Advances in research into the preparation and biological activity of maslinic acid

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.

2019 ◽  
Vol 20 (11) ◽  
pp. 2828 ◽  
Author(s):  
Ioana Zinuca Pavel ◽  
Rene Csuk ◽  
Corina Danciu ◽  
Stefana Avram ◽  
Flavia Baderca ◽  
...  

Maslinic acid is a pentacyclic triterpene with a plethora of biological activities, including anti-inflammatory, antioxidant, antimicrobial, cardioprotective, and antitumor effects. New derivatives with improved properties and broad-spectrum activity can be obtained following structural changes of the compound. The present study was aimed to characterize a benzylamide derivative of maslinic acid—benzyl (2α, 3β) 2,3-diacetoxy-olean−12-en-28-amide (EM2)—with respect to the anti-angiogenic and anti-inflammatory effects in two in vivo experimental models. Consequently, the compound showed good tolerability and lack of irritation in the chorioallantoic membrane assay with no impairment of the normal angiogenic process during the tested stages of development. In the acute ear inflammation murine model, application of EM2 induced a mild anti-inflammatory effect that was potentiated by the association with zinc chloride (ZnCl2). A decrease in dermal thickness of mice ears was observed when EM2 and ZnCl2 were applied separately or in combination. Moreover, hyalinization of the dermis appeared only when EM2 was associated with ZnCl2, strongly suggesting the role of their combination in wound healing.


2020 ◽  
Vol 23 (24) ◽  
pp. 2679-2721 ◽  
Author(s):  
Evangelia-Eirini N. Vlachou ◽  
Konstantinos E. Litinas

Pyrano- and dipyranocoumarins are classes of naturally occurring organic compounds with very interesting biological activities. This review focuses on the synthetic strategies for the synthesis of pyranocoumarins and dipyranocoumarins and the biological properties of those compounds. The synthesis involves the formation of the pyran ring, at first, from a coumarin or the formation of pyranone moiety from an existing pyran. Pyranocoumarins and dipyranocoumarins present anti-HIV, anti-cancer, neuroprotective, antidiabetic, antibacterial, antifungal, anti-inflammatory activities. Especially khellactones and calanolides are usually potent and selective in anti-HIV activity. Decursin and decursinol derivatives are effective as anticancer, neuroprotective, antidiabetic, antibacterial, and antifungal agents.


2019 ◽  
Vol 20 (4) ◽  
pp. 444-452 ◽  
Author(s):  
Joanna Drogosz ◽  
Anna Janecka

Sesquiterpene lactones, secondary metabolites of plants, present in a large number of species mostly from the Asteracea family, are used in the traditional medicine of many countries for the treatment of various pathological conditions. They exert a broad range of activities, including antiinflammatory, anti-bacterial and anti-cancer properties. The best-known sesquiterpene lactones which are already used as drugs or are used in clinical trials are artemisinin, thapsigargin and parthenolide. Yet another sesquiterpene lactone, helenalin, an active component of Arnica montana, known for its strong anti-inflammatory activity, has been used for centuries in folk medicine to treat minor injuries. Unfortunately, helenalin’s ability to cause allergic reactions and its toxicity to healthy tissues prevented so far the development of this sesquiterpene lactone as an anticancer or anti-inflammatory drug. Recently, the new interest in the biological properties, as well as in the synthesis of helenalin analogs has been observed. This review describes helenalin's major biological activities, molecular mechanisms of action, its toxicity and potential for further research.


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.


2021 ◽  
Vol 10 (6) ◽  
pp. 299-303
Author(s):  
Mirosława Grymel ◽  
◽  
Patrycja Grabiec ◽  
Kamila Nurkowska ◽  
◽  
...  

Cannabidiol (CBD) is one of the main active ingredients in hemp. It shows a number of valuable biological properties, such as anti-cancer, anti-depressant or anti-inflammatory. The aim of the article was to present the most importantproperties of cannabidiol and its possible application in cosmetology and dermatology. The wide therapeutic potential of CBD makes it possible to use in the treatment of, not only cancer or mental disorders, but also many dermatoses.


2013 ◽  
Vol 8 (3) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
James N. Jacob ◽  
Dinesh K. Badyal ◽  
Suman Bala ◽  
Masoud Toloue

Curcumin, obtained from turmeric, has several biological properties to make it a desirable template for drug development. A lipophilic derivative of curcumin, diacetyl curcumin (DAC) and a hydrophilic derivative, diglutaryl curcumin (DGC) were synthesized and their in vivo analgesic and anti-inflammatory activities were compared with those of curcumin and aspirin. The in vitro anti-cancer activities of curcumin and the two derivatives against three cell cancer lines were compared with those against a non-cancerous cell line. The inhibitory effects were comparable to each other and nearing that of curcumin while they showed low inhibitory effect towards the non-cancerous cell line. The mouse tail flick assay showed that curcumin, DAC and DGC increased latency time. DGC was most effective as an analgesic, even more so than aspirin. The maximum percentage effect (MPE) was highest with DGC at 3 hours. The carrageenan induced paw edema model indicated anti-inflammatory activity of all three curcumin formulations. The percentage inhibition of paw edema was maximum for DAC, followed by aspirin and curcumin.


2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Wei Hsum Yap ◽  
Yang Mooi Lim

Chronic inflammation drives the development of various pathological diseases such as rheumatoid arthritis, atherosclerosis, multiple sclerosis, and cancer. The arachidonic acid pathway represents one of the major mechanisms for inflammation. Prostaglandins (PGs) are lipid products generated from arachidonic acid by the action of cyclooxygenase (COX) enzymes and their activity is blocked by nonsteroidal anti-inflammatory drugs (NSAIDS). The use of natural compounds in regulation of COX activity/prostaglandins production is receiving increasing attention. In Mediterranean diet, olive oil and table olives contain significant dietary sources of maslinic acid. Maslinic acid is arising as a safe and novel natural pentacyclic triterpene which has protective effects against chronic inflammatory diseases in variousin vivoandin vitroexperimental models. Understanding the anti-inflammatory mechanism of maslinic acid is crucial for its development as a potential dietary nutraceutical. This review focuses on the mechanistic action of maslinic acid in regulating the inflammation pathways through modulation of the arachidonic acid metabolism including the nuclear factor-kappa B (NF-κB)/COX-2 expression, upstream protein kinase signaling, and phospholipase A2enzyme activity. Further investigations may provide insight into the mechanism of maslinic acid in regulating the molecular targets and their associated pathways in response to specific inflammatory stimuli.


2021 ◽  
Vol 10 (3) ◽  
pp. 101-108
Author(s):  
Mirosława Grymel ◽  

Acmella oleracea is an interesting plant with a high spilanthol content, which due to its specific activity is considered as a valuable bioactive substance. Spilanthol displays a broad spectrum of biological activity, including analgesic, anti-inflammatory, antifungal, antioxidant, anti-cancer and bacteriostatic effects. In addition, it inhibits contractions of the facial muscles, and thanks to it was called a natural herbal botox. The interest in spilanthol by the cosmetics industry, leads that effective methods of its isolation from plant material are still being sought. The aim of the study was to present the possibility of using spilanthol in cosmetology and aesthetic dermatology. In this work, application studies presented, confirm the possibility of its use as a natural component of anti-wrinkle cosmetics.


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