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Three new compounds of Umbelopsis dimorpha VDG10, a dominant endophytic fungus from Vaccinium dunalianum Wight. dunalianum Wight的优势内生真菌Umbelopsis dimorpha VDG10的三个新化合物。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-12-24 DOI: 10.1016/j.fitote.2024.106358
Zhi-Yu Zhang, Xiao-Man Fu, Yuan-Cao Shu, Xu-Jie Qin, Ying-Jun Zhang, Ping Zhao, Xiao-Qin Yang, Li-Hua Zou, Wei-Hua Wang, Guo-Lei Zhu

Three novel compounds, including an aromatic amino acid, dimorine A (1), a suncheonoside derivative, dimoroside A (2), and a phenylpropanoid glycoside, dimoroside B (3), together with four known compounds (4-7) were separated from Umbelopsis dimorpha VDG10, the predominant endophytic fungus found in the roots of Vaccinium dunalianum Wight (Ericaceae). Their structures were elucidated by spectroscopic methods, and the ECD spectrum confirmed the absolute configuration of 3. In addition, the antifungal activities of novel compounds against five phytopathogenic fungi were evaluated. The results indicated that compound 3 has a better inhibitory effect on Alternaria brassicicola than the broad-spectrum antifungal agent thiabendazole, and its MICs of 15.63-7.82 μg/mL.

从杜鹃根内生真菌Umbelopsis dimoroa VDG10中分离出芳香氨基酸二moroine A(1)、二moroside衍生物二moroside A(2)和苯丙苷二moroside B(3) 3个新化合物和4个已知化合物(4-7)。用光谱学方法鉴定了它们的结构,ECD谱图证实了3的绝对构型。此外,还对新化合物对5种植物病原真菌的抑菌活性进行了评价。结果表明,化合物3对十字花科真菌的抑制效果优于广谱抗真菌剂噻苯达唑,其mic值为15.63 ~ 7.82 μg/mL。
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引用次数: 0
Endophytes as bioenhancers of plant growth: An overview. 内生菌作为植物生长的生物促进剂:综述。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-12-22 DOI: 10.1016/j.fitote.2024.106355
P Aishwarya, K G Sabarinathan, M Gomathy, P Meenakshisundaram, K Manonmani, A Ahaz Kar

The need for food production rises with the era of expanding population. As a result, there is more indirect demand for chemical pesticides and fertilizers. Serious environmental concerns result from the continuous and careless usage of chemicals. Additionally, they could make the land infertile. One of the finest substitutes for chemicals is to use microorganisms, particularly endophytes. Endophytes uses both direct and indirect mechanisms to encourage plant growth by increased mineral availability, resilience to biotic and abiotic stresses, synthesis of significant phytohormones. This review is focused on exploring the plant growth promoting effect of endophytes and its potential implications in the crop production.

随着人口的增长,对粮食生产的需求也在增加。因此,对化学农药和化肥的间接需求增加。持续和不小心使用化学品造成了严重的环境问题。此外,它们会使土地变得贫瘠。最好的化学品替代品之一是利用微生物,特别是内生菌。内生菌利用直接和间接的机制来促进植物生长,增加矿物质的利用率,对生物和非生物胁迫的恢复力,合成重要的植物激素。本文就内生菌对植物生长的促进作用及其在作物生产中的潜在应用进行了综述。
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引用次数: 0
Identification and comparative genomic analysis of endophytic fungi in Bletilla striata and its potential for promoting militarine bioaccumulation. 白芨内生真菌的鉴定、比较基因组分析及其促进军事生物积累的潜力。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-12-22 DOI: 10.1016/j.fitote.2024.106356
Xueyan Jia, Yang Li, Lang Chen, Yexin Xiao, Ning Yang, Hongyuan Luo, Jing Guan, Delin Xu

Bletilla striata (Thunb.) Reichb.f is renowned for its traditional medicinal applications and a spectrum of pharmacological activities, which is intricately linked to militarine. Addressing sustainable production of B. striata and militarine necessitates innovative strategies. Endophytic fungi, residing within plant tissues and establishing symbiotic relationships, act as secondary genomes of plants, co-regulating plant growth and secondary metabolite synthesis. Despite their potential, the genetic and metabolic diversity, functional activity, and regulatory interactions of endophytic fungi with B. striata remain unexplored. This study aims to bridge this gap by investigating endophytic fungi that could enhance B. striata growth and militarine biosynthesis. The study revealed that endophytic fungi from pseudobulbs, roots, and stems were co-cultured with callus tissue of B. striata, and it was discovered that Serendipita indica from the Serendipita genus can enhance militarine accumulation. Subsequently, key genes, core enzymes, and regulatory factors related to militarine biosynthesis in the S. indica genome were analyzed. By employing advanced biotechnological and comparative genomic approaches, we elucidated the composition and distribution of regulatory factors across different endophytic fungal genomes associated with B. striata. This research not only advances our understanding of the symbiotic relationship between B. striata and its endophytic fungi but also provides a foundational blueprint for the sustainable exploitation and enhancement of militarine production.

白芨(白芨)Reichb。F以其传统医学应用和一系列药理活动而闻名,这与军事有着复杂的联系。解决条纹藻和军用植物的可持续生产问题需要创新的战略。内生真菌作为植物的次生基因组,存在于植物组织中,与植物建立共生关系,共同调控植物生长和次生代谢物合成。尽管具有潜力,但内生真菌与纹状芽孢杆菌的遗传和代谢多样性、功能活性以及调控相互作用仍未被探索。本研究旨在通过研究能够促进纹状芽孢杆菌生长和军事生物合成的内生真菌来弥补这一空白。研究发现,将来自假球茎、根和茎的内生真菌与纹状体愈伤组织共培养,发现来自Serendipita属的Serendipita indica能促进军力积累。随后,分析了籼稻基因组中与军事生物合成相关的关键基因、核心酶和调控因子。采用先进的生物技术和比较基因组学方法,研究了不同内生真菌基因组中调控因子的组成和分布。该研究不仅加深了我们对纹状芽孢杆菌及其内生真菌共生关系的认识,而且为纹状芽孢杆菌的可持续开发和提高军事生产水平提供了基础蓝图。
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引用次数: 0
Biomimetic synthesis of rare cannabigerol-type cannabinoids and evaluation of their cytotoxic effect on human glioblastoma cell lines. 稀有大麻酚型大麻素的仿生合成及其对人胶质母细胞瘤细胞系的细胞毒作用评价。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-12-22 DOI: 10.1016/j.fitote.2024.106354
Martina Giangrossi, Stefano Salamone, Aurora Camola, Orazio Taglialatela-Scafati, Giuseppina Chianese, Ernesto Gargiulo, Massimo Nabissi, Federica Pollastro

Although Cannabis sativa L. is well known for being prolific in phytocannabinoids, their biosynthetic modular mechanism is ruled by a main enzyme: the geranyltransferase able to pursue the C-isoprenylation of olivetolic acid with the geranyldiphosphate. However, the existence of more than 160 meroterpenoids can be partially explained by a side degree of promiscuity of the geranyltransferase itself, able to recognise different substrate than the ordinary ones. This biological process led to the identification of several unconventional phytocannabinoids with a limited distribution in the plant both for occurrence and concentration. Taking advance of the existing synthetic protocols and using as example the enzymatic promiscuity, we propose a bio-inspired synthesis of naturally occurring minor cannabinoids related to the cannabigerol-type and their preliminary biological inspection in U87, U251 and T98 human glioblastoma cell lines to investigate their potential contribute as supplement in anticancer therapy.

虽然大麻以富含植物大麻素而闻名,但它们的生物合成模块化机制是由一种主要酶控制的:香叶基转移酶,该酶能够与香叶基二磷酸进行橄榄酸的c -异戊二烯化。然而,超过160种巯基萜类化合物的存在可以部分解释为香叶基转移酶本身的一种程度的混杂性,它能够识别不同于普通底物的底物。这一生物学过程导致了几种非常规植物大麻素的鉴定,这些大麻素在植物中的分布和浓度都是有限的。在现有合成方案的基础上,以酶促乱交为例,我们提出了一种生物启发合成天然存在的与大麻酚类型相关的少量大麻素,并在U87、U251和T98人胶质母细胞瘤细胞系中进行了初步的生物学检测,以研究它们作为抗癌治疗补充的潜在贡献。
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引用次数: 0
Assessing the genetic diversity of Eupatorium adenophorum (Ageratina adenophora) through the development of ISSR-derived SCAR (sequence characterized amplified region) markers. 利用issr衍生的SCAR(序列特征扩增区)标记评估紫茎泽兰(Ageratina adenophora)遗传多样性。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-12-20 DOI: 10.1016/j.fitote.2024.106352
Sushmita Dwivedi, Mamta Baunthiyal

Eupatorium adenophorum (Ageratina adenophora) is regarded as an invasive weed in many regions of the world. Yet, it is notable for its possible therapeutic uses, including the treatment of blood coagulation, antibacterial, anti-inflammatory, antiseptic, analgesic, and other ailments. Till now, there is not much information available regarding the molecular characterization of E. adenophorum thus, the present study attempted to assess the genetic diversity of E. adenophorum, through DNA fingerprints of this species obtained by using Inter Simple Sequence Repeats Polymerase Chain Reaction (ISSR-PCR) methods. In the study, 50 primers were used to screen ISSR markers. Using the nucleotide sequences of certain ISSR markers, primers for unique sequence-characterized amplified regions (SCAR) were created. These primers effectively amplified the 219, 231, 810, 350, and 500 bp SCAR markers that are exclusive to E. adenophorum. Furthermore, this plant identification technique has the potential to amplify specific markers from mixed DNA samples with high specificity, offering a promising approach for distinguishing closely related species.

紫茎泽兰(Ageratina adenophora)在世界上许多地区被视为一种入侵杂草。然而,值得注意的是它可能的治疗用途,包括治疗凝血、抗菌、抗炎、防腐、止痛和其他疾病。到目前为止,关于紫茎甘蓝分子特征的信息还不多,因此,本研究试图通过采用ISSR-PCR方法获得紫茎甘蓝的DNA指纹图谱来评估其遗传多样性。本研究使用50条引物筛选ISSR标记。利用某些ISSR标记的核苷酸序列,构建了独特序列特征扩增区(SCAR)引物。这些引物有效扩增了219、231、810、350和500 bp的SCAR标记,这些标记是紫茎甘蓝所特有的。此外,这种植物鉴定技术具有从混合DNA样品中以高特异性扩增特定标记的潜力,为区分近亲物种提供了一种有前途的方法。
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引用次数: 0
Epigenetic regulation by naringenin and naringin: A literature review focused on the mechanisms underlying its pharmacological effects. 柚皮素和柚皮苷的表观遗传调控作用:综述其药理作用机制。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-12-19 DOI: 10.1016/j.fitote.2024.106353
Xiao Wu, Hao Wu, Mengli Zhong, Yixuan Chen, Weiwei Su, Peibo Li

Epigenetics refers to heritable changes in gene expression or phenotypic changes that occur without changing the gene sequence. The main methods of epigenetics include non-coding RNA, histone modification, and DNA modification, which play an essential role in gene expression regulation and even the occurrence of diverse diseases. Naringenin, the aglycone form of naringin, is a natural flavonoid compound mainly found in fruits or plant derivatives such as citrus, tomatoes, and cherries. Naringenin and naringin exhibit a broad spectrum of biological activities and pharmacological effects, including anti-cancer, cardiovascular disease improving, anti-inflammatory, and anti-oxidant activities, all of which are advantageous for human health. Recent studies have uncovered that naringenin and naringin influence gene expression by modulating epigenetic pathways, including microRNA (miRNA) regulation. This mechanism plays a crucial role in the therapeutic potential for various diseases. This paper reviews the epigenetic researches on the physiological activities of naringenin and naringin. It highlights how these compounds can exert diverse effects through different signaling pathways, thereby ameliorating associated diseases. These findings provide valuable insights for the future applications of naringenin and naringin.

表观遗传学是指在不改变基因序列的情况下发生的基因表达的可遗传变化或表型变化。表观遗传学的主要方法包括非编码RNA、组蛋白修饰和DNA修饰,它们在基因表达调控乃至多种疾病的发生中起着至关重要的作用。柚皮素是柚皮素的苷元形式,是一种天然的类黄酮化合物,主要存在于水果或植物衍生物中,如柑橘、西红柿和樱桃。柚皮素和柚皮苷具有广泛的生物活性和药理作用,包括抗炎、抗氧化、抗癌、改善心血管疾病等,对人体健康都有好处。最近的研究发现,柚皮素和柚皮苷通过调节包括microRNA调控在内的表观遗传途径影响基因表达。这一机制在多种疾病的治疗潜力中起着至关重要的作用。本文综述了柚皮素和柚皮苷生理活性的表观遗传学研究进展。它强调了这些化合物如何通过不同的信号通路发挥不同的作用,从而改善相关疾病。这些发现为柚皮素和柚皮苷的未来应用提供了有价值的见解。
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引用次数: 0
Sesquiterpene lactones from Seriphidium transiliense and their anti-inflammation activity. 绢蝇倍半萜内酯及其抗炎活性。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-12-19 DOI: 10.1016/j.fitote.2024.106349
Fangsheng Wang, Huizhen Wen, Liu Liu, Jun Li, Fei He, Haji Akber Aisa, Xuelei Xin

Six undescribed sesquiterpene lactones (1-6) and fifteen known compounds (7-21) were isolated from Seriphidium transiliense. The chemical structures were determined by extensive NMR spectroscopic data, HRESIMS, ECD and X-ray diffraction. Among the known compounds, twelve known compounds were isolated for the first time from this plant, including taurine (9), 11-epitaurin (10), α-santonin (11), artesin (13), 11-epiartesin (14), 1α-hydroxy-3β-acetoxyeudesm-4-en-6β, 7α, 11βH-12, 6-olide (15), 1α-hydroxy-3β-acetoxyeudesm-4-en-6β, 7α, 11αH-12, 6-olide (16), artegallin (17), 8α-hydroxytaurin (18), 8α-acetoxytaurine (19), methyl-4α-hydroxy-11(13)-eudesmen-12-oatesaniculamoid D (20), and saniculamoid D (21). The absolute configuration of 2 was determined by X-ray. The X-ray crystal structures of 15 and 16 were reported for the first time. At a concentration of 20 μM, all compounds (1-21) showed significant inhibition of NO production in LPS- stimulated BV2 cells. Among them, compounds 3 and 4 inhibited NO release with IC50 values of 19.30 and 22.05 μM, respectively. Based on the present results, these compounds may be potential anti-inflammatory agents.

从绢蝇中分离得到6个未描述的倍半萜内酯(1-6)和15个已知的化合物(7-21)。化学结构是通过广泛的核磁共振光谱数据,hresms, ECD和x射线衍射确定的。其中,首次从该植物中分离得到12个已知化合物,分别为牛磺酸(9)、11-表黄素(10)、α-山芦苷(11)、青蒿素(13)、11-表黄素(14)、1α-羟基-3β-乙酰氧基yeudesm-4-en-6β、7α、11α -h -12、6-烯内酯(15)、1α-羟基-3β-乙酰氧基yeudesm-4-en-6β、7α、11α -h -12、6-烯内酯(16)、青蒿素(17)、8α-羟基牛磺酸(18)、8α-乙酰氧基牛磺酸(19)、甲基-4α-羟基-11(13)、8α-乙酰氧基牛磺酸(19)、甲基-4α-羟基-11(18)、8α-乙酰氧基牛磺酸-12-燕麦酰胺D(20)、saniculamoid D(21)。用x射线测定了2的绝对构型。其中15和16的x射线晶体结构为首次报道。在20 μM的浓度下,所有化合物(1-21)均能显著抑制LPS刺激的BV2细胞NO的产生。其中化合物3和4抑制NO释放的IC50值分别为19.30和22.05 μM。基于目前的结果,这些化合物可能是潜在的抗炎剂。
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引用次数: 0
Bioactive metabolites of Brazilian Red Propolis: Cytotoxic, antimalarial, and antimicrobial properties. 巴西红蜂胶的生物活性代谢物:细胞毒性、抗疟疾和抗菌特性。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-12-18 DOI: 10.1016/j.fitote.2024.106351
Jennyfer Andrea Aldana-Mejía, Victor Pena Ribeiro, Kumudini M Meepagala, Jairo Kenupp Bastos, Samir A Ross

Brazilian Red Propolis (BRP) is a natural product known for its rich chemical composition and therapeutic potential. This study investigates the phytochemical profile and evaluates the cytotoxic, antiplasmodial, and antimicrobial properties of red propolis extract and its isolated compounds vestitol (1), neovestitol (2), medicarpin (3), 7-O-methylvestitol (4), and oblongifolin B (5). The extract showed selective cytotoxicity against cancer cell lines (IC50: 16-39 μg/mL). Compound 3 exhibited a promising cytotoxicity against SK-OV-3 with and IC50 of 6.65 μM. BRP had moderate antimicrobial effects; however, 3 was effective against Cryptococcus neoformans (IC50: 19.29 μM), while 5 was active against Pseudomonas aeruginosa (IC50: 15.77 μM). BRP exhibited antiplasmodial activity against Plasmodium falciparum strains D6 and W2 (IC50: 13.8 μg/mL and 5.7 μg/mL); also, 4 and 5 had IC50 concentrations ranging from: 2.99-6.96 μM). Molecular docking for P. falciparum lactate dehydrogenase (PfLDH), suggest that compound 4 has significant interactions with critical residues in the PfLDH active site, such as TYR85, THR97, and ASP53, and falls within optimal ranges for oral bioavailability. These findings highlight the significant bioactive potential of BRP and its compounds, suggesting their potential as therapeutic agents in vitro and in-silico. Further studies are recommended to explore their mechanisms of action and therapeutic applications.

巴西红蜂胶(BRP)是一种天然产品,以其丰富的化学成分和治疗潜力而闻名。本研究研究了红蜂胶提取物及其分离化合物vestitol(1)、neovestitol(2)、medicarpin(3)、7-O-methylvestitol(4)和oblongifolin B(5)的植物化学性质,并对其细胞毒、抗疟原虫和抗菌性能进行了评价。该提取物对癌细胞具有选择性细胞毒性(IC50: 16-39 μg/mL)。化合物3对SK-OV-3具有良好的细胞毒性,IC50为6.65 μM。BRP抗菌效果中等;其中,3株对新型隐球菌(IC50: 19.29 μM)有效,5株对铜绿假单胞菌(IC50: 15.77 μM)有效。BRP对恶性疟原虫D6和W2株具有抗疟原虫活性(IC50分别为13.8 和5.7 μg/mL);4和5的IC50浓度范围为:2.99 ~ 6.96 μM)。对恶性疟原虫乳酸脱氢酶(PfLDH)的分子对接表明,化合物4与PfLDH活性位点的关键残基如TYR85、THR97和ASP53有显著的相互作用,处于口服生物利用度的最佳范围内。这些发现突出了BRP及其化合物的显著生物活性潜力,表明它们在体外和计算机上作为治疗药物的潜力。建议进一步研究其作用机制和治疗应用。
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引用次数: 0
Identification of components that increase NAD+ levels in oxygen-glucose deprived HUVEC s from Schisandra chinensis (Turcz.) Baill. Based on spectrum-effect correlation analysis and target cell extraction. 五味子缺氧葡萄糖HUVEC中增加NAD+水平的成分鉴定(图)Baill。基于光谱效应相关分析和目标细胞提取。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-12-17 DOI: 10.1016/j.fitote.2024.106347
Liwenyu Chen, Yi Yu, Min Lin, Ming Liang, Chen Yang, Xutian Kan, Xiaoliang Lin, Jin Qi

Schisandra chinensis (Turcz.) Baill, a traditional Chinese medicine with significant nourishing functions, has a regulatory effect on the cardiovascular system, digestive system, central nervous system, and endocrine and immune systems. It can protect the cardiovascular system, improve immunity, and has anti-oxidant and anti-aging properties. This study aimed to identify the chisandra chinensis components that increased NAD+ levels, by using spectrum-effect analysis and experimental validations. First, the quality of the S. chinensis extract was analyzed by HPLC-MS. The extract of S. chinensis increased the NAD+ levels of HUVECs during oxygen and glucose deprivation injury, and protected HUVEC s from injury from superoxide dismutase (SOD) and aging. The relationships of spectral effects were studied by partial least square regression. Coupled with target cell extraction, the material basis for increasing NAD+ levels in S. chinensis was obtained. The pharmacological activity of S. chinensis was verified at the cellular level. The related enzymes of the NAD+ synthesis and decomposition pathways were identified, showing that S. chinensis increased the level of NAD+ by increasing the activity of related enzymes in the synthesis pathways of NMNAT1, NMNAT2, NMNAT3, and NAMPT, but had no effect on the decomposition pathway. Finally, four constituents were confirmed, in vitro, to be the basis of S. chinensis-induced increases in the levels of NAD+. The EC50 values of the four constituents were also determined.

五味子(土耳其)牛耳是一种具有显著滋补功能的中药,对心血管系统、消化系统、中枢神经系统、内分泌和免疫系统都有调节作用。它可以保护心血管系统,提高免疫力,并具有抗氧化和抗衰老的特性。本研究旨在通过光谱效应分析和实验验证,鉴定五味子中提高NAD+水平的成分。首先,采用高效液相色谱-质谱法对五味子提取物进行质量分析。五味子提取物可提高缺氧和葡萄糖剥夺损伤时HUVEC细胞NAD+水平,保护HUVEC细胞免受超氧化物歧化酶(SOD)损伤和衰老。利用偏最小二乘回归研究了光谱效应之间的关系。结合靶细胞的提取,获得了提高五味子NAD+水平的物质基础。在细胞水平上验证了五味子的药理活性。对NAD+合成和分解途径的相关酶进行了鉴定,结果表明,羊草通过提高NMNAT1、NMNAT2、NMNAT3和NAMPT合成途径中相关酶的活性来提高NAD+水平,但对分解途径没有影响。最后,在体外实验中,四种成分被证实是中国葡萄球菌诱导NAD+水平升高的基础。测定了四种成分的EC50值。
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引用次数: 0
Pentacyclic triterpenoids with cytotoxic activity from the stems of Syzygium jambos (L.) Alston. 具有细胞毒性活性的五环三萜类化合物,来自茜草茎(L. Alston)。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-12-12 DOI: 10.1016/j.fitote.2024.106346
Zhilong Liu, Yuepei Huang, Jieting Chen, Lihua Peng, Weilin Qiao, Wei Li, De-An Guo

Phytochemical investigation of the stems of Syzygium jambos (L.) Alston resulted in the isolation of five new pentacyclic triterpenoids, including three oleananes (1, 2, and 5) and two ursanes (3 and 4), along with 23 known compounds (6-28). Their structures were elucidated by comprehensive spectroscopic analysis and chemical methods. All isolated compounds were evaluated for their cytotoxic activities against two lung carcinoma cell lines, H1975 and HCC827. Among them, compounds 2, 7, 11, 13-16, 18, and 23 exhibited significant cytotoxic activities against H1975 and/or HCC827 cells, with IC50 values below 10 μM. Furthermore, the preliminary structure-activity relationships of these pentacyclic triterpenoids are also discussed.

杨木(Syzygium jambos)茎部植物化学研究Alston分离出5个新的五环三萜,包括3个齐墩烷(1、2和5)和2个熊烷(3和4),以及23个已知化合物(6-28)。通过综合光谱分析和化学方法对其结构进行了鉴定。所有分离得到的化合物对两种肺癌细胞株H1975和HCC827的细胞毒活性进行了评价。其中化合物2、7、11、13-16、18和23对H1975和/或HCC827细胞具有显著的细胞毒活性,IC50值均在10 μM以下。并初步讨论了这些五环三萜的构效关系。
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引用次数: 0
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