Design, synthesis, cytotoxic, and anti-inflammatory activities of some novel analogues of aloe-emodin isolated from the rhizomes of Rheum emodi

2022 ◽  
pp. 1-7
G. Dileep Kumar ◽  
Bandi Siva ◽  
K. Ashwini ◽  
J. Vinod Kumar ◽  
V. Ramalingam ◽  
Xiang Qiu ◽  
Heying Pei ◽  
Hengfan Ni ◽  
Zhengying Su ◽  
Yong Li ◽  

2019 ◽  
Vol 16 (10) ◽  
pp. 1157-1166
Rodrigo César da Silva ◽  
Fabiano Veiga ◽  
Fabiana Cardoso Vilela ◽  
André Victor Pereira ◽  
Thayssa Tavares da Silva Cunha ◽  

Background: : A new series of O-benzyloximes derived from eugenol was synthesized and was evaluated for its antinociceptive and anti-inflammatory properties. Methods: : The target compounds were obtained in good global 25-28% yields over 6 steps, which led us to identify compounds (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-(4- (methylthio)benzyloxime (8b), (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-4- bromobenzyloxime (8d) and (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-4- (methylsulfonyl)benzyloxime (8f) as promising bioactive prototypes. Results:: These compounds have significant analgesic and anti-inflammatory effects, as evidenced by formalin-induced mice paw edema and carrageenan-induced mice paw edema tests. In the formalin test, compounds 8b and 8f evidenced both anti-inflammatory and direct analgesic activities and in the carrageenan-induced paw edema, with compounds 8c, 8d, and 8f showing the best inhibitory effects, exceeding the standard drugs indomethacin and celecoxib. Conclusion: : Molecular docking studies have provided additional evidence that the pharmacological profile of these compounds may be related to inhibition of COX enzymes, with slight preference for COX-1. These results led us to identify the new O-benzyloxime ethers 8b, 8d and 8f as orally bioactive prototypes, with a novel structural pattern capable of being explored in further studies aiming at their optimization and development as drug candidates.

2021 ◽  
Vol 12 (4) ◽  
pp. 602-608
Xin-Yuan Liang ◽  
Narsaiah Battini ◽  
Yan-Fei Sui ◽  
Mohammad Fawad Ansari ◽  
Lin-Ling Gan ◽  

Tetrazole aloe-emodin 4b displayed potent efficacy against MRSA, and it was found to rapidly permeate the bacterial membrane to intercalate into DNA and form supermolecule with MRSA DNA isomerase (PDB code: 2XCS).

2012 ◽  
Vol 60 (10) ◽  
pp. 1290-1300 ◽  
Amal Abdel Haleem Mohamed Eissa ◽  
Gamal Abd El-Hakeem Soliman ◽  
Moayad Hussein Khataibeh

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