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Novel phenanthrene/bibenzyl trimers from the tubers of Bletilla striata attenuate neuroinﬂammation via inhibition of NF-κB signaling pathway

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Chinese Journal of natural medicines 2024年第5期22卷 441-454页

作者： SHAO Siyuan SUN Mohan MA Xianjie JIANG Jianwei TIAN Jinying ZHANG Jianjun YE Fei LI Shuai State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China

Five novel(9,10-dihydro)phenanthrene and bibenzyl trimers,as well as two previously identified biphenanthrenes and bibenzyls,were isolated from the tubers of Bletilla *** structures were elucidated through comprehensive analyses of NMR and HRESIMS spectroscopic *** absolute configurations of these compounds were determined by calculating rotational energy barriers and comparison of experimental and calculated ECD *** 5b and 6 exhibited inhibitory effects on LPS-induced NO production in BV-2 cells,with IC_(50) values of 12.59±0.40 and 15.59±0.83μmol·L^(-1),respectively.A mechanistic study suggested that these compounds may attenuate neuroinflammation by reducing the activation of the AKT/IκB/NF-κB signaling ***,compounds 3a,6,and 7 demonstrated significant PTP1B inhibitory activities,with IC_(50) values of 1.52±0.34,1.39±0.11,and 1.78±0.01μmol·L^(-1),*** investigation revealed that compound 3a might inhibit LPS-induced PTP1B overexpression and NF-κB activation,thereby mitigating the neuroinflammatory response in BV-2 cells.

关键词： Bletilla striata Phenanthrene/bibenzyl trimer NO inhibition AKT/IκB/NF-κB signaling pathway PTP1B inhibitory effect

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Neosophoflavonoids A–C, A class of highly oxidized hybrid flavonoids from Sophora flavescens with antidiabetic effects

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Chinese Chemical Letters 2024年第10期35卷 295-298页

作者： Xu Zhang Jiang Li Kai-Zhou Lu Ya-Nan Yang Jian-Shuang Jiang Xiang Yuan Zi-Ming Feng Fei Ye Pei-Cheng Zhang State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences and PekingUnionMedical CollegeBeijing100050China

Three highly oxidized hybrid flavonoids neosophoflavonoids A–C(1,2a,and 2b)were isolated from the roots of Sophora *** A possesses a unique highly oxidized heptacyclic6/6/6/6/6/6/5 *** B and C are isomers and share the same highly oxidized hexacyclic 6/6/6/6/6/6 *** planar structures were elucidated from 1D/2D nuclear magnetic resonance(NMR),ultraviolet spectroscopy(UV),infrared spectroscopy(IR),and high resolution electrospray ionization mass spectroscopy(HRESIMS)*** absolute configurations were determined by thorough GIAO13C NMR(DP4+)calculation protocol and electronic circular dichroism(ECD)calculation *** plausible biosynthetic routes for the compounds were also *** compounds exhibited significant protein tyrosine phosphatase-1B(PTP1B)inhibitory activity with half maximal inhibitory concentration(IC_(5)0)values 3.94±0.01,0.38±0.13,and 0.70±0.01μmol/L,*** addition,compared to a positive control fenofibrate(Feno)at 20μmol/L,compounds 2a and 2b exhibited stronger inhibitory effects on lipid accumulation in the oleic acid(OA)-induced cell model at 5 and 10μmol/L.

关键词： Sophora flavescens Highly oxidized hybrid flavonoids Neosophoflavonoids A-C PTP1B inhibition Lipid accumulation inhibition

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Full biosynthetic pathway of pyrrolobenzoxazines

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Chinese Chemical Letters 2025年第1期36卷 433-436页

作者： Kunya Wang Bingyu Liu Daojiang Yan Jian Bai Haibo Yu Youcai Hu State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China

Pyrrolobenzoxazines are a rare terpene-amino acid family of natural products with potent biological ***,we reported the full biosynthetic pathway of paeciloxazine(1),a typical pyrrolobenzoxazine,with significant insecticidal *** on heterologous expression,chemical complement experiment,and in vitro biochemical assays,we demonstrated the sesquiterpene portion of 1 derived from discontinuously oxidations of amorphdiene,in which P450 monooxygenase PaxH catalyzed a cascade of hydroxylation and epoxidation,while two flavin dependent monooxygenases are involved in the transformation of the esterified tryptophan into a pyrrolobenzoxazine ***,a total of 15 compounds were generated through heterologous expression,of which 13,17 and 20 showed potential antiepileptic *** study fully elucidated the biosynthetic pathway of paeciloxazine(1)and showed the diversity and complexity of constructing natural products by organisms.

关键词： Pyrrolobenzoxazines Paeciloxazine Biosynthesis P450 monooxygenase Antiepileptic activity

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The raphe nuclei are the early lesion site of gastric α-synuclein propagation to the substantia nigra

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Acta Pharmaceutica Sinica B 2024年第5期14卷 2057-2076页

作者： Chenglu Zhang Ruxue Bo Tiantian Zhou Naihong Chen Yuhe Yuan State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Chinese Academy of Medical Sciences&Peking Union Medical College Institute of Materia MedicaBeijing 100050China

Parkinson's disease(PD)is a neurodegeneration disease withα-synuclein accumulated in the substantia nigra pars compacta(SNpc)and most of the dopaminergic neurons are lost in SNpc while patients are diagnosed with *** the pathology at an early stage contributes to the development of the disease-modifying *** the“gut–brain”hypothesis is proposed to explain the underlying mechanism,where the earlier lesioned site in the brain of gastricα-synuclein and howα-synuclein further spreads are not fully *** we report that caudal raphe nuclei(CRN)are the early lesion site of gastricα-synuclein propagating through the spinal cord,while locus coeruleus(LC)and substantia nigra pars compacta(SNpc)were further affected over a time frame of 7 ***α-synuclein propagation via CRN leads to neuron loss and disordered neuron activity,accompanied by abnormal motor and non-motor *** neuron circuits are observed among CRN,LC,and SNpc,which contribute to the venerability of dopaminergic neurons in *** results show that CRN is the key region for the gastricα-synuclein spread to the *** study provides valuable details for the“gut–brain”hypothesis and proposes a valuable PD model for future research on early PD intervention.

关键词： Raphe nuclei α-Synuclein Gastrointestinal tract Electrophysiology Locus coeruleus Substantia nigra pars compacta Parkinson's disease Spinal cord

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Glycnsisitin A:A promising bicyclic peptide against heart failure that facilitates TFRCmediated uptake of iron in cardiomyocytes

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Acta Pharmaceutica Sinica B 2024年第7期14卷 3125-3139页

作者： Jichao Zhou Yuanyuan Liu Xiaoli Wei Meng Yuan Xu Zhang Lingfeng Qin Bing Cui Pingping Li Jing Zhang Ziming Feng Jianshuang Jiang Xiang Yuan Ruibing Xu Zhimeng Zhang Peicheng Zhang Xiaowei Zhang Yanan Yang State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China

Zhigancao decoction is a traditional prescription for treating irregular pulse and palpitations in *** the monarch drug of Zhigancao decoction,the bioactive molecules of licorice against heart diseases remain *** established the HRESIMS-guided method leading to the isolation of three novel bicyclic peptides,glycnsisitins A-C(1-3),with distinctive C-C and C-O-C side-chain-toside-chain linkages from the roots of Glycyrrhiza uralensis(Licorice).Glycnsisitin A demonstrated stronger cardioprotective activity than glycnsisitins B and C in an in vitro model of doxorubicin(DOX)-induced cardiomyocyte *** A treatment not only reduced the mortality of heart failure(HF)mice in a dose-dependent manner but also significantly attenuated DOX-induced cardiac dysfunction and myocardial *** set enrichment analysis(GSEA)of the differentially expressed genes indicated that the cardioprotective effect of glycnsisitin A was mainly attributed to its ability to maintain iron homeostasis in the ***,glycnsisitin A interacted with transferrin and facilitated its binding to the transferrin receptor(TFRC),which caused increased uptake of iron in *** findings highlight the key role of bicyclic peptides as bioactive molecules of Zhigancao decoction for the treatment of HF,and glycnsisitin A constitutes a promising therapeutic agent for the treatment of HF.

关键词： Glycyrrhiza uralensis Bicyclic peptides Myocardial energy metabolism Iron homeostasis TFRC

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Effective assignment of positional isomers in dimeric shikonin and its analogs by ^(1)H NMR spectroscopy

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Chinese Chemical Letters 2024年第5期35卷 223-226页

作者： Ling-Hao Zhao Hai-Wei Yan Jian-Shuang Jiang Xu Zhang Xiang Yuan Ya-Nan Yang Pei-Cheng Zhang State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China

An approach for distinguishing two types of positional isomers of dimeric shikonin and its analogs was explored with ^(4)JC,H long-range correlation by prolonging the acquisition time at ^(2,3)JC,H values of 2.0 and ***,the ^(1)H(proton)nuclear magnetic resonance(NMR)pattern of phenolic hydroxyl protons was developed as a“diagnosis signal”to ascertain the relative location of each side chain in DMSO-d_(6) at sample concentrations of 0.022-0.034 mol/*** chemical shift differences of 0.6ppm between OH-5' and OH-1 and between OH-8'and OH-4 are assigned to Type A and Type B,*** reported ambiguous structures were corrected by this ***,the steric structures of isolated compounds were elucidated by quantum chemical calculations of electronic circular dichroism(ECD)spectra.

关键词： Arnebia euchroma Dimeric hydroxyl naphthoquinones Positional isomers ^(1)H NMR spectroscopy Chemical shift difference

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A multi-enzymatic cascade reaction for the synthesis of bioactive C-oligosaccharides

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Chinese Chemical Letters 2024年第6期35卷 451-455页

作者： Kebo Xie Qian Zhang Fei Ye Jungui Dai State Key Laboratory of Bioactive Substance and Function of Natural Medicines CAMS Key Laboratory of Enzyme and Biocatalysis of Natural Drugs and NHC Key Laboratory of Biosynthesis of Natural ProductsInstitute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China

C-Oligosaccharides are rare in nature and possess diverse ***,their chemical synthesis faces many *** this work,enzymatic introduction of C-linked sugar chains to target aglycones was successfully achieved by multi-enzymatic cascade reactions.A C-glycosyltransferase from Aloe barbadensis was employed to introduce the first C-linked glucose and then a cyclomaltodextrin glucanotransferase from Bacillus licheniformis was used to extend the sugar chain.A total of twenty C-oligosaccharides with 2-6 sugars were synthesized from scale-up reactions and exhibited good water solubility and sodium-dependent glucose transporter 2(SGLT2)inhibitory ***,a glucoamylase was used to control the length of the sugar chain and the C-maltosides were efficiently *** findings not only expanded the structural diversity of C-oligosaccharides,but also provided a strategy for the modification of C-glycoside drugs to improve the druggability.

关键词： C-Oligosaccharides C-Glycosyltransferase Cyclomaltodextrin glucanotransferase Glucoamylase Enzymatic synthesis SGLT2 inhibitory activity

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A fungal CYP from Beauveria bassiana with promiscuous steroid hydroxylation capabilities

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Chinese Chemical Letters 2024年第5期35卷 218-222页

作者： Yu Peng Yue Wang Tian-Jiao Chen Jing-Jing Chen Jin-Ling Yang Ting Gong Ping Zhu State Key Laboratory of Bioactive Substance and Function of Natural Medicines NHC Key Laboratory of Biosynthesis of Natural ProductsCAMS Key Laboratory of Enzyme and Biocatalysis of Natural DrugsInstitute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China

Hydroxylation of steroid core is critical to the synthesis of steroid *** sp^(3) C-H hydroxylation is challenging through chemical catalysis,alternatively,fungal biotransformation offers a possible solution to this ***,mining and metabolic engineering of cytochrome P450 monooxygenases(CYPs)is usually regarded as a more eco-friendly and efficient ***,we report the mining and identification of a new steroid CYP(CYP68BE1)from Beauveria bassiana by transcriptomics,heterologous expression,in vivo and in vitro functional *** catalytic promiscuity of CYP68BE1 was explored,and CYP68BE1 showed promiscuously and catalytically versatile,which is qualified for monohydroxylation on C11α,C1α,C6βand dihydroxylation on C1β,11αand C6β,11αof six steroids,leading to the production of key steroid intermediates required in the industrial synthesis of some indispensable steroid *** dynamics simulations were performed,revealing the molecular basis of different binding orientations of CYP68BE1 with different *** discovery of CYP68BE1 offers a promising biocatalyst for enriching the steroid structural and functional diversity,which also can be applied to biosynthesize valuable steroid drug intermediates.

关键词： Fungal CYPs Steroid hydroxylase Beauveria bassiana Promiscuous biocatalyst Molecular dynamics

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Editing function of type Ⅱ thioesterases in the biosynthesis of fungal polyketides

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Chinese Chemical Letters 2024年第10期35卷 325-328页

作者： Fenglin Jiang Anan Liu Qian Wei Youcai Hu State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China

Polyketide synthases(PKSs)are megasynthases with multiple autonomously folding domains,which operate cooperatively in the PKS assemblies to synthesize specific polyketide *** nonreactive intermediates tethered to acyl carrier protein(ACP)domain in the PKS will block the elongation process of polyketide *** this study,we systematically elucidate the editing function of fungal typeⅡthioesterases(TEIIs)to hydrolyze ACP domain-bounded nonreactive acyl groups,which are uploaded by substrate promiscuous fungal phosphopantetheinyl ***,the TEIIs encoded in gene clusters of nonreducing PKS with reductase domain exhibit universal editing ***,editing function was also found for TEIIs encoded in gene clusters of highly-reducing PKS with condensation ***,the editing TEIIs with function of recovery PKS are applied to improve the yield of the fungal polyketides in *** study provides valuable insights into the editing process of fungal PKSs,highlights the crucial role of TEIIs in enhancing polyketide production and introduces a novel metabolic engineering strategy for fungal polyketide biosynthesis by leveraging the editing function of TEIIs.

关键词： Editing enzyme Type II thioesterase Biosynthesis Polyketide synthase Metabolic engineering

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Penicillin G acylase-responsive near-infrared fluorescent probe:Unravelling biofilm regulation and combating bacterial infections

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Chinese Chemical Letters 2024年第11期35卷 423-429页

作者： Yang Liu Leilei Zhang Kaixuan Liu Ling-Ling Wu Hai-Yu Hu State Key Laboratory of Bioactive Substance and Function of Natural Medicines Beijing Key Laboratory of Active Substance Discovery and Druggability EvaluationInstitute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China

Antibiotic resistance poses a critical threat to human healthcare,largely driven by bacterial *** biofilms resist the immune system and antibiotics,rendering enclosed microbial cells 10-1000times more antibiotic-resistant than planktonic cells,leading to severe ***,there is an urgent need to develop innovative tools for investigating biofilm regulators and devising novel antibacterial *** this study,we developed Cy-NEO-PA,a near-infrared(NIR)fluorescent probe responsive to penicillin G acylase(PGA),with bacteria-targeting *** probe was designed to visualize the influence of environmental factors on biofilm formation in Acinetobacter baumannii(***).Our findings demonstrated that glucose suppressed PGA production,leading to enhanced biofilm formation,whereas phenylacetic acid(PAA)stimulated PGA production and inhibited biofilm formation in *** observations highlight the remarkable capability of Cy-NEO-PA to accurately measure PGA dynamics,shedding light on the critical role of PGA in biofilm ***,Cy-NEO-PA exhibited excellent biocompatibility,potent reactive oxygen species(ROS)generation,efficient photothermal conversion,and bacteria-targeting abilities,making it a promising agent for combating bacterial infections and promoting wound healing through photothermal(PTT)/photodynamic(PDT)*** discoveries emphasize the significant role of PGA in antibacterial therapy and offer valuable insights for the design of effective strategies targeting PGA to combat biofilm-associated infections.

关键词： Penicillin G acylase Phototherapy Biofilm regulation Wound healing Photothermal Photodynamic

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