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Food Science and Human Wellness 2023年第2期12卷 647-661页

作者： Siyuan Su Xiang Ding Yiling Hou Binbin Liu Zhouhe Du Junfeng Liu Key Laboratory of Southwest China Wildlife Resources Conservation College of Life SciencesChina West Normal UniversityNanchong 637009China Sericultural Research Institute Sichuan Academy of Agricultural SciencesNanchong 637000China College of Environmental Science and Engineering China West Normal UniversityNanchong 637009China

A new water-soluble heteropolysaccharide with a molecular weight of 15 k Da was isolated from the fruiting bodies of Boletus reticulatus Schaeff.Structural characterization results revealed that B.reticulatus Schaeff polysaccharide(BRS-X)had a backbone of 1,6-linkedα-D-galactose and 1,2,6-linkedα-D-galactose which branches were mainly composed of a terminal 4-linkedβ-D-glucose and the ratio of D-galactose and D-glucose was 5:1.Bioactivity assays indicated that BRS-X displayed a strong proliferative activity in T cells and B cells and promoted the secretion of immunoglobulin G(Ig G),Ig E,Ig D and Ig M.In addition,BRS-X could facilitate the proliferation and phagocytosis of RAW264.7 cells and could significantly inhibit the growth of tumors in S180-bearing mice.The results of transcriptome sequencing analysis illustrated that total 46 genes enriched in MAPK and total 34 genes enriched in PI3 K/Akt signaling pathways in BRS-X group.The protein VEGF and VEGFR expression were significantly reduced under the treatment with BRS-X.These findings provide a scientific basis for the edible and medicinal value of BRS-X.

关键词： Boletus reticulatus Schaeff Polysaccharides Structure identification Immunomodulatory activity antitumor activity

A novel lectin from mushroom Phellodon melaleucus displays hemagglutination activity,and antitumor activity in a B16 melanoma mouse model

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Food Science and Human Wellness 2023年第5期12卷 1885-1892页

作者： Yuanhui Li Peng Wang Zejun Zhang Qinghong Liu Department of Vegetables College of HorticultureChina Agricultural UniversityBeijing 100193China College of Food Science&Nutritional Engineering China Agricultural UniversityBeijing 100193China

A novel lectin(termed PML)was purified from fruiting bodies of the edible mushroom Phellodon melaleucus(division Basidiomycota)by ion exchange,hydrophobic interaction,and gel filtration chromatographies,with overall titer recovery~60%and 20-fold purification.PML displayed hemagglutination activity 13319 units/mg toward rabbit erythrocytes.SDS-PAGE and gel filtration analyses revealed that PML is a homodimeric lectin with a molecular weight of 28.8 kDa.PML hemagglutination activity was not inhibited by various simple sugars or their derivatives,but was enhanced by cations Ca^(2+),Mg^(2+),Zn^(2+),and Cu^(2+).The activity was stable in pH range 6–9 and in the temperature range 20–60°C.Circular dichroism(CD)spectroscopic analysis showed that PML was composed primarily ofβ-sheets with lowα-helix content.In a B16 melanoma mouse model,PML treatment significantly inhibited tumor growth,and increased cytokine IL-10 content.Our findings suggest that PML is a potential anticancer therapeutic agent.

关键词： Phellodon melaleucus Lectin Hemagglutination activity Cytokine IL-10 antitumor activity

Elemene antitumor Drugs Development Based on "Molecular Compatibility Theory" and Clinical Application: A Retrospective and Prospective Outlook

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Chinese Journal of Integrative Medicine 2024年第1期30卷 62-74页

作者： JIANG Xiao-ying SHI Li-ping ZHU Jun-long BAI Ren-ren XIE Tian School of Pharmacy Hangzhou Normal UniversityHangzhou(311121)China Key Laboratory of Elemene Class Anti-cancer Chinese Medicines Engineering Laboratory of Development and Application of Traditional Chinese MedicinesCollaborative Innovation Center of Traditional Chinese Medicines of Zhejiang ProvinceHangzhou Normal UniversityHangzhou(311121)China Good Clinical Practice Center Affliliated Hospital of Nanjing University of Chinese MedicineNanjing(210000)China

Elemene, derived from Curcuma wenyujin, one of the "8 famous genuine medicinal materials of Zhejiang province," exhibits remarkable antitumor activity. It has gained wide recognition in clinical practice for effectiveness on tumors. Dr. XIE Tian introduced the innovative concept of "molecular compatibility theory" by combining Chinese medicine principles, specifically the "monarch, minister, assistant, and envoy" theory, with modern biomedical technology. This groundbreaking approach, along with a systematic analysis of Chinese medicine and modern biomedical knowledge, led to the development of elemene nanoliposome formulations. These novel formulations offer numerous advantages, including low toxicity, well-defined composition, synergistic effects on multiple targets, and excellent biocompatibility. Following the principles of the "molecular compatibility theory", further exploration of cancer treatment strategies and methods based on elemene was undertaken. This comprehensive review consolidates the current understanding of elemene's potential antitumor mechanisms, recent clinical investigations, advancements in drug delivery systems, and structural modifications. The ultimate goal of this review is to establish a solid theoretical foundation for researchers, empowering them to develop more effective antitumor drugs based on the principles of "molecular compatibility theory".

关键词： molecular compatibility theory Chinese integrative medicine elemene antitumor activity drug delivery structural modification

Design of pH-responsive antimicrobial peptide melittin analog-camptothecin conjugates for tumor therapy

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Asian Journal of Pharmaceutical Sciences 2024年第1期19卷 135-146页

作者： Sujie Huang Yuxuan Gao Ling Ma Bo Jia Wenhao Zhao Yufan Yao Wenyuan Li Tongyi Lin Rui Wang Jingjing Song Wei Zhang Institute of Pharmacology School of Basic Medical SciencesLanzhou UniversityLanzhou 730000China Key Laboratory of Preclinical Study for New Drugs of Gansu Province School of Basic Medical Sciences&Research Unit of Peptide ScienceChinese Academy of Medical SciencesLanzhou UniversityLanzhou 730000China State Key Laboratory of Veterinary Etiological Biology College of Veterinary MedicineLanzhou UniversityLanzhou 730000China Lanzhou University Second Hospital Lanzhou UniversityLanzhou 730000China

Melittin,a classical antimicrobial peptide,is a highly potent antitumor agent.However,its significant toxicity seriously hampers its application in tumor therapy.In this study,we developed novel melittin analogs with pH-responsive,cell-penetrating and membranelytic activities by replacing arginine and lysine with histidine.After conjugation with camptothecin(CPT),CPT-AAM-1 and CPT-AAM-2 were capable of killing tumor cells by releasing CPT at low concentrations and disrupting cell membranes at high concentrations under acidic conditions.Notably,we found that the C-terminus of the melittin analogs was more suitable for drug conjugation than the N-terminus.CPT-AAM-1 significantly suppressed melanoma growth in vivo with relatively low toxicity.Collectively,the present study demonstrates that the development of antitumor drugs based on pH-responsive antimicrobial peptide-drug conjugates is a promising strategy.

关键词： Antimicrobial peptide Peptide-drug conjugate Cell-penetrating activity Membrane disruption antitumor activity

Evodiamine-inspired dual inhibitors of histone deacetylase 1(HDAC1) and topoisomerase 2(TOP2) with potent antitumor activity

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Acta Pharmaceutica Sinica B 2020年第7期10卷 1294-1308页

作者： Yahui Huang Shuqiang Chen Shanchao Wu Guoqiang Dong Chunquan Sheng Department of Medicinal Chemistry School of PharmacySecond Military Medical UniversityShanghai 200433China School of Pharmaceutical Sciences Zhengzhou UniversityZhengzhou 450001China

A great challenge in multi-targetingdrug discovery is to identify drug-like lead compounds with therapeutic advantages over single target inhibitors and drug combinations.Inspired by our previous efforts in designing antitumor evodiamine derivatives,herein selective histone deacetylase 1(HDAC1)and topoisomerase 2(TOP2)dual inhibitors were successfully identified,which showed potent in vitro and in vivo antitumor potency.Particularly,compound 30 a was orally active and possessed excellent in vivo antitumor activity in the HCT116 xenograft model(TGI=75.2%,150 mg/kg,p.o.)without significant toxicity,which was more potent than HDAC inhibitor vorinostat,TOP inhibitor evodiamine and their combination.Taken together,this study highlights the therapeutic advantages of evodiamine-based HDAC1/TOP2 dual inhibitors and provides valuable leads for the development of novel multi-targeting antitumor agents.

关键词： Evodiamine Histone deacetylase Topoisomerase Dual inhibitors antitumor activity

LA-D-B1,a novel Abemaciclib derivative,exerts anti-breast cancer effects through CDK4/6

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BIOCELL 2024年第5期48卷 847-860页

作者： LING MA ZIRUI JIANG XIAO HOU YUTING XU ZIYUN CHEN SIYI ZHANG HANXUE LI SHAOJIE MA GENG ZHANG XIUJUN WANG JING JI Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening College of PharmacyJiangsu Ocean UniversityLianyungang222000China School of Medicine Xiamen UniversityXiamen361102China

Background:Regulatory proteins involved in human cellular division and proliferation,cyclin-dependent kinases 4 and 6(CDK4/6)are overexpressed in numerous cancers,including triple-negative breast cancer(TNBC).TNBC is a common pathological subtype of breast cancer that is prone to recurrence and metastasis,and has a single treatment method.As one of the CDK4/6 inhibitors,abemaciclib can effectively inhibit the growth of breast tumors.In this study,we synthesized LA-D-B1,a derivative of Abemaciclib,and investigated its anti-tumor effects in breast cancer.Methods:Cellular viability was assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT)assay.Cell cloning and migration abilities were determined by colony formation assay and wound healing assay.Cell invasion abilities and adhesion were determined by cell invasion assay and cell adhesion assay.The impact of compound LA-D-B1 on cell proliferation and the cell cycle was analyzed through Western blotting,which quantified the levels of proteins associated with the cyclin-dependent kinase(CDK)4/6-cyclin D-Rb-E2F pathway.The in vivo anti-tumor activity of compound LA-D-B1 was investigated using a chick chorioallantoic membrane(CAM)model.Results:The study demonstrated that LA-D-B1 effectively suppressed breast cancer cell proliferation,induced apoptosis,and caused cell cycle arrest.Furthermore,LA-D-B1 reduced the expression of key proteins in the CDK4/6-cyclin D-Rb-E2F pathway,including CDK4,CDK6 and E2F1.The results also indicated significant antitumor activity of LA-D-B1 in a transplanted tumor model.Conclusion:In this study,LA-D-B1 demonstrated a potent anti-tumor effect by effectively suppressing cell proliferation and inhibiting cell cycle progression in breast cancer.These findings highlight the potential of LA-D-B1 as a valuable compound for enhancing therapeutic outcomes and controlling the progression of breast cancer.

关键词： CDK4/6 inhibitor Breast cancer antitumor activity Cell cycle

Synthesis and antitumor activity of Capecitabine Derivatives

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Chemical Research in Chinese Universities 2015年第1期31卷 78-83页

作者： JIA Xuedong LIU Xlujun WANG Jian WANG Minghua GUO Huiyuan LIU Mingliang Institute of Medicinal Biotechnology Chinese Academy of Medical Sciences and Peking Union Medical College Beijing 100050 P. R. China The First Affiliated Hospital of Zhengzhou University Zhengzhou 450052 P. R. China No.5 Hospital of Harbin Harbin 150040 P. R. China

A series of capecitabine derivatives with a Boc group at the N4-position was synthesized and their in vitro antitumor activities against HepG2（liver hepatocellular carcinoma） were primarily evaluated. Some compounds were chosen for further evaluation of their in vivo efficacy on nude mice xenografted human hepatoma HepG2. The results showed that compounds 3 and 6 had considerable in vivo activity against HepG2, with tumor growth inhibition rates of 70% and 64% on day 21, respectively, and 56% and 55% on day 35, respectively, which are roughly comparable to capecitabine（74% and 59% on days 21 and 35, respectively）.

关键词： Capecitabine Derivative antitumor activity

The effect of microneedles on the skin permeability and antitumor activity of topical 5-fluorouracil

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Acta Pharmaceutica Sinica B 2014年第1期4卷 94-99页

作者： Youssef W.Naguib Amit Kumar Zhengrong Cui The University of Texas at Austin College of PharmacyPharmaceutics DivisionAustinTX 78712USA

Topical 5-fluorouracil(5-FU)is approved for the treatment of superficial basal cell carcinoma and actinic keratosis.However,5-FU suffers from poor skin permeation.Microneedles have been successfully applied to improve the skin permeability of small and large molecules,and even nanoparticles,by creating micron-sized pores in the stratum corneum layer of the skin.In this report,the feasibility of using microneedles to increase the skin permeability of 5-FU was tested.Using full thickness mouse skin mounted on Franz diffusion apparatus,it was shown that the flux of 5-FU through the skin was increased by up to 4.5-fold when the skin was pretreated with microneedles(500μm in length,50μm in base diameter).In a mouse model with B16-F10 mouse melanoma cells implanted in the subcutaneous space,the antitumor activity of a commercially available 5-FU topical cream(5%)was significantly enhanced when the cream was applied on a skin area that was pretreated with microneedles,as compared to when the cream was simply applied on a skin area,underneath which the tumor cells were implanted,and without pretreatment of the skin with microneedles.Fluorouracil is not approved for melanoma therapy,but the clinical efficacy of topical 5-FU against tumors such as basal cell carcinoma may be improved by integrating microneedle technology into the therapy.

关键词： Microneedles 5-Fluorouracil Cytotoxicity Melanoma Immunohistochemistry Flux Transdermal antitumor activity Skin permeability

Synthesis and antitumor activity Evaluation of γ-Monofluorinated and γγy-Difluorinated Goniothalamin Analogues

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Chinese Journal of Chemistry 2013年第6期31卷 805-812页

作者： Yi Yang Zhenjun Yang Chunru Cheng Fengling Qing School of Chemistry and Pharmaceutical Engineering Sichuan University of Science & Engineering Zigong Sichuan 643000 China Key Laboratory of Organofluorine Chemistry Shanghai Institute of Organic Chemistry Chinese Academy of Sciences Shanghai 200032 China State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical Sciences Peking University 38 Xueyuan Road Beijing 100083 China

A series of novel γ,γ-difluorinated Goniothalamin analogues 4a--4i and 6a--6i were synthesized. The key steps included the construction of C-5 stereocenter adjacent to gem-difluoromethylene group by way of lipase AK catalyzed kinetic resolution, the introduction of aryl group via Stille coupling, and lactonization by 1,5-oxidative cycli- zation. These γ,γ-difluorinated Goniothalamin analogues 4a-4i and their enanfiomers 6a--6i, together with several corresponding 7-monofluorinated Goniothalamin analogues were biologically evaluated against four different cancer cell lines. Compound 7h showed a nearly equivalent potency as the parent （R）-Goniothalamin in the micromolar range. The different fluorine effects between fluoromethylene and gem-difluoromethylene on antitumor activity were discussed through the analysis of bioassay data.

关键词： Goniothalamin Stille coupling fluorine antitumor activity

Synthesis, Crystal Structure and antitumor activity of 6,7,8-Trimethoxy-1-(4-methoxy-3-nitrophenyl)-4- (pyridin-4-ylmethyl)-3,4-dihydroisoquinoline

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Chinese Journal of Structural Chemistry 2011年第5期30卷 717-723页

作者：朱雯雯宋云龙郑灿辉吕加国陈军黄晶晶周有骏朱驹 Department of Medicinal Chemistry School of PharmacyThe Second Military Medical University Department of Pharmacy Chengdu Military Command General Hospital

A novel class of 3,4-dihydroisoquinolines （7a～e） was designed, synthesized and characterized by IR, NMR and ESI-MS. The crystal structure of compound 7a （6,7,8-trime- thoxy-1-（4-methoxy-3-nitrophenyl）-4-（pyridin-4-methyl）-3,4-dihydroisoquinoline, C25H25N3O6, Mr=463.48） was determined by X-ray diffraction analysis. The crystal belongs to the monoclinic system, space group P21/n with a=12.074（5）, b=12.896（6）, c=15.450（7）, β=105.846（5）°, V=2314.4（17） 3, Z=4, Dc=1.330 Mg/m3, μ（MoKα）=0.096 mm-1, F（000）=976, S=0.991, the final R=0.0467 and wR=0.1231 for 4545 unique reflections （Rint=0.0656） with 3117 observed ones. The bioassay showed that compounds 7a～e exhibit moderate antitumor activities in vitro.

关键词： 3,4-dihydroisoquinoline crystal structure synthesis antitumor activity