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Dammarane-type triterpenoids from Gynostemma longipes and their protective activities on hypoxia-induced injury in PC12 cells

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Chinese Journal of Natural Medicines 2024年第5期22卷 466-480页

作者： LIANG Haizhen CHEN Xiaojuan LI Qi ZHANG Mengmeng LU Pengxin ZHANG Jie SONG Juan ZHANG Tao GUO Baolin MA Baiping Department of pharmaceutical Sciences Beijing Institute of Radiation MedicineBeijing 100850China institute of Medicinal Plant development Chinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100193China AnKang Chia Tai pharmaceutical Co. Ltd.Shaanxi 725000China

Sixteen new dammarane-type triterpenoid saponins(1-16)featuring diverse structural variations in the side chain at C-17,along with twenty-one known analogues(17-37),have been isolated from the rhizomes of Gynostemma longipes ***,a plant renowned for its medicinal and edible *** structural elucidation of these compounds was accomplished through comprehensive analyses of 1D and 2D NMR and HRMS spectroscopic data,supplemented by comparison with previously reported *** assays on the isolates for their protective effects against hypoxia-induced damage in pheochromocytoma cells(PC12 cells)revealed that nine saponins exhibited significant anti-hypoxic *** investigation into the anti-hypoxia mechanisms of the representative saponins demonstrated that compounds 22 and 36 markedly reduced the levels of hypoxia-induced ***,these compounds were found to decrease the release of lactate dehydrogenase(LDH)and malondialdehyde(MDA),while increasing the activity of superoxide dismutase(SOD),thereby indicating that the saponins could mitigate hypoxia-induced injuries by ameliorating apoptosis and oxidative *** findings offer substantial evidence for the future utilization and development of ***,identifying dammarane-type triterpenoid saponins as its active anti-hypoxic constituents.

关键词： Gynostemma longipes Dammarane-type saponins Anti-hypoxia effect Apoptosis

Novel Pt(IV) complex OAP2 induces STING activation and pyroptosis via mitochondrial membrane remodeling for synergistic chemo-immunotherapy

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Acta Pharmaceutica Sinica B 2024年第4期14卷 1742-1758页

作者： Renming Fan Ruizhuo Lin Shuo Zhang Aohua Deng Yongrui Hai Junyan Zhuang Yang Liu Maosheng Cheng Gaofei Wei institute of Medical Research Northwestern Polytechnical UniversityXi'an 710072China Research&development institute of Northwestern Polytechnical University in Shenzhen Shenzhen 518057China Key Laboratory of Structure-Based Drug Design and Discovery Ministry of EducationSchool of Pharmaceutical EngineeringShenyang Pharmaceutical UniversityShenyang 110016China

Mitochondrial membrane remodeling can trigger the release of mitochondrial DNA (mtDNA), leading to the activation of cellular oxidative stress and immune responses. While the role of mitochondrial membrane remodeling in promoting inflammation in hepatocytes is well-established, its effects on tumors have remained unclear. In this study, we designed a novel Pt(IV) complex, OAP2, which is composed of oxaliplatin (Oxa) and acetaminophen (APAP), to enhance its anti-tumor effects and amplify the immune response. Our findings demonstrate that OAP2 induces nuclear DNA damage, resulting in the production of nuclear DNA. Additionally, OAP2 downregulates the expression of mitochondrial Sam50, to promote mitochondrial membrane remodeling and trigger mtDNA secretion, leading to double-stranded DNA accumulation and ultimately synergistically activating the intracellular cGAS-STING pathway. The mitochondrial membrane remodeling induced by OAP2 overcomes the limitations of Oxa in activating the STING pathway and simultaneously promotes gasdermin-D-mediated cell pyroptosis. OAP2 also promotes dendritic cell maturation and enhances the quantity and efficacy of cytotoxic T cells, thereby inhibiting cancer cell proliferation and metastasis. Briefly, our study introduces the first novel small-molecule inhibitor that regulates mitochondrial membrane remodeling for active immunotherapy in anti-tumor research, which may provide a creative idea for targeting organelle in anti-tumor therapy.

关键词： Anti-tumor drug Prodrug Platinum Chemo-immunotherapy Mitochondrial membrane modeling STING Pyroptosis mtDNA

New phenylbutenoids and terpene glycosides from Ginkgo biloba leaves

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Chinese Journal of Natural Medicines 2024年第2期22卷 161-170页

作者： SUN Zeshi LIN Shan WU Zhi-Li DONG Hong-Yuan XU Xi-Ke LI Hui-Liang WANG Jinxin School of Pharmacy Second Military Medical UniversityShanghai 200433China State Key Laboratory of New Drug and pharmaceutical Process Shanghai Institute of Pharmaceutical IndustryChina State Institute of Pharmaceutical IndustryShanghai 201203China

Our continued works on the chemical constituents of Ginkgo biloba(***)leaves has led to the isolation of two novel phenylbutenoids(1,2),along with five previously unidentified terpene glycosides(3−7).Among them,compounds 1 and 2 represent unique(Z)-phenylbutenoids,3−6 are megastigmane glycosides,and 7 is identified as a rare bilobanone glycoside(Fig.1).This study marks the first reported isolation of phenylbutenoid and bilobanone glycoside from *** chemical structures of these compounds were elucidated through extensive spectroscopic analysis,including HR-ESI-MS and various 1D and 2D NMR ***,the absolute configurations of these molecules were determined using Mosher’s method,ECD experiments,and Cu-KαX-ray crystallographic analyses.

关键词： Ginkgo biloba Phenylbutenoid Megastigmane glycoside Bilobanone glycoside

Real-time model correction using Kalman filter for Raman-controlled cell culture processes

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Chinese Journal of Chemical Engineering 2024年第6期70卷 251-260页

作者： Xiaoxiao Dong Zhuohong He Xu Yan Dong Gao Jingyu Jiao Yan Sun Haibin Wang Haibin Qu pharmaceutical Informatics institute College of Pharmaceutical SciencesZhejiang UniversityHangzhou 310058China Hisun Biopharmaceutical Co.Ltd. Hangzhou 311404China

Raman spectroscopy has found extensive use in monitoring and controlling cell culture *** this context,the prediction accuracy of Raman-based models is of paramount ***,models established with data from manually fed-batch cultures often exhibit poor performance in Raman-controlled ***,there is a need for effective methods to rectify these *** objective of this paper is to investigate the efficacy of Kalman filter(KF)algorithm in correcting Raman-based models during cell ***,partial least squares(PLS)models for different components were constructed using data from manually fed-batch cultures,and the predictive performance of these models was ***,various correction methods including the PLS-KF-KF method proposed in this study were employed to refine the PLS ***,a case study involving the auto-control of glucose concentration demonstrated the application of optimal model correction *** results indicated that the original PLS models exhibited differential performance between manually fed-batch cultures and Raman-controlled *** glucose,the root mean square error of prediction(RMSEP)of manually fed-batch culture and Raman-controlled culture was 0.23 and 0.40 g·L^(-1).With the implementation of model correction methods,there was a significant improvement in model performance within Raman-controlled *** RMSEP for glucose from updating-PLS,KF-PLS,and PLS-KF-KF was 0.38,0.36 and 0.17 g·L^(-1),***,the proposed PLS-KF-KF model correction method was found to be more effective and stable,playing a vital role in the automated nutrient feeding of cell cultures.

关键词： Raman spectroscopy Model correction Algorithm Model-predictive control Bioprocess

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Advancing ophthalmic delivery of flurbiprofen via synergistic chiral resolution and ion-pairing strategies

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Asian Journal of pharmaceutical Sciences 2024年第3期19卷 181-193页

作者： Zhining Ma Yuequan Wang Huiyang He Tong Liu Qikun Jiang Xiaohong Hou School of Pharmacy Shenyang Pharmaceutical University Wuya College of Innovation Shenyang Pharmaceutical University Liaoning Provincial institute of Drug Inspection and Testing School of pharmaceutical Engineering Shenyang Pharmaceutical University

Flurbiprofen （FB）,a nonsteroidal anti-inflammatory drug,is widely employed in treating ocular inflammation owing to its remarkable anti-inflammatory ***,the racemic nature of its commercially available formulation （Ocufen?） limits the full potential of its therapeutic activity,as the （S）-enantiomer is responsible for the desired antiinflammatory ***,the limited corneal permeability of FB significantly restricts its *** this study,we successfully separated the chiral isomers of FB to obtain the highly active （S）-***,utilizing ion-pairing technology,we coupled （S）-FB with various counter-ions,such as sodium,diethylamine,trimethamine（TMA）,and l-arginine,to enhance its ocular bioavailability.A comprehensive evaluation encompassed balanced solubility,octanol-water partition coefficient,corneal permeability,ocular pharmacokinetics,tissue distribution,and in vivo ocular anti-inflammatory activity of each chiral isomer *** the various formulations,S-FBTMA exhibited superior water solubility （about 1–12 mg/ml）,lipid solubility (1owpharmaceutical enterprises focused on drug development with a valuable avenue for improving therapeutic outcomes.

关键词： Flurbiprofen Anti-inflammatory Ophthalmic delivery Chiral resolution Ion-pairing

Charge adaptive phytochemical-based nanoparticles for eradication of methicillin-resistant staphylococcus aureus biofilms

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Asian Journal of pharmaceutical Sciences 2024年第3期19卷 164-180页

作者： Xilong Cui Fanhui Liu Shuang Cai Tingting Wang Sidi Zheng Xinshu Zou Linlin Wang Siqi He Yanhua Li Zhiyun Zhang College of Veterinary Medicine Northeast Agricultural University Heilongjiang Key Laboratory for Animal Disease Control and pharmaceutical development

The intrinsic resistance of MRSA coupled with biofilm antibiotic tolerance challenges the antibiotic treatment of MRSA biofilm ***-based nanoplatform is a promising emerging approach for treatment of biofilm ***,their therapeutic efficacy was restricted by the low drug loading capacity and lack of ***,we constructed a surface charge adaptive phytochemical-based nanoparticle with high isoliquiritigenin (ISL) loading content for effective treatment of MRSA biofilm.A dimeric ISL prodrug (ISL-G2) bearing a lipase responsive ester bond was synthesized,and then encapsulated into the amphiphilic quaternized *** obtained ISL-G2loaded NPs possessed positively charged surface,which allowed cis-aconityl-D-tyrosine(CA-Tyr) binding via electrostatic interaction to obtain ISL-G2@TMDCOS-Tyr *** NPs maintained their negatively charged surface,thus prolonging the blood circulation *** response to low pH in the biofilms,the fast removal of CA-Tyr led to a shift in their surface charge from negative to positive,which enhanced the accumulation and penetration of NPs in the ***,the pH-triggered release of D-tyrosine dispersed the biofilm and lipase-triggered released of ISL effectively kill biofilm *** in vivo study was performed on a MRSA biofilm infected wound *** phytochemical-based system led to～2log CFU (>99%) reduction of biofilm MRSA as compared to untreated wound (P<0.001)with negligible biotoxicity in *** phytochemical dimer nanoplatform shows great potential for long-term treatment of resistant bacterial infections.

关键词： MRSA biofilm Isoliquiritigenin Dimer prodrug Charge adaptive Responsive nanoparticles

The role of Piezo1 and Piezo2 proteins in tissue engineering:A Comprehensive review

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Engineered Regeneration 2024年第2期5卷 170-185页

作者： Tejaswini Tadge Ashwini Pattewar Namdev More Srivalliputtur Sarath Babu Ravichandiran Velyutham Govinda Kapusetti National institute of pharmaceutical Education and Research KolkataWest Bengal 700054India National institute of pharmaceutical Education and Research AhmedabadGujarat 382355India

Almost every life form,from the tiniest bacterium to humans,is mechanosensitive,implying it can use mechani-cal stresses to trigger certain physiological responses in the form of electric *** largely relies on ion channels that respond to mechanical forces,such as the epithelial sodium channels/degenerins,tran-sient receptor potential channel,and the two-pore domain potassium ***1 and Piezo2 proteins were discovered to be the biggest non-selective mechanosensitive cation channels in the cell membrane.A substantial amount of research has previously been published on the Piezo channel’s function in touch sensation,balance,and cardiovascular ***,the mechanistic perspective must be refined to fully understand the role of Piezo proteins in tissue *** review centers on the latest insights into the structure of Piezo chan-nels,activation mechanisms,and its interactions with cytoskeletal components,by emphasizing the physiological activities of Piezo channels in different *** study also places focus on the possibilities of targeting this cation channel family as a tissue regeneration aid.

关键词： Piezo1 Piezo2 Mechanotransduction Tissue regeneration Mechanoreceptors

Design and optimization of a greener sinomenine hydrochloride preparation process considering variations among different batches of the medicinal herb

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Chinese Journal of Chemical Engineering 2024年第7期71卷 77-90页

作者： Dandan Ren Jiale Xie Tianle Chen Haibin Qu Xingchu Gong pharmaceutical Informatics institute College of Pharmaceutical SciencesZhejiang UniversityHangzhou 310058China National Key Laboratory of Chinese Medicine Modernization Zhejiang UniversityHangzhou 310058China Jinhua institute of Zhejiang University Jinhua 321016China

The current methods used to industrially produce sinomenine hydrochloride involve several issues,including high solvent toxicity,long process flow,and low atomic utilization efficiency,and the greenness scores of the processes are below 65 *** solve these problems,a new process using anisole as the extractant was *** exhibits high selectivity for sinomenine and can be connected to the subsequent water-washing *** alkalization of the medicinal material,heating extraction,water washing,and acidification crystallization were carried *** process was modeled and *** design space was *** recommended operating ranges for the critical process parameters were 3.0–4.0 h for alkalization time,60.0–80.0℃ for extraction temperature,2.0–3.0(volume ratio)for washing solution amount,and 2.0–2.4 mol·L^(-1) for hydrochloric acid *** new process shows good robustness because different batches of medicinal materials did not greatly impact crystal purity or sinomenine transfer *** sinomenine transfer rate was about 20%higher than that of industrial *** greenness score increased to 90 points since the novel process proposed in this research solves the problems of long process flow,high solvent toxicity,and poor atomic economy,better aligning with the concept of green chemistry.

关键词： Sinomenine hydrochloride Process optimization Anisole

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High-throughput discovery of highly selective reversible hMAO-B inhibitors based on at-line nanofractionation

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Acta Pharmaceutica Sinica B 2024年第4期14卷 1772-1786页

作者： Yu Fan Jincai Wang Jingyi Jian Yalei Wen Jiahao Li Hao Tian Jacques Crommen Wei Bi Tingting Zhang Zhengjin Jiang institute of pharmaceutical Analysis/Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research/International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug development of Ministry of Education(MOE)of China/College of Pharmacy Jinan UniversityGuangzhou 510632China KU Leuven-University of Leuven Pharmaceutical AnalysisDepartment of Pharmaceutical and Pharmacological SciencesLeuven 3000Belgium Laboratory of Analytical pharmaceutical Chemistry Department of Pharmaceutical SciencesCIRMUniversity of LiegeLiege B-4000Belgium Department of Neurology the First Affiliated Hospital of Jinan University/Clinical Neuroscience Institutethe First Affiliated Hospital of Jinan UniversityGuangzhou 510630China

Human monoamine oxidase B(hMAO-B)has emerged as a pivotal therapeutic target for Parkinson's *** to adverse effects and shortage of commercial drugs,there is a need for novel,highly selective,and reversible hMAO-B inhibitors with good blood-brain barrier *** this study,a high-throughput at-line nanofractionation screening platform was established with extracts from Chuanxiong Rhizoma,which resulted in the discovery of 75 active compounds,including phenolic acids,volatile oils,and phthalides,two of which were highly selective novel natural phthalide hMAO-B inhibitors that were potent,selective,reversible and had good blood‒brain *** docking and molecular dynamics simulations elucidated the inhibition ***(IC_(50)=103 nmol/L;SI=645)and neocnidilide(IC_(50)=131 nmol/L;SI=207)demonstrated their excellent potential as hMAO-B *** offset the limitations of deactivating enzymes associated with irreversible hMAO-B inhibitors such as *** SH-SY5Y cell assays,sedanolide(EC_(50)=0.962μmol/L)and neocnidilide(EC_(50)=1.161μmol/L)exhibited significant neuroprotective effects,comparable to the positive drugs rasagiline(EC_(50)=0.896μmol/L)and safinamide(EC_(50)=1.079μmol/L).These findings underscore the potential of sedanolide as a novel natural hMAO-B inhibitor that warrants further development as a promising drug candidate.

关键词： Human monoamine oxidase B inhibitors High-throughput screening At-linenanofractionation Parkinson's disease Cellular neuroprotection Traditional Chinese medicines(TCMs)