scholarly journals Inhibition of Human Cathepsins B and L by Caffeic Acid and Its Derivatives

Biomolecules ◽  
2020 ◽  
Vol 11 (1) ◽  
pp. 31
Author(s):  
Liza Ulčakar ◽  
Marko Novinec
Keyword(s):  
Caffeic Acid ◽  
Cathepsin B ◽  
Biological Activities ◽  
Caffeic Acid Phenethyl Ester ◽  
Promising Candidate ◽  
Pathological Conditions ◽  
Wide Range ◽  
Endopeptidase Activity ◽  
Catalytic Mechanisms ◽  
Dipeptidase Activity

Caffeic acid (CA) and its derivatives caffeic acid phenethyl ester (CAPE) and chlorogenic acid (CGA) are phenolic compounds of plant origin with a wide range of biological activities. Here, we identify and characterize their inhibitory properties against human cathepsins B and L, potent, ubiquitously expressed cysteine peptidases involved in protein turnover and homeostasis, as well as pathological conditions, such as cancer. We show that CAPE and CGA inhibit both peptidases, while CA shows a preference for cathepsin B, resulting in the strongest inhibition among these combinations. All compounds are linear (complete) inhibitors acting via mixed or catalytic mechanisms. Cathepsin B is more strongly inhibited at pH 7.4 than at 5.5, and CA inhibits its endopeptidase activity preferentially over its peptidyl-dipeptidase activity. Altogether, the results identify the CA scaffold as a promising candidate for the development of cathepsin B inhibitors, specifically targeting its endopeptidase activity associated with pathological proteolysis of extracellular substrates.

scholarly journals Caffeic Acid Phenethyl Ester Reduces Ischemia-Induced Kidney Mitochondrial Injury in Rats

2017 ◽  
Vol 2017 ◽  
pp. 1-11 ◽  
Author(s):  
Sonata Trumbeckaite ◽  
Neringa Pauziene ◽  
Darius Trumbeckas ◽  
Mindaugas Jievaltas ◽  
Rasa Baniene
Keyword(s):  
Caffeic Acid ◽  
Biological Activities ◽  
Rat Kidney ◽  
Caffeic Acid Phenethyl Ester ◽  
Biologically Active ◽  
Protective Effects ◽  
Mitochondrial Injury ◽  
Wide Range ◽  
Biochemical Mechanisms

During partial nephrectomy, the avoidance of ischemic renal damage is extremely important as duration of renal artery clamping (i.e., ischemia) influences postoperative kidney function. Mitochondria (main producer of ATP in the cell) are very sensitive to ischemia and undergo damage during oxidative stress. Finding of a compound which diminishes ischemic injury to kidney is of great importance. Caffeic acid phenethyl ester (CAPE), biologically active compound of propolis, might be one of the promising therapeutic agents against ischemia-caused damage. Despite wide range of biological activities of CAPE, detailed biochemical mechanisms of its action at the level of mitochondria during ischemia are poorly described and need to be investigated. We investigated if CAPE (22 mg/kg and 34 mg/kg, injected intraperitoneally) has protective effects against short (20 min) and longer time (40 min) rat kidney ischemia in an in vitro ischemia model. CAPE ameliorates in part ischemia-induced renal mitochondrial injury, improves oxidative phosphorylation with complex I-dependent substrate glutamate/malate, increases Ca2+ uptake by mitochondria, blocks ischemia-induced caspase-3 activation, and protects kidney cells from ischemia-induced necrosis. The protective effects on mitochondrial respiration rates were seen after shorter (20 min) time of ischemia whereas reduction of apotosis and necrosis and increase in Ca2+ uptake were revealed after both, shorter and longer time of ischemia.

scholarly journals Perbedaan kadar caffeic acid phenethyl ester pada propolis ekstrak etanol dan propolis ekstrak air

2013 ◽  
Vol 11 (2) ◽  
pp. 43-47
Author(s):  
RIANI DWI HASTUTI ◽  
DIDING PRASETYO ◽  
SRI HARTATI HADINOTO
Keyword(s):  
Caffeic Acid ◽  
Water Extract ◽  
Ethanol Extract ◽  
Caffeic Acid Phenethyl Ester ◽  
Rat Aorta ◽  
Raw Material ◽  
Wide Range ◽  
Significant Difference ◽  
Post Test ◽  
The Difference

Hastuti RD, Prasetyo D, Hadinoto SH. 2013. The difference of caffeic acid phenethyl ester level in ethanol extract propolis and water extract propolis. Biofarmasi 11: 43-47. Propolis is a natural product derived from plant resin collected by honeybeen and its composition has wide range of biological activity. CAPE is the ester of caffeic acid, a derivative of phenolic acid, a flavonoid-like compound, one of the major components of propolis. CAPE is reported can protect nephrotoxicity due to cisplatin induction, inhibiting the growth of various types of abnormal cells, having an anti-inflammation activity, antioxidant activity, cyclooxygenase activity, vasodilatation activity in rat aorta, potential inhibitor of nitric oxidant, inhibitor oxidative process, and effectively suppress the growth of cataract in rat. Propolis can not be used as raw material, and it must be purified by extraction with solvent. Different solvents may extract different compounds, influencing its activity. The purpose of this research was to determine the difference levels of CAPE in ethanol extract propolis and water extract propolis. This research was a pure experimental research using the post-test only design. The sample of this research was raw propolis taken from bees farming in Gejen RT. 03 RW. 02, Kerjo, Karanganyar. Sampling was performed by a purposive sampling. Sample was extracted with a maserasion method with the solvents of ethanol and water. In each extract propolis was made five samples. The determination of the level of CAPE on propolis was performed by using UV-Vis spectrophotometry with Prussian Blue method. The data of the level of CAPE was analyzed by the statistical test of independent t-test. The results showed that the average of CAPE level in ethanol extract propolis was 12.268±0.658 μg/mL and the average of CAPE level in water extract propolis was 5.564±0.332 μg/mL, with p=0.125 (p>0.05). There was no significant difference between extract ethanol propolis and water extract propolis.

scholarly journals Pharmacological Effects of Sacred Oils Belonging to Ancient Civilizations

2021 ◽  
pp. 55-68
Author(s):  
Baraa Al-mansour
Keyword(s):  
Medicinal Plants ◽  
Essential Oils ◽  
Biological Activities ◽  
Well Being ◽  
Religious Ritual ◽  
Pathological Conditions ◽  
Wide Range ◽  
Spiritual Well Being ◽  
Ancient Civilizations ◽  
Aromatic Oils

Over the centuries, humanity has known and utilized some sacred oils extracted from their medicinal plants for therapeutic purpose. They are considered as good source of bioactive compounds having a wide range of vital biological activities. Aromatic oils have been a part of human history for more than 3,500 years BC and appeared with regularity throughout all major civilizations down the ages, with uses ranging from religious ritual, food flavoring, medicines, perfumery and the masking of bad odors. It is impossible to date exactly when plants were first used medicinally, since such a development would have taken place over thousands of years. During recent decades, many researchers have investigated the mechanisms of action and the therapeutic use of essential oils as physical, emotional, and spiritual well-being. This review, highlights on some sacred essential oils extracted from important traditional medicinal plants that possesses several pharmacological properties, considering that the safety and versatility of this these supplement should allow for its use in numerous pathological conditions.

scholarly journals Anticancer Activity in Honeybee Propolis: Functional Insights to the Role of Caffeic Acid Phenethyl Ester and Its Complex With γ-Cyclodextrin

2018 ◽  
Vol 17 (3) ◽  
pp. 867-873 ◽  
Author(s):  
Yoshiyuki Ishida ◽  
Ran Gao ◽  
Navjot Shah ◽  
Priyanshu Bhargava ◽  
Takahiro Furune ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Caffeic Acid ◽  
Caffeic Acid Phenethyl Ester ◽  
Careful Examination ◽  
Dna Damage Signaling ◽  
Therapeutic Benefits ◽  
Wide Range

Besides honey, honeybees make a sticky substance (called propolis/bee glue) by mixing saliva with poplar tree resin and other botanical sources. It is known to be rich in bioactivities of which the anticancer activity is most studied. Caffeic acid phenethyl ester (CAPE) is a key anticancer component in New Zealand propolis. We have earlier investigated the molecular mechanism of anticancer activity in CAPE and reported that it activates DNA damage signaling in cancer cells. CAPE-induced growth arrest of cells was mediated by downregulation of mortalin and activation of p53 tumor suppressor protein. When antitumor and antimetastasis activities of CAPE were examined in vitro and in vivo, we failed to find significant activities, which was contrary to our expectations. On careful examination, it was revealed that CAPE is unstable and rather gets easily degraded into caffeic acid by secreted esterases. Interestingly, when CAPE was complexed with γ-cyclodextrin (γCD) the activities were significantly enhanced. In the present study, we report that the CAPE-γCD complex with higher cytotoxicity to a wide range of cancer cells is stable in acidic milieu and therefore recommended as an anticancer amalgam. We also report a method for preparation of stable and less-pungent powder of propolis that could be conveniently used for health and therapeutic benefits.

Therapeutic Potential of Caffeic Acid Phenethyl Ester (CAPE) in Diabetes

2019 ◽  
Vol 25 (37) ◽  
pp. 4827-4836 ◽  
Author(s):  
Valeria Pittalà ◽  
Loredana Salerno ◽  
Giuseppe Romeo ◽  
Rosaria Acquaviva ◽  
Claudia Di Giacomo ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Caffeic Acid ◽  
Antioxidant Defense ◽  
Molecular Mechanisms ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Caffeic Acid Phenethyl Ester ◽  
Sugar Levels ◽  
Main Components

Diabetes mellitus is a complex metabolic disease characterized by high blood sugar levels. Different pathogenic processes are involved in the etiology of the disease. Indeed, chronic diabetes hyperglycemia is often associated with severe long-term complications including cardiovascular symptoms, retinopathy, nephropathy, and neuropathy. Although the precise molecular mechanisms underlying diabetes are not yet clear, it is widely accepted that increased levels of oxidative stress are involved in the onset, development and progression of diabetes and its related complications. In this regard, the use of natural antioxidant polyphenols, able to control free radical production, to increase intracellular antioxidant defense and to prevent the onset of oxidative stress, can be of high interest. Caffeic acid phenethyl ester (CAPE), a natural polyphenolic substance, is one of the main components of propolis. Due to its multifaceted biological activities, including antioxidant, antimicrobial, anti-inflammatory, antitumor, and immunomodulatory effects, CAPE has received great attention during the last few decades. In the present paper the therapeutic potential of CAPE in diabetes is extensively reviewed.

scholarly journals Caffeic Acid Phenethyl Ester (CAPE) Induces VEGF Expression and Production in Rat Odontoblastic Cells

2019 ◽  
Vol 2019 ◽  
pp. 1-12 ◽  
Author(s):  
Hitomi Kuramoto ◽  
Kouji Hirao ◽  
Hiromichi Yumoto ◽  
Yuki Hosokawa ◽  
Tadashi Nakanishi ◽  
...  
Keyword(s):  
Dental Caries ◽  
Caffeic Acid ◽  
Dental Pulp ◽  
Biological Activities ◽  
Specific Inhibitor ◽  
Caffeic Acid Phenethyl Ester ◽  
Vegf Receptor ◽  
Normal Medium ◽  
Reparative Dentin ◽  
Pulp Inflammation

Caffeic acid phenethyl ester (CAPE), the main component of propolis, has various biological activities including anti-inflammatory effect and wound healing promotion. Odontoblasts located in the outermost layer of dental pulp play crucial roles such as production of growth factors and formation of hard tissue termed reparative dentin in host defense against dental caries. In this study, we investigated the effects of CAPE on the upregulation of vascular endothelial growth factor (VEGF) and calcification activities of odontoblasts, leading to development of novel therapy for dental pulp inflammation caused by dental caries. CAPE significantly induced mRNA expression and production of VEGF in rat clonal odontoblast-like KN-3 cells cultured in normal medium or osteogenic induction medium. CAPE treatment enhanced nuclear factor-kappa B (NF-κB) transcription factor activation, and furthermore, the specific inhibitor of NF-κB significantly reduced VEGF production. The expression of VEGF receptor- (VEGFR-) 2, not VEGFR-1, was up regulated in KN-3 cells treated with CAPE. In addition, VEGF significantly increased mineralization activity in KN-3 cells. These findings suggest that CAPE might be useful as a novel biological material for the dental pulp conservative therapy.

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

Synthesis, Characterization and Antiproliferative Activity Assessment of a Novel 1H-5-mercapto-1,2,4 Triazole Derivative

2017 ◽  
Vol 68 (4) ◽  
pp. 745-747 ◽  
Author(s):  
Marius Mioc ◽  
Sorin Avram ◽  
Vasile Bercean ◽  
Mihaela Balan Porcarasu ◽  
Codruta Soica ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Vascular Endothelial ◽  
Triazole Derivative ◽  
Activity Assessment ◽  
Wide Range ◽  
Specific Receptors ◽  
Endothelial Growth Factor ◽  
Selection Of

Angiogenesis plays an important function in tumor proliferation, one of the main angiogenic promoters being the vascular endothelial growth factor (VEGF) which activates specific receptors, particularly VEGFR-2. Thus, VEGFR-2 has become an essential therapeutic target in the development of new antitumor drugs. 1,2,4-triazoles show a wide range of biological activities, including antitumor effect, which was documented by numerous reports. In the current study the selection of 5-mercapto-1,2,4-triazole structure (1H-3-styryl-5-benzylidenehydrazino-carbonyl-methylsulfanil-1,2,4-triazole, Tz3a.7) was conducted based on molecular docking that emphasized it as suitable ligand for VEGFR-2 and EGFR1 receptors. Compound Tz3a.7 was synthesized and physicochemically and biologically evaluated thus revealing a moderate antiproliferative activity against breast cancer cell line MDA-MB-231.

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