PMID- 37126969
OWN - NLM
STAT- MEDLINE
DCOM- 20230522
LR  - 20230522
IS  - 1618-095X (Electronic)
IS  - 0944-7113 (Linking)
VI  - 115
DP  - 2023 Jul
TI  - Discovery of anti-allergic components in Guomingkang Formula using sensitive HEMT 
      biochips coupled with in vitro and in vivo validation.
PG  - 154837
LID - S0944-7113(23)00198-8 [pii]
LID - 10.1016/j.phymed.2023.154837 [doi]
AB  - BACKGROUND: Allergic rhinitis (AR) is a prevalent allergic disease, which 
      seriously affects the sufferers' life quality and increases the socioeconomic 
      burden. Guominkang (GMK), a well-known prescription for AR treatment, showed 
      satisfactory effects; while its anti-allergic components remain to be disclosed. 
      AlGaN/GaN HEMT biochip is more sensitive and cost-effective than other binding 
      equipments, indicating its great potential for screening of active ingredients 
      from herbal medicines. METHODS: AR mouse models were first established to test 
      the anti-allergic effect of GMK and discover the ingredients absorbed into blood 
      by ultra-high performance liquid chromatography-mass spectra (UHPLC-MS). Then, 
      novel Syk/Lyn/Fyn-functionalized high electron mobility transistor (HEMT) 
      biochips with high sensitivity and specificity were constructed and applied to 
      screen the active components. Finally, the results from HEMT biochips screening 
      were validated via in silico (molecular docking and molecular dynamics 
      simulation), in vitro (RBL-2H3 cells), and in vivo (PCA mice model) assays. 
      RESULTS: GMK showed a potent therapeutic effect on AR mice, and fifteen 
      components were identified from the medicated plasma. Furthermore, hamaudol was 
      firstly found to selectively inhibit the Syk and Lyn, and emodin was to 
      selectively inhibit Lyn, which were further confirmed by isothermal titration 
      calorimetry, molecular docking, and molecular dynamics simulation analyses. 
      Suppression of the activation of FcepsilonRI-MAPK signals might be the possible 
      mechanism of the anti-allergic effect of hamaudol. CONCLUSIONS: The targets of 
      emodin and hamaudol were discovered by HEMT biochips for the first time. This 
      study provided a novel and effective strategy to discover active components in a 
      complex herbal formula by using AlGaN/GaN HEMT biochips.
CI  - Copyright (c) 2023. Published by Elsevier GmbH.
FAU - Tang, Ding
AU  - Tang D
AD  - Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New 
      Drugs Research and International Cooperative Laboratory of Traditional Chinese 
      Medicine Modernization and Innovative Drug Development of Chinese Ministry of 
      Education, College of Pharmacy, Jinan University, Guangzhou 511436, PR China; Key 
      Laboratory of Ministry of Education on Traditional Chinese Medicine Resource and 
      Compound Prescription, Hubei Province Key Laboratory of Traditional Chinese 
      Medicine Resource and Chemistry, College of Pharmacy, Hubei University of Chinese 
      Medicine, Wuhan, Hubei 430065, China.
FAU - Wang, Chen
AU  - Wang C
AD  - Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New 
      Drugs Research and International Cooperative Laboratory of Traditional Chinese 
      Medicine Modernization and Innovative Drug Development of Chinese Ministry of 
      Education, College of Pharmacy, Jinan University, Guangzhou 511436, PR China.
FAU - Gu, Zhiqi
AU  - Gu Z
AD  - Key Laboratory of Multifunctional Nanomaterials and Smart Systems, Suzhou 
      Institute of Nano-Tech and Nano-Bionics, Chinese Academy of Sciences, Suzhou 
      215125, PR China.
FAU - Li, Jiadong
AU  - Li J
AD  - Key Laboratory of Multifunctional Nanomaterials and Smart Systems, Suzhou 
      Institute of Nano-Tech and Nano-Bionics, Chinese Academy of Sciences, Suzhou 
      215125, PR China.
FAU - Jin, Lu
AU  - Jin L
AD  - Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New 
      Drugs Research and International Cooperative Laboratory of Traditional Chinese 
      Medicine Modernization and Innovative Drug Development of Chinese Ministry of 
      Education, College of Pharmacy, Jinan University, Guangzhou 511436, PR China.
FAU - Li, Juan
AU  - Li J
AD  - Key Laboratory of Ministry of Education on Traditional Chinese Medicine Resource 
      and Compound Prescription, Hubei Province Key Laboratory of Traditional Chinese 
      Medicine Resource and Chemistry, College of Pharmacy, Hubei University of Chinese 
      Medicine, Wuhan, Hubei 430065, China.
FAU - Wang, Zhixin
AU  - Wang Z
AD  - Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New 
      Drugs Research and International Cooperative Laboratory of Traditional Chinese 
      Medicine Modernization and Innovative Drug Development of Chinese Ministry of 
      Education, College of Pharmacy, Jinan University, Guangzhou 511436, PR China. 
      Electronic address: zhixin.wang@ufl.edu.
FAU - Jiang, Ren-Wang
AU  - Jiang RW
AD  - Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New 
      Drugs Research and International Cooperative Laboratory of Traditional Chinese 
      Medicine Modernization and Innovative Drug Development of Chinese Ministry of 
      Education, College of Pharmacy, Jinan University, Guangzhou 511436, PR China. 
      Electronic address: trwjiang@jnu.edu.cn.
LA  - eng
PT  - Journal Article
DEP - 20230418
PL  - Germany
TA  - Phytomedicine
JT  - Phytomedicine : international journal of phytotherapy and phytopharmacology
JID - 9438794
RN  - 0 (aluminum gallium nitride)
RN  - 0 (Anti-Allergic Agents)
RN  - KA46RNI6HN (Emodin)
SB  - IM
MH  - Mice
MH  - Animals
MH  - *Anti-Allergic Agents/pharmacology
MH  - Molecular Docking Simulation
MH  - *Emodin/pharmacology
MH  - *Rhinitis, Allergic/drug therapy
MH  - Disease Models, Animal
OTO - NOTNLM
OT  - Allergic rhinitis (AR)
OT  - Biochip
OT  - Guomingkang (GMK)
OT  - Hamaudol
OT  - High electron mobility transistor (HEMT)
OT  - Src family kinases (SFKs)
COIS- Declaration of Competing Interest The authors declare that they have no known 
      competing financial interests or personal relationships that could have appeared 
      to influence the work reported in this paper.
EDAT- 2023/05/02 00:42
MHDA- 2023/05/22 06:42
CRDT- 2023/05/01 18:05
PHST- 2023/01/29 00:00 [received]
PHST- 2023/04/04 00:00 [revised]
PHST- 2023/04/18 00:00 [accepted]
PHST- 2023/05/22 06:42 [medline]
PHST- 2023/05/02 00:42 [pubmed]
PHST- 2023/05/01 18:05 [entrez]
AID - S0944-7113(23)00198-8 [pii]
AID - 10.1016/j.phymed.2023.154837 [doi]
PST - ppublish
SO  - Phytomedicine. 2023 Jul;115:154837. doi: 10.1016/j.phymed.2023.154837. Epub 2023 
      Apr 18.