Acta Pharmaceutica

Acta Pharmaceutica Sinica

Sinica BB2024;14(5):iii–xi
2019;9(4):724e733

Chinese Pharmaceutical Association

Institute of Materia Medica, Chinese Academy of Medical Sciences

Acta Pharmaceutica Sinica B

w w w. e l s ev i e r. c o m / l o c a t e / a p s b
w w w. s c i e n c e d i r e c t . c o m

Graphical
ORIGINAL ARTICLEAbstracts/Acta Pharmaceutica Sinica B, 14 (2024) iii–xi

Emodin
Reviews alleviates cardiac fibrosis by
suppressing activation of cardiac fibroblasts via
Acta Pharmaceutica Sinica B, 14 (2024) 1895

upregulating
Targeting RAF dimers in RASmetastasis associated
mutant tumors: From biology to clinic protein 3
Huanhuan Yin, Qiulin Tang, Hongwei Xia, Feng Bi
Division of Abdominal Cancer, Department of Medical Oncology, Cancer Center and
a,y a,y a,y
Dan Xiao
Laboratory , YueTargeted
of Molecular Zhang Therapy , Rui Wang
in Oncology, , Yujie
West China FuaSichuan
Hospital, , Tong Zhoub,
University, Chengdu 610041,
a China a a a a
Hongtao Diao
Homo- and heterodimers a
, Zhixia Wang , Yuan Lin , Zhange Li , Lin
of RAF kinases play a pivotal rolecin the signaling transduction and drug resistance
Wen ,
c
Xujuan
in RAS mutantKang
tumors. , Philipp Kopylov , Dmitri Shchekochikhin ,

Yong Zhanga,d,*, Baofeng Yanga,e,*

a
Department of Pharmacology (State-Province Key Laboratories of Biomedicine-Pharmaceutics of China, Key
Laboratory of Cardiovascular Research, Ministry of Education), Harbin Medical University, Harbin 150081, China
b
Department of Pharmacy, The First Affiliated Hospital of Harbin Medical University, HarbinActa Pharmaceutica
150081, China Sinica B, 14 (2024) 1924
c
Department of Preventive
Oligomerization and Emergency
of drug transporters: Cardiology,
Forms, Sechenov
functions, First Moscow State Medical University, Moscow
and mechanisms
119991, Russian Federation
Chunxu a Mei Honga,b
d
InstituteNi
of ,Metabolic Disease, Heilongjiang Academy of Medical Science, Harbin 150086, China
e
aCollege
Departmentof Life Sciences, South
of Pharmacology andChina Agricultural
Therapeutics, University,
Melbourne Guangzhou
School 510642,
of Biomedical Sciences, Faculty of Medicine,
China
Dentistry and Health Sciences, The University of Melbourne, Melbourne 3010, Australia
bGuangdong Provincial Key Laboratory of Protein Function and Regulation in

Agricultural
Received 13 Organisms, Southreceived
November 2018; China Agricultural University,
in revised form 21 MarchGuangzhou 510642,
2019; accepted China2019
2 April
As transmembrane proteins, drug transporters are prone to form oligomers. Oligomeric complexes
formed among drug transporters or with other regulatory proteins may play important roles in transporter
function and expression.

KEY WORDS Abstract Excess activation of cardiac fibroblasts inevitably induces cardiac fibrosis. Emodin has been
used as a natural medicine against several chronic diseases. The objective of this study is to determine
Emodin; Acta Pharmaceutica Sinica B, 14 (2024) 1939
the effects of emodin on cardiac fibrosis and the underlying molecular mechanisms. Intragastric administra-
Cardiac fibrosis;
BileMTA3;
acids and coronavirus disease 2019 tion of emodin markedly decreased left ventricular wall thickness in a mouse model of pathological cardiac
hypertrophy with excess fibrosis induced by transaortic constriction (TAC) and suppressed activation of car-
Xiaoru Huanga,b
Angiotensin II;, Xuening Liua,b, Zijian Lia,b,c
Cardiac fibroblast; diac fibroblasts induced by angiotensin II (AngII). Emodin upregulated expression of metastasis associated
aDepartment of Pharmacy, Peking University Third Hospital, Beijing 100191, China
Mouse protein 3 (MTA3) and restored the MTA3 expression in the setting of cardiac fibrosis. Moreover, overexpres-
bDepartment of Pharmaceutical Management and Clinical Pharmacy, College of
sion of MTA3 promoted cardiac fibrosis; in contrast, silence of MTA3 abrogated the inhibitory effect of
Pharmacy, Peking University, Beijingemodin 100191, China activation. Our findings unraveled the potential of emodin to alleviate cardiac fibrosis
on fibroblast
cDepartment of Cardiology and Institute of Vascular Medicine, Peking University Third
via upregulating MTA3 and highlight the regulatory role of MTA3 in the development of cardiac fibrosis.
Hospital, Beijing Key Laboratory of Cardiovascular Receptors Research, Key Laboratory
of Cardiovascular Molecular Biology and Regulatory Peptides, Ministry of Health, State
Key Laboratory authors.
*Corresponding of Vascular Homeostasis
Tel.: þ86 and fax:
451 86671354; Remodeling, Peking University, Beijing
þ86 451 86669482.
100191, China
E-mail addresses: hmuzhangyong@hotmail.com (Yong Zhang), yangbf@ems.hrbmu.edu.cn (Baofeng Yang).
The
y review summarizes the latest basic and clinical evidence linking bile acid effects to COVID-19 and potential mechanisms.
These authors made equal contributors to this work.
Peer review under responsibility of Institute of Materia Medica, Chinese Academy of Medical Sciences and Chinese Pharmaceutical Association.

https://doi.org/10.1016/j.apsb.2019.04.003
2211-3835ª 2019 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by
Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
iv Contents

Acta Pharmaceutica Sinica B, 14 (2024) 1951

The inhibitory effect of adenosine on tumor adaptive immunity and intervention
strategies
Longsheng Wanga, Jie Zhanga, Wenxin Zhanga, Mingming Zhenga, Hongjie Guoa,
Xiaohui Pana, Wen Lia, Bo Yanga,b, Ling Dinga,c
aZhejiang Province Key Laboratory of Anti-Cancer Drug Research, Institute of
Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang
University, Hangzhou 310058, China
bThe Innovation Institute for Artificial Intelligence in Medicine, Zhejiang University,

Hangzhou 310018, China

cNanhu Brain-Computer Interface Institute, Hangzhou 311100, China

Adenosine suppresses tumor immune cells within the tumor microenvironment by inhibiting antigen presentation, T-cell activation and infiltration,
and T-cell-mediated killing of tumor cells, thereby impairing tumor adaptive immunity.

Acta Pharmaceutica Sinica B, 14 (2024) 1965

Bispecific antibody drug conjugates: Making 1+1>2
Yilin Gua, Zhijia Wanga, Yuxi Wanga,b
aTargeted Tracer Research and Development
Laboratory, Institute of Respiratory Health, Frontiers
Science Center for Disease-Related Molecular
Network, National Clinical Research Center for
Geriatrics, West China Hospital, Sichuan University,
Chengdu 610041, China
bFrontiers Medical Center, Tianfu Jincheng

Laboratory, Chengdu 610212, China

In comparison to traditional ADCs, bispecific antibody drug conjugates present distinct design considerations and properties as the next-generation
ADCs.

Acta Pharmaceutica Sinica B, 14 (2024) 1987

Discovery of GluN2A subtype-selective N-methyl-d-aspartate (NMDA) receptor
ligands
Liyang Jiang, Na Liu, Fabao Zhao, Boshi Huang, Dongwei Kang, Peng Zhan,
Xinyong Liu
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology
(Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of
Medicine, Shandong University, Jinan 250012, China
GluN1/2A subtype NMDA receptor plays a significant role in CNS disorders. This paper
summarized GluN2A subtype selective antagonists, PAMs, and NAMs with their SARs and
biological profiles.

Acta Pharmaceutica Sinica B, 14 (2024) 2006

Oral peptide therapeutics for diabetes treatment: State-of-the-art and future perspectives
Bingwen Dinga,b, Zhu Zhua,c, Cong Guoa,b, Jiaxin Lia,b, Yong Gana,b,d, Miaorong Yua,b
aStateKey Laboratory of Drug Research and Center of Pharmaceutics, Shanghai Institute
of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
bUniversity of Chinese Academy of Sciences, Beijing 100049, China
cSchool of Pharmacy, Henan University, Kaifeng 475004, China
dNMPA Key Laboratory for Quality Research and Evaluation of Pharmaceutical Excipients,

National Institutes for Food and Drug Control, Beijing 100050, China
This review assesses physiological advantages, absorption barriers, and delivery strategies for oral
administration of anti-diabetic peptides, with a focus on their translational potential from both physiological
and commercial perspectives.
 Contents v

Original articles
Acta Pharmaceutica Sinica B, 14 (2024) 2026
ALS-linked C9orf72 dipeptide repeats inhibit starvation-
induced autophagy through modulating BCL2–BECN1
interaction
Shiqiang Xua, Qilian Maa,d, Junwen Shena, Ningning Lia,
Shan Suna,e, Nana Wanga, Yang Chena, Chunsheng Dongf,
Kin Yip Tame, Jochen H.M. Prehnd, Hongfeng Wanga,b,
Zheng Yinga,b,c
aJiangsu Key Laboratory of Neuropsychiatric Diseases and
College of Pharmaceutical Sciences, Soochow University,
Suzhou 215123, China
bMOE Key Laboratory of Geriatric Diseases and

Immunology, College of Pharmaceutical Sciences, Suzhou Medical College of Soochow University, Suzhou 215123, China
cJiangsu Province Engineering Research Center of Precision Diagnostics and Therapeutics Development, Soochow University,

Suzhou 215123, China

dDept. of Physiology & Medical Physics and FUTURE-NEURO Research Centre, Royal College of Surgeons in Ireland, Dublin

D02 YN77, Ireland

eFaculty of Health Sciences, University of Macau, Taipa, Macau 999078, China
fInsititutes of Biology and Medical Science, Soochow University, Suzhou 215123, China

ALS/FTD-linked C9orf72 DPRs inhibit starvation-induced autophagy by enhancing BCL2–BECN1/Beclin 1 interaction. Under this condition,
pharmacological disruption of the interaction between BECN1 and BCL2 can restore autophagy and may therefore reduce C9orf72 DPR-induced
neurotoxicity.

Acta Pharmaceutica Sinica B, 14 (2024) 2039

Exosomes derived from pulmonary metastatic sites enhance osteosarcoma lung
metastasis by transferring the miR-194/215 cluster targeting MARCKS
Pei Yu, Yubao Han, Lulu Meng, Yanyuan Tian, Zhiwei Jin, Jun Luo, Chao Han,
Wenjun Xu, Lingyi Kong, Chao Zhang
State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Bioactive
Natural Product Research, School of Traditional Chinese Pharmacy, China
Pharmaceutical University, Nanjing 211198, China
Exosomes of pulmonary metastatic osteosarcoma transport the miR-194/215 cluster to primary
osteosarcoma, promoting secondary metastasis via the MARCKS/PHLPP/p-AKT/Slug pathway,
while disrupting miR-194/215 delivery and hinders the progression of osteosarcoma.

Acta Pharmaceutica Sinica B, 14 (2024) 2057

The raphe nuclei are the early lesion site of gastric a-synuclein propagation
to the substantia nigra
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 Medica, Beijing 100050, China
This study shows gastric a-synuclein propagates through the spinal cord to the caudal
raphe nuclei, and further induces lesions in the locus coeruleus and substantia nigra via
potential neuronal circuits.
vi Contents

Acta Pharmaceutica Sinica B, 14 (2024) 2077

Targeting PKM2 signaling cascade with salvianic acid A normalizes
tumor blood vessels to facilitate chemotherapeutic drug delivery
Cheng Qiana, Yueke Zhoua, Teng Zhanga, Guanglu Dongb, Mengyao Songa,
Yu Tanga, Zhonghong Weia, Suyun Yub, Qiuhong Shenb, Wenxing Chena,
Jaesung P. Choic, Juming Yand, Chongjin Zhongb, Li Wane, Jia Lif,
Aiyun Wanga, Yin Lua, Yang Zhaoa,b
aJiangsu Key Laboratory for Pharmacology and Safety Evaluation of
Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing
210023, China
bSchool of Medicine & Holistic Integrative Medicine, Nanjing University

of Chinese Medicine, Nanjing 210023, China

cCentre for Inflammation, Faculty of Science, Centenary Institute, School of Life Sciences, University of Technology Sydney,

Sydney NSW 2050, Australia

dJiangsu Key Laboratory of Immunity and Metabolism, Department of Pathogenic Biology and Immunology, National Experimental

Demonstration Center for Basic Medicine Education, Xuzhou Laboratory of Infection and Immunity, Xuzhou Medical University,
Xuzhou 221004, China
eDepartment of General Surgery, Jiangsu Province Hospital of Chinese Medicine, Affiliated Hospital of Nanjing University of

Chinese Medicine, Nanjing 210029, China

fMacquarie Medical School, Faculty of Medicine, Human Health Sciences, Macquarie University, Sydney NSW 2109, Australia

SAA alters endothelial glycolysis via binding to PKM2 and determines the fate of endothelial tight junctions by virtue of regulating b-Catenin/
Claudin-5 axis cascade, thereby inciting tumor vascular normalization.

Acta Pharmaceutica Sinica B, 14 (2024) 2097

DDAH1 promotes neurogenesis and neural repair in cerebral ischemia
Qiming Gaoa, Pinfei Nia, Yilin Wangb, Peiyun Huoa, Xiaojie Zhangc, Sihan Wanga, Fuyao Xiaoa,
Yixuan Lia, Wei Fengd, Juntao Yuand, Teng Zhange, Qiang Lia, Boyu Fana, Yuhao Kana, Zhirui Lia,
Yimiao Qia, Junfei Xinga, Zhenghong Yangb, Haixiao Chenga, Xinran Gaoa, Xiaoyan Fengf, Ming Xuea,
Yang Liuc, Yumin Luob, Zhongbing Lud, Yuming Zhaoa
aDepartment of Pharmacology, School of Basic Medical Sciences, Capital Medical University, Beijing
100069, China
bCerebrovascular Diseases Research Institute and Department of Neurology, Xuanwu Hospital of Capital

Medical University, Beijing 100053, China

cState Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry,

Chinese Academy of Sciences, Beijing 100190, China

dCollege of Life Science, University of Chinese Academy of Sciences, Beijing 100049, China
eDepartment of Laboratory Animal, School of Basic Medical Sciences, Capital Medical University, Beijing 100069, China
fDepartment of Physiology and Pathophysiology, School of Basic Medical Sciences, Capital Medical University, Beijing 100069, China

In the hippocampus, DDAH1 regulates the genes for the synthesis of ACh (Chat, Slc5a7 and Slc18a3) possibly through transcription factor HIF-1a
which promotes neurogenesis and neural repair post-stroke.

Acta Pharmaceutica Sinica B, 14 (2024) 2119

Transcription factor EHF interacting with coactivator AJUBA aggravates malignancy and
acts as a therapeutic target for gastroesophageal adenocarcinoma
Li Penga,b, Yanyi Jiangc, Hengxing Chena, Yongqiang Wanga,b, Qiusheng Land,
Shuiqin Chena,b, Zhanwang Huanga,b, Jingyuan Zhanga,b, Duanqing Tiana,b, Yuntan Qiua,
Diankui Caie, Jiangyun Penga, Daning Lua,b, Xiaoqing Yuana,b, Xianzhu Yangf, Dong Yina,b
aGuangdong Provincial Key Laboratory of Malignant Tumor Epigenetics and Gene Regulation,
Guangdong-Hong Kong Joint Laboratory for RNA Medicine, Sun Yat-sen Memorial Hospital,
Sun Yat-sen University, Guangzhou 510120, China
bMedical Research Center, Sun Yat-sen Memorial Hospital, Sun Yat-sen University, Guangzhou

510120, China
cHefei Institutes of Physical Science, Chinese Academy of Sciences, Hefei 230031, China
dDepartment of Gastrointestinal Surgery, Sun Yat-sen Memorial Hospital, Sun Yat-sen

University, Guangzhou 510120, China

eDepartment of Hepatobiliary Surgery, Sun Yat-sen Memorial Hospital, Sun Yat-sen University, Guangzhou 510120, China
fSchool of Biomedical Sciences and Engineering, South China University of Technology, Guangzhou International Campus,

Guangzhou 511442, China

EHF is upregulated by a core transcriptional regulatory circuitry and promotes malignancy of gastroesophageal adenocarcinoma via AJUBA coactivation
through the KRAS pathway, offering a novel dual-targeting therapeutic strategy.
 Contents vii

Acta Pharmaceutica Sinica B, 14 (2024) 2137

Small molecule conjugates with selective estrogen receptor b agonism promote
anti-aging benefits in metabolism and skin recovery
Tarik Zahra,b, Vijay K. Bodac,d, Jian Gee,f, Lexiang Yua,g, Zhongzhi Wuc,d,
Jianwen Quee,f,h, Wei Lic,d, Li Qianga,g
aNaomi Berrie Diabetes Center, Columbia University, New York, NY 10032, USA
bDepartment of Molecular Pharmacology and Therapeutics, Columbia University,
New York, NY 10032, USA
cDepartment of Pharmaceutical Sciences, College of Pharmacy, University of

Tennessee Health Science Center, Memphis, TN 38163, USA

dDrug Discovery Center, College of Pharmacy, University of Tennessee Health

Science Center, Memphis, TN 38163, USA

eDivision of Digestive and Liver Diseases, Columbia University, New York, NY 10032, USA
fCenter for Human Development, Columbia University, New York, NY 10027, USA
gDepartment of Pathology and Cell Biology, Columbia University, New York, NY 10032, USA
hDepartment of Medicine, Columbia University, New York, NY 10032, USA

The use of selective estrogen receptor b conjugate agonists in mice provides anti-aging benefits in metabolism and skin health.

Acta Pharmaceutica Sinica B, 14 (2024) 2153

5S-Heudelotinone alleviates experimental colitis by shaping the
immune system and enhancing the intestinal barrier in a gut
microbiota-dependent manner
Qing Menga, Jianshuang Guoa, Ke Lvb, Yang Liua, Jin Zhanga,
Mingyue Lia, Xirui Chenga, Shenghua Chenb, Xiaoguang Huoc,
Quan Zhanga, Yue Chena,b, Jing Lia,b
aStateKey Laboratory of Medicinal Chemical Biology, College
of Pharmacy, Nankai University, Tianjin 300353, China
bCollege of Chemistry and Frontiers Science Center for New

Organic Matter, Haihe Laboratory of Sustainable Chemical

Transformations, Nankai University, Tianjin 300071, China
cAccendatech Company, Ltd., Tianjin 300193, China

Natural product 5S-heudelotinone alleviated experimental colitis in a gut microbiota-dependent manner. This work provided a novel candidate for
the treatment of IBD.

Acta Pharmaceutica Sinica B, 14 (2024) 2177

First total synthesis, antitumor evaluation and target identification of
mornaphthoate E: A new tubulin inhibitor template acting on PI3K/Akt signaling
pathway
Peipei Shana, Tao Yeb, Ying-De Tangb, Hui Songb, Chao Wangb, Kongkai Zhuc,
Feifei Yangb, Shi-Lei Zhangd, Pei-Wen Sub, Shuanhu Gaoe, Hua Zhangb
aInstituteof Translational Medicine, the Affiliated Hospital of Qingdao University,
College of Medicine, Qingdao University, Qingdao 266021, China
bSchool of Biological Science and Technology, University of Jinan, Jinan 250022,

China
cAdvanced Medical Research Institute, Cheeloo College of Medicine, Shandong

University, Jinan 250012, China

dCollege of Pharmaceutical Sciences, Soochow University, Suzhou 215127, China
eSchool of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China

The first total synthesis of (±)-mornaphthoate E, identified as tubulin inhibitor, was achieved. The in vitro and in vivo antitumor effects were evaluated
for pure enantiomers and racemate, respectively.
viii Contents

Acta Pharmaceutica Sinica B, 14 (2024) 2194

Branched glycopolymer prodrug-derived nanoassembly combined with a
STING agonist activates an immuno-supportive status to boost anti-PD-L1
antibody therapy
Zhilin Lia,d, Qianfeng Zhanga, Zhiqian Lia, Long Rena, Dayi Pana,
Qiyong Gonga,b,c, Zhongwei Gua, Hao Caia, Kui Luoa,b
aDepartment of Radiology, Huaxi MR Research Center (HMRRC), Clinical
Research Center for Breast, Department of Breast Surgery, Department of
Thoracic Surgery and Institute of Thoracic Oncology, Frontiers Science
Center for Disease-Related Molecular Network, State Key Laboratory of
Biotherapy, West China Hospital Sichuan University, Chengdu 610041,
China
bFunctional and Molecular Imaging Key Laboratory of Sichuan Province,

and Research Unit of Psychoradiology, Chinese Academy of Medical Sciences, Chengdu 610041, China
cDepartment of Radiology, West China Xiamen Hospital of Sichuan University, Xiamen 361021, China
dKey Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, Yunnan Key Laboratory of Research and

Development for Natural Products, School of Pharmacy, Yunnan University, Kunming 650500, China
A branched glycopolymer-EPI prodrug-derived nanoassembly combined with a STING agonist to remodel an immunosuppressive microenvironment
to an immuno-supportive one, thus potentiating the therapy effect of anti-PD-L1 antibodies.

Acta Pharmaceutica Sinica B, 14 (2024) 2210

Rhizoma Drynariae-derived nanovesicles reverse osteoporosis by potentiating
osteogenic differentiation of human bone marrow mesenchymal stem cells via
targeting ERa signaling
Qing Zhaoa,b, Junjie Fengc,d, Fubin Liua,b, Qianxin Liange, Manlin Xiea,b,
Jiaming Donga,b, Yanfang Zoua,b, Jiali Yea,b, Guilong Liua,b,f, Yue Caoa,b,
Zhaodi Guoa,b, Hongzhi Qiaog, Lei Zhenga,b,c,d, Kewei Zhaoa,b
aGuangzhou Key Laboratory of Chinese Medicine Research on Prevention and
Treatment of Osteoporosis, the Third Affiliated Hospital of Guangzhou University
of Chinese Medicine, Guangzhou 510378, China
bGuangdong Engineering Research Center of Chinese Herbal-derived Vesicles,

Guangzhou University of Chinese Medicine, Guangzhou 510006, China

cDepartment of Laboratory Medicine, Nanfang Hospital, Southern Medical

University, Guangzhou 510515, China

dGuangdong Engineering and Technology Research Center for Rapid Diagnostic Biosensors, Nanfang Hospital, Southern Medical

University, Guangzhou 510515, China

eThe Fifth Affiliated Hospital Sun Yat-sen University, Zhuhai 519000, China
fDepartment of Blood Transfusion, Guangdong Heyou International Hospital, Foshan 528306, China
gSchool of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China

The natural product Rhizoma Drynariae-derived nanovesicles isolated and purified from fresh Rhizoma Drynariae, have a high efficacy agonist of
estrogen receptor a and a potential nano-drug platform for the prevention and treatment of postmenopausal osteoporosis.

Acta Pharmaceutica Sinica B, 14 (2024) 2228

A combined nanotherapeutic approach targeting farnesoid X
receptor, ferroptosis, and fibrosis for nonalcoholic steatohepatitis
treatment
Jiangtao Fua, Pingping Zhanga, Zhiguo Suna, Guodong Lua,
Qi Caoa, Yiting Chena, Wenbin Wua, Jiabao Zhanga,b,
Chunlin Zhuanga,b, Chunquan Shenga,b, Jiajun Xuc, Ying Lua,b,
Pei Wanga,b
aThe Center for Basic Research and Innovation of Medicine and
Pharmacy (MOE), School of Pharmacy, Naval Medical University,
Shanghai 200433, China
bNational Demonstration Center for Experimental Pharmaceutical

Education, Naval Medical University/Second Military Medical

University, Shanghai 200433, China
cDepartment of Diving and Hyperbaric Medicine, Naval Special Medical Center, Naval Medical University, Shanghai 200433,

China
The PEGylated and thiolated hollow mesoporous silica nanoparticles (MSN), loaded with OCA, S-nitrosothiol, and liproxstatin-1, exhibit potent
therapeutic action against NASH by simultaneously targeting FXR, ferroptosis, and fibrosis.
 Contents ix

Acta Pharmaceutica Sinica B, 14 (2024) 2247

Radiation-based immunogenic vaccine combined with a macrophage
“checkpoint inhibitor” for boosting innate and adaptive immunity against
metastatic colon cancers
Hongbo Xua, Xianya Qina, Yuanyuan Guoc, Siyu Zhaoa, Xingxing Fenga,
Runzan Zhanga, Tianyi Tiana, Li Konga, Conglian Yanga, Zhiping Zhanga,b
aTongjiSchool of Pharmacy, Huazhong University of Science and Technology,
Wuhan 430030, China
bHubei Engineering Research Center for Novel Drug Delivery System, Wuhan

430030, China
cWuhan Liyuan Hospital of Tongji School of Pharmacy, Huazhong University of

Science and Technology, Wuhan 430077, China

Frozen dying tumor cells (FDT) combined with efferocytosis inhibitors can mobilize dendritc
cells and macrophages simultaneously, thereby eliciting robust innate and adaptive immunity
against peritoneal carcinomatosis in colon cancer.

Acta Pharmaceutica Sinica B, 14 (2024) 2263

A pH/ROS dual-responsive system for effective chemoimmunotherapy
against melanoma via remodeling tumor immune microenvironment
Leilei Wanga, Shanshan Hea, Rong Liua, Yuan Xuea, Yuan Quana,
Rongying Shia, Xueying Yanga, Qing Lina, Xun Suna, Zhirong Zhanga,
Ling Zhangb
aKey Laboratory of Drug-Targeting and Drug Delivery System of the
Education Ministry, West China School of Pharmacy, Sichuan University,
Chengdu 610041, China
bMed-X Center for Materials, College of Polymer Science and Engineering,

Sichuan University, Chengdu 610065, China

An ROS/pH-responsive nanoparticle (DPQ-DOX NPs) was prepared in which doxorubicin
and quercetin worked synergistically, which could enhance the effect of anti-tumor
chemoimmunotherapy by remodeling tumor microenvironment through the COX2–PGE2 axis.

Acta Pharmaceutica Sinica B, 14 (2024) 2281

Inhalable metal–organic framework-mediated cuproptosis
combined with PD-L1 checkpoint blockade for lung metastasis
synergistic immunotherapy
Chongzheng Yana,b, Ying Liua,b, Guozhi Zhaoa,b, Huatian Yanga,b,
Huaiyou Lva,b, Genju Lia,b, Yuhan Lia,b, Yaqing Fua,b,
Fengqin Suna,b, Yafei Fenga,b, Yizhe Lia,b, Zhongxi Zhaoa,b
aDepartment of Pharmaceutics, Key Laboratory of Chemical
Biology of Ministry of Education, School of Pharmaceutical
Sciences, Cheelloo College of Medicine, Shandong University,
Jinan 250012, China
bKey University Laboratory of Pharmaceutics & Drug Delivery

Systems of Shandong Province, School of Pharmaceutical

Sciences, Cheeloo College of Medicine, Shandong University, Jinan 250012, China
A cuproptosis-mediated immunotherapy nanoplatform (OMP) was constructed for lung metastasis treatment by inhalation administration. Moreover,
OMP synergized with PD-L1 checkpoint blockade provoked more powerful anti-tumor immunity to suppress lung metastasis.
x Contents

Acta Pharmaceutica Sinica B, 14 (2024) 2298

Metal natural product complex Ru-procyanidins with quadruple enzymatic activity
combat infections from drug-resistant bacteria
Jie Shana,b, Xu Jina,b, Cong Zhangc, Muchen Huangd, Jianghao Xinge, Qingrong Lib,
Yuyu Cuia, Qiang Niud, Xu Lin Chena, Xianwen Wangb,f
aDepartment of Burns, the First Affiliated Hospital of Anhui Medical University, Hefei
230022, China
bSchool of Biomedical Engineering, Research and Engineering Center of Biomedical

Materials, Anhui Provincial Institute of Translational Medicine, Anhui Medical

University, Hefei 230032, China
cDivision of Gastroenterology, the First Affiliated Hospital of USTC, Division of Life

Science and Medicine, University of Science and Technology of China, Hefei, Anhui
230026, China
dThe Second Clinical Medical College, Anhui Medical University, Hefei 230022, China
eDepartment of Oncology, the First Affiliated Hospital of Anhui Medical University,

Hefei 230022, China

fCollege and Hospital of Stomatology, Anhui Medical University, Key Lab. of Oral

Diseases Research of Anhui Province, Hefei 230032, China

Ru-PC NPs, a novel nanozyme with quadruple enzymatic activity, effectively treats infected wounds. They demonstrate strong antimicrobial effects,
antioxidant capacity, and anti-inflammatory properties, promoting M2 macrophage conversion for enhanced healing.

Acta Pharmaceutica Sinica B, 14 (2024) 2317

In situ autophagy regulation in synergy with phototherapy for breast cancer
treatment
Huijuan Zhanga,b,c, Xiangyang Xuana, Yaping Wanga, Zijun Qia, Kexuan Caoa,
Yingmei Tiana, Chaoqun Wanga, Junbiao Changc,d, Zhenzhong Zhanga,b,
Lin Houa,b
aSchool of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001,
China
bKey Laboratory of Targeting Therapy and Diagnosis for Critical Diseases,

Zhengzhou 450001, China

cCollaborative Innovation Center of New Drug Research and Safety Evaluation,

Zhengzhou 450001, China

dSchool of Chemistry and Molecular Engineering, Zhengzhou University,

Zhengzhou 450001, China

Tf-Te/HCQ was synthesized as a tumor-activated autophagy regulator. It can efficiently block
PTT/PDT-induced autophagy by co-delivery of Fe2+ and hydroxychloroquine (HCQ) for the
synergistic therapy of breast cancer.

Acta Pharmaceutica Sinica B, 14 (2024) 2333

Molecular characterization and structure basis of a
malonyltransferase with both substrate promiscuity and
catalytic regiospecificity from Cistanche tubulosa
Xiao Liua, Yuyu Liua,b, Xiping Xua,b, Wenqian Huanga,b,
Yaru Yana,b, Yingxia Wanga,b, Weisheng Tiana,b,
Ting Moa,b, Xiaoxue Cuia,b, Jun Lia,b, She-Po Shia,
Pengfei Tua
aModern Research Center for Traditional Chinese
Medicine, Beijing Research Institute of Chinese Medicine,
Beijing University of Chinese Medicine, Beijing 100029, China
bModern Research Center for Traditional Chinese Medicine, School of Chinese Materia Medica, Beijing University of Chinese

Medicine, Beijing 100029, China

CtMaT1, a plant malonyltransferase with both unprecedented substrate promiscuity and malonylation regiospecificity, was functionally and structurally
identified, and employed in universal enzymatic synthesis of diverse malonylated glycosides with potential druggabilities.
 Contents xi

Short communication

Acta Pharmaceutica Sinica B, 14 (2024) 2349

Development of an active-site titrant for SARS-CoV-2
main protease as an indispensable tool for evaluating
enzyme kinetics
Rabea Vogeta, Julian Breidenbacha, Tobias Claffa,
Alexandra Hingsta, Katharina Sylvestera,
Christian Steinebacha, Lan Phuong Vua, Renato
H. Weißeb, Ulrike Bartzc, Norbert Sträterb, Christa
E. Müllera, Michael Gütschowa
aPharmaceutical Institute, Pharmaceutical & Medicinal
Chemistry, University of Bonn, Bonn 53121, Germany
bInstitute of Bioanalytical Chemistry, Center for Biotechnology and Biomedicine, Leipzig University, Leipzig 04103, Germany
cDepartment of Natural Sciences, University of Applied Sciences Bonn-Rhein-Sieg, Rheinbach 53359, Germany

The exact concentration of enzymatically active SARS-CoV-2 main protease (Mpro) was determined by means of a newly developed active-site titrant
and employed for the kinetic characterization of Mpro substrates.

Corrections

Acta Pharmaceutica Sinica B, 14 (2024) 2358

Author correction to ‘Pharmacologically targeting molecular motor promotes mitochondrial fission for anti-cancer’ [Acta
Pharm Sin B 11 (2021) 1853–1866]

Acta Pharmaceutica Sinica B, 14 (2024) 2359

Author correction to “Co-delivery of nigericin and decitabine using hexahistidine-metal nanocarriers for pyroptosis-induced
immunotherapeutics” [Acta Pharm Sin B 12 (2022) 4458–4471]