Pentacyclic triterpene acid conjugated with mitochondria-targeting cation F16: Synthesis and evaluation of cytotoxic activities

Author(s):  
Anna Yu. Spivak ◽  
Darya A. Nedopekina ◽  
Rinat R. Gubaidullin ◽  
Eldar V. Davletshin ◽  
Adis A. Tukhbatullin ◽  
...  
1991 ◽  
Vol 54 (3) ◽  
pp. 755-758 ◽  
Author(s):  
S. K. Singh ◽  
V. J. Tripathi ◽  
R. H. Singh

2022 ◽  
Vol 23 (1) ◽  
pp. 544
Author(s):  
Shinhui Lee ◽  
Hee-Soo Seol ◽  
Sanung Eom ◽  
Jaeeun Lee ◽  
Chaelin Kim ◽  
...  

Monoamine serotonin is a major neurotransmitter that acts on a wide range of central nervous system and peripheral nervous system functions and is known to have a role in various processes. Recently, it has been found that 5-HT is involved in cognitive and memory functions through interaction with cholinergic pathways. The natural flavonoid kaempferol (KAE) extracted from Cudrania tricuspidata is a secondary metabolite of the plant. Recently studies have confirmed that KAE possesses a neuroprotective effect because of its strong antioxidant activity. It has been confirmed that KAE is involved in the serotonergic pathway through an in vivo test. However, these results need to be confirmed at the molecular level, because the exact mechanism that is involved in such effects of KAE has not yet been elucidated. Therefore, the objective of this study is to confirm the interaction of KAE with 5-HT3A through electrophysiological studies at the molecular level using KAE extracted from Cudrania tricuspidata. This study confirmed the interaction between 5-HT3A and KAE at the molecular level. KAE inhibited 5-HT3A receptors in a concentration-dependent and voltage-independent manner. Site-directed mutagenesis and molecular-docking studies confirmed that the binding sites D177 and F199 are the major binding sites of human 5-HT3A receptors of KAE.


2012 ◽  
Vol 48 (4) ◽  
pp. 597-600 ◽  
Author(s):  
Qiong-ming Xu ◽  
Yan-li Liu ◽  
Yu-lin Feng ◽  
Li-hua Tang ◽  
Shi-lin Yang

1990 ◽  
Vol 29 (10) ◽  
pp. 3360-3362 ◽  
Author(s):  
S.K. Singh ◽  
V.J. Tripathi ◽  
R.H. Singh

2021 ◽  
Author(s):  
Huijuan Gao ◽  
Hong Wu

Abstract BackgroundDiabetic nephropathy has been a devastating complication. Clinically, there is an urgent need for nephroprotective agents to delay the onset of diabetic nephropathy and ameliorate its symptoms. Maslinic acid is a pentacyclic triterpene acid with protective effect on multiple organs from oxidative stress and inflammation. However, the therapeutic effect of maslinic acid on diabetic nephropathy remains unclear.MethodsC57BL/6J male mice administrated with 50 mg/kg of Streptozocin (STZ) daily were used to establish diabetic mouse model (blood glucose levels > 300 mg/dL). Urinary levels of albumin, total proteins, and creatinine were analyzed by an automatic analyzer. H&E staining was used to evaluate renal damage. qRT-PCR and ELISA assay were performed to investigate the inflammation and oxidative stress of renal tissues. Western-blotting assay was used to demonstrate the activation of AMPK signaling.ResultsMaslinic acid treatment alleviated the loss of body weight and blood glucose in diabetic mice. The renal structure and function were protected by maslinic acid in diabetic mice. 20 mg/kg maslinic acid treatment for 8 weeks alleviated the oxidative stress and inflammation in the kidney of diabetic rats dramatically. Maslinic acid treatment activated renal AMPK/SIRT1 signaling.ConclusionMaslinic acid ameliorated diabetic nephropathy via activating AMPK/SIRT1 signaling pathway.


2019 ◽  
Vol 7 (3) ◽  
pp. 104-107
Author(s):  
Cheolin Park ◽  
Jae Sik LEE's

  Corosolic acid is a pentacyclic triterpene acid found in banaba leaves, Lagerstroemia speciosa which is similar in structure to useful pharmaceutical material such as ursolic acid and has been reported to have beneficial activities, as found in in vitro and several animal studies including human studies, particularly due to its effects on lowering of blood sugar. This review paper is focused on various pharmaceutical effects including decreasing of blood sugar of corosolic acid from published articels and can be helpful on the understanding of those effects which can be appliable on maintenace and treatment against several diseas        


1995 ◽  
Vol 58 (7) ◽  
pp. 1056-1058 ◽  
Author(s):  
T. N. Misra ◽  
R. S. Singh ◽  
H. S. Pandey ◽  
C. Prasad ◽  
S. C. Sharma

Author(s):  
Jianqiang Deng ◽  
Huiyun Wang ◽  
Xiaodong Mu ◽  
Xiuting He ◽  
Fenglan Zhao ◽  
...  

: Maslinic acid, a pentacyclic triterpene acid, is mainly isolated from olives. Maslinic acid and its derivatives exhibit a broad range of biological properties, such as anti-inflammatory, anti-cancer, anti-diabetic, antimicrobial, neuroprotective and hepatoprotective activities. In this mini-review, the progress of research into maslinic acid with regard to its bioactivities, extraction, semi-synthetic preparation and patents is reported. The relationships between the structure and the activity of maslinic acid and its derivatives are also discussed.


Phytomedicine ◽  
2019 ◽  
Vol 63 ◽  
pp. 153037 ◽  
Author(s):  
Xi-Lin Ouyang ◽  
Feng Qin ◽  
Ri-Zhen Huang ◽  
Dong Liang ◽  
Chun-Gu Wang ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1081 ◽  
Author(s):  
André Barreto Cunha ◽  
Ronan Batista ◽  
María Ángeles Castro ◽  
Jorge Mauricio David

Betulinic acid (BA, 3β-hydroxy-lup-20(29)-en-28-oic acid) is a pentacyclic triterpene acid present predominantly in Betula ssp. (Betulaceae) and is also widely spread in many species belonging to different plant families. BA presents a wide spectrum of remarkable pharmacological properties, such as cytotoxic, anti-HIV, anti-inflammatory, antidiabetic and antimicrobial activities, including antiprotozoal effects. The present review first describes the sources of BA and discusses the chemical strategies to produce this molecule starting from betulin, its natural precursor. Next, the antiprotozoal properties of BA are briefly discussed and the chemical strategies for the synthesis of analogues displaying antiplasmodial, antileishmanial and antitrypanosomal activities are systematically presented. The antiplasmodial activity described for BA was moderate, nevertheless, some C-3 position acylated analogues showed an improvement of this activity and the hybrid models—with artesunic acid—showed the most interesting properties. Some analogues also presented more intense antileishmanial activities compared with BA, and, in addition to these, heterocycles fused to C-2/C-3 positions and amide derivatives were the most promising analogues. Regarding the antitrypanosomal activity, some interesting antitrypanosomal derivatives were prepared by amide formation at the C-28 carboxylic group of the lupane skeleton. Considering that BA can be produced either by isolation of different plant extracts or by chemical transformation of betulin, easily obtained from Betula ssp., it could be said that BA is a molecule of great interest as a starting material for the synthesis of novel antiprotozoal agents.


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