drug Administration clinical trial phase for cancer treatment. Despite its long history, the modern scientific explorations of its phytochemistry composition and Pharmacological activities still need to be systematically summarized. By analyzing and summarizing the current research of HQD, this review aimed to clarify existing research gaps and propose recommendations for future researches. The search terms “Huangqin decoction” and “Huangqin tang” were utilized to obtain the relevant literature from online databases including Web of Science, PubMed, Google Scholar, SciFinder, and China National Knowledge Infrastructure. Furthermore, traditional medical books in China were also collected. In total, 192 chemical constituents were identified in HQD using analytical methods. The quality evaluation of HQD primarily focused on its chemical fingerprint. In addition, pharmacokinetic studies on HQD centered on the active components present in its constituent herbs. Pharmacological studies showed HQD had anti-ulcerative colitis, anti-cancer, anti-bacterial properties, and regulated metabolism. Its main mechanisms involved signaling pathways like PI3K/AKT/mTOR, miR-185-3p/MLCK/pMLC, and IFN-γ/JAK/ETS, which collectively maintained immune balance, intestinal microbiota, and epithelial barrier integrity. In clinical applications, HQD was commonly used for the treatment of digestive system diseases, cancer, and metabolic syndrome. However, there remained some limitations in the investigation of HQD. Future studies focusing on the elucidation of chemical constituents, the improvement of quality control, and the clarification of functional mechanisms are worthy of exploration.

黄芩汤(HQD)是一种由黄芩、芍药、甘草和枣子组成的传统中药方剂,用于治疗热泻已有1800多年的历史。其现代改良药物配方YIV906是目前第一个进入美国食品药品监督管理局癌症治疗临床试验阶段的中药处方植物药。尽管其历史悠久,但其植物化学成分和药理活性的现代科学探索仍需系统总结。本文通过对HQD的研究现状进行分析和总结,旨在澄清现有的研究空白,并对未来的研究提出建议。在Web of Science、PubMed、b谷歌Scholar、SciFinder和中国国家知识基础设施数据库中检索“黄芩汤”和“黄芩汤”,获取相关文献。此外,还收集了中国传统医学书籍。利用分析方法共鉴定出192种化学成分。HQD质量评价主要集中在化学指纹图谱上。此外,HQD的药代动力学研究主要集中在其成分草药中存在的有效成分。药理研究表明,HQD具有抗溃疡性结肠炎、抗癌、抗菌、调节代谢等作用。其主要机制涉及PI3K/AKT/mTOR、miR-185-3p/MLCK/pMLC和IFN-γ/JAK/ETS等信号通路,它们共同维持免疫平衡、肠道微生物群和上皮屏障的完整性。在临床应用中,HQD常用于治疗消化系统疾病、癌症和代谢综合征。然而,对HQD的研究仍存在一定的局限性。未来的研究重点是化学成分的阐明、质量控制的改进和作用机制的阐明,值得探索。
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引用次数: 0
The anti-inflammatory and anticancer effects of argentatins are dependent on their chemical structure 阿根廷蛋白的抗炎和抗癌作用取决于它们的化学结构
IF 6.3 2区 生物学 Q1 PLANT SCIENCES Pub Date : 2026-07-12 DOI: 10.1007/s11101-026-10264-4
Aniela M. Silva-Nolasco, Miguel A. de la Cruz-Morcillo, M. Mercedes García-Martínez, Guayente Latorre, M. Engracia Carrión, Amaya Zalacain, Mariano Martínez-Vázquez, Manuel Carmona

The guayule shrub, Parthenium argentatum A. Gray, has a long history of use as an alternative source of natural rubber and latex. However, the resin produced by this shrub, which contains a considerable number of secondary metabolites, has yet to be fully exploited. The most abundant metabolites in guayule resin are the argentatins, which chemically correspond to cycloartenol- and lanostane-type triterpenes, and represent up to 27% of the total resin content. These compounds have significant potential for pharmaceutical development, particularly in relation to their anti-inflammatory, antimicrobial, and antitumorigenic properties. The present study reviews the principal pharmacological and biomedical activities ascribed to the argentatins and demonstrates that minor chemical modifications in their structure through semi-synthesis or biotransformation has the potential to enhance their activity to > tenfold compared with the original compound in approximately 80% of cases. The exploration and utilization of these compounds might increase the commercial utilization of guayule cultivation, facilitating the development of new applications and opportunities for this versatile shrub in the healthcare sector.

银胶菊灌木,Parthenium argentatum a . Gray,作为天然橡胶和乳胶的替代来源有着悠久的使用历史。然而,这种灌木所产生的树脂含有相当数量的次生代谢物,尚未被充分利用。银胶菊树脂中最丰富的代谢物是银胶菊苷,其化学性质相当于环artenol型和羊毛甾烷型三萜,占树脂总含量的27%。这些化合物在药物开发方面具有重要的潜力,特别是它们的抗炎、抗菌和抗肿瘤特性。本研究回顾了阿根廷蛋白的主要药理和生物医学活性,并表明通过半合成或生物转化对其结构进行微小的化学修饰,在大约80%的情况下,与原始化合物相比,它们的活性有可能提高到10倍。这些化合物的探索和利用可能会增加银胶菊种植的商业利用,促进这种多功能灌木在医疗保健部门的新应用和机会的发展。
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引用次数: 0
Integrated scientometric mapping and chemometric profiling of Siparuna guianensis essential oil: chemical variability, antioxidant and biological activity 桂树精油的综合科学计量作图和化学计量分析:化学变异、抗氧化和生物活性
IF 6.3 2区 生物学 Q1 PLANT SCIENCES Pub Date : 2026-07-12 DOI: 10.1007/s11101-026-10282-2
Danylo Duran Silva Santos, Lucas Villar Pedrosa Silva Pantoja, Joana Julia dos Santos Moraes, Eliza de Jesus Barros dos Santos, Ravendra Kumar, Mateus Machado Lima, Karyme do Socorro de Souza Vilhena, Antônio Maia de Jesus Chaves Neto, Brenda Costa da Conceição, Marta Eduarda Oliveira Barbosa, Eloise Karoline Serrão Cardoso, Cristiane Socorro Ferraz Maia, Enéas Andrade Fontes-Junior, Mozaniel Santana de Oliveira

Siparuna guianensis is a neotropical aromatic species widely used in traditional medicine whose essential oil exhibits diverse biological activities. However, current evidence remains fragmented and strongly influenced by chemical variability across populations and extraction conditions. This study integrates scientometric mapping, multivariate chemometric analysis, and critical pharmacological review to clarify the relationship between chemical composition and biological activity of S. guianensis essential oil. Publications indexed in Web of Science were analyzed to identify research trends, collaboration networks, and thematic focus. Reported chemical composition data were subjected to principal component analysis and hierarchical clustering to define chemotype patterns and associate them with biological outcomes. The literature reveals a highly centralized and chemistry-driven research field dominated by vector-control and pest-management studies, with limited mechanistic pharmacology in mammalian systems. Chemometric results demonstrate pronounced chemical polymorphism, separating monoterpene-rich and sesquiterpene-rich chemotypes. Monoterpene profiles, particularly those dominated by β-myrcene and aliphatic ketones, are mainly linked to insecticidal and repellent effects, whereas sesquiterpene-rich oils containing germacrene D, curzerenone, spathulenol, and α-bisabolol are more frequently associated with antimicrobial, antiparasitic, enzyme-inhibitory, and antitumoral activities. Despite promising results, most studies remain preliminary. Pharmacological translation will require chemotype standardization, mechanistic validation, safety profiling, and advanced formulation strategies to enable reproducible and clinically relevant applications.

桂树是一种被广泛应用的新热带芳香植物,其精油具有多种生物活性。然而,目前的证据仍然是支离破碎的,并且受到不同种群和提取条件的化学变异的强烈影响。本研究结合科学计量图谱、多元化学计量分析和关键药理评价等方法,阐明桂枝精油的化学成分与生物活性之间的关系。对Web of Science收录的出版物进行分析,以确定研究趋势、合作网络和主题重点。报告的化学成分数据进行主成分分析和分层聚类,以确定化学型模式,并将其与生物学结果相关联。文献揭示了一个高度集中和化学驱动的研究领域,主要是媒介控制和害虫管理研究,在哺乳动物系统中的机械药理学研究有限。化学计量学结果显示明显的化学多态性,分离了富单萜和富倍半萜的化学型。单萜,尤其是那些以β-桃金烯和脂肪酮为主的单萜,主要与杀虫和驱避作用有关,而富含倍半萜的油,含有石榴烯D、curzerenone、spathulenol和α-bisabolol,则更经常与抗菌、抗寄生虫、酶抑制和抗肿瘤活性有关。尽管结果令人鼓舞,但大多数研究仍处于初步阶段。药理学翻译将需要化学型标准化、机制验证、安全性分析和先进的配方策略,以实现可重复和临床相关的应用。
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引用次数: 0
Biflavonoids in the Thymelaeaceae: a review on chemical diversity and bioactivity 百里香科生物黄酮类化合物的化学多样性和生物活性研究进展
IF 6.3 2区 生物学 Q1 PLANT SCIENCES Pub Date : 2026-07-04 DOI: 10.1007/s11101-026-10258-2
Yanli Li, Ye Dong, Lingzhi Li

Biflavonoids from the Thymelaeaceae family are gaining increasing attention due to their diverse pharmacological activities and considerable potential as therapeutic agents. Biflavonoids derived from genera such as Stellera, Wikstroemia, and Daphne have emerged as focal points in natural product-based drug discovery. Previous studies have documented the ethnopharmacological applications of Thymelaeaceae species while providing analyses of their phytochemical constituents. However, systematic reviews critically evaluating the structural diversity, pharmacological activities, and structure–activity relationships of Thymelaeaceae-derived biflavonoids remain scarce. Therefore, the main objective of this review is to summarize recent research reports on biflavonoids isolated from Thymelaeaceae plants up to the present, including their structural features, classification based on linkage patterns, and pharmacological activities, with particular emphasis on anticancer, antiviral, and anti-inflammatory effects. Furthermore, this article discusses structure–activity relationships of representative biflavonoids, highlighting how specific structural features—such as C-3/C-3″ linkages, methoxy substitution, and stereochemical configuration—critically influence their bioactivity. By identifying current research gaps and proposing future directions, this review aims to provide a comprehensive reference for the continued development of Thymelaeaceae biflavonoids as potential drug candidates.

Graphical abstract

百里香科生物类黄酮因其丰富的药理活性和作为治疗药物的巨大潜力而受到越来越多的关注。生物黄酮类化合物的来源,如斯特拉属,Wikstroemia和达芙妮已成为天然产品为基础的药物发现的焦点。以往的研究记录了百里香科植物的民族药理学应用,并对其植物化学成分进行了分析。然而,对百里香科生物类黄酮的结构多样性、药理活性和构效关系进行批判性评价的系统综述仍然很少。因此,本文对近年来从百里香科植物中分离的生物黄酮的研究进展进行综述,包括其结构特征、基于连锁模式的分类以及药理活性,重点介绍其抗癌、抗病毒和抗炎作用。此外,本文讨论了代表性生物类黄酮的构效关系,强调了特定的结构特征-如C-3/C-3″键,甲氧基取代和立体化学构型-如何严重影响其生物活性。本文旨在通过对百里香科生物黄酮类化合物研究现状的梳理和展望,为进一步开发百里香科生物黄酮类化合物提供参考。图形抽象
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引用次数: 0
Serrulatane diterpenoids: a review of their biosynthesis, chemical diversity, and biological significance in plants and marine organisms Serrulatane二萜:在植物和海洋生物中的生物合成、化学多样性及其生物学意义的综述
IF 6.3 2区 生物学 Q1 PLANT SCIENCES Pub Date : 2026-07-02 DOI: 10.1007/s11101-026-10271-5
Yhiya Amen, Ahmed Othman

Serrulatane diterpenoids represent a structurally unique and biologically significant class of natural products, predominantly found in various plant genera and marine organisms, such as soft corals. Characterized by a distinctive bicarbocyclic skeleton and diverse oxygenation patterns, these compounds arise via an unconventional biosynthetic pathway involving the cisoid nerylneryl diphosphate (NNPP) and class I terpene synthases, diverging from the typical geranylgeranyl diphosphate (GGPP)-dependent route common to most diterpenes. Exhibiting potent antiviral, cytotoxic, and antimicrobial activities, serrulatanes hold promise as leads for pharmaceutical development, while also serving as chemotaxonomic markers and ecological defense agents in both terrestrial and marine environments. This review comprehensively summarizes the current knowledge on the naturally occurring serrulatane diterpenoids reported to date, detailing their sources, structural features, and biological activities, and highlighting their importance in chemical ecology and drug discovery.

山精二萜是一种结构独特且具有重要生物学意义的天然产物,主要存在于各种植物属和海洋生物中,如软珊瑚。这些化合物具有独特的双碳环骨架和不同的氧化模式,它们是通过一种非常规的生物合成途径产生的,涉及顺尾草烯基二磷酸(NNPP)和I类萜烯合成酶,与大多数二萜常见的典型的依赖于香叶基二磷酸(GGPP)的途径不同。由于具有强大的抗病毒、细胞毒性和抗菌活性,serrulatanes有望成为药物开发的先导,同时也可作为陆地和海洋环境中的化学分类标记和生态防御剂。本文综述了迄今为止关于天然存在的山精氨酸二萜类化合物的研究进展,详细介绍了它们的来源、结构特征和生物活性,并强调了它们在化学生态学和药物发现中的重要性。
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引用次数: 0
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Phytochemistry Reviews
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