scholarly journals Transforming Tea Catechins into Potent Anticancer Compound: Analysis of Three Boronated-PEG Delivery System

Micromachines ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 45
Author(s):  
Mingyan Guo ◽  
Lukas Marek ◽  
Yixia Liang ◽  
Phei Er Saw
Keyword(s):  
Phenolic Compounds ◽  
Cancer Therapy ◽  
Antioxidant Properties ◽  
Epigallocatechin Gallate ◽  
Systemic Circulation ◽  
Tea Catechins ◽  
Anticancer Properties ◽  
Naturally Occurring ◽  
Toxic Drugs ◽  
Anticancer Compound

Chemotherapy has led to many undesirable side effects, as these are toxic drugs that are unable to differentiate between cancer and normal cells. Polyphenols (tea catechins) are an ideal option as alternative chemotherapeutics owing to their inherent anticancer properties, antioxidant properties and being naturally occurring compounds, are deemed safe for consumption. However, without proper administration, the bioavailability of these compounds is low and inefficient. Therefore, proper delivery of these phenolic compounds is vital for cancer therapy. Herein, we analyzed three potential solutions to creating nanoparticle drugs using naturally occurring phenolic compounds (piceatannol (PIC), epigallocatechin gallate hydrophilic (EGCG) and l-epicatechin (EPI)). By using a simple pi-pi stacking mechanism, we utilized boronated PEG (PEG-Br) as an anchor to efficiently load EPI, PIC and EGCG, respectively, to produce three effective phenolic compound-based nanoparticles, which could be delivered safely in systemic circulation, yet detach from its cargo intracellularly to exert its anticancer effect for effective cancer therapy.

scholarly journals Alterations on phenolic compounds and antioxidant activity during sour grape juice concentrate processing

2018 ◽  
Vol 33 (2) ◽  
pp. 136-144 ◽  
Author(s):  
Ali Guler ◽  
Ozlem Tokusoglu ◽  
Nevzat Artik
Keyword(s):  
Phenolic Compounds ◽  
Antioxidant Capacity ◽  
Antioxidant Properties ◽  
Epigallocatechin Gallate ◽  
Grape Juice ◽  
Phenolic Contents ◽  
Juice Concentrate ◽  
Evaporation Stage ◽  
Sour Grape ◽  
Hplc Data

The alterations of phenolic compounds and antioxidant capacity of sour grape juice were investigated during the concentration process stages. Phenolics and antioxidant properties of the samples changed more at the vacuum evaporation stage than that of the other stages. After evaporation, the antioxidant capacity of the samples decreased approximately between 14.2 and 17.0 % for DPPH and ABTS methods, respectively. Besides, phenolic contents also decreased approximately as 14.8%. HPLC data on phenolics of sour grape juice during concentrate processing gave 12 polyphenols, including gallic acid, (+)-catechin, (-)-epigallocatechin, vanillic acid, (-)-epigallocatechin gallate, (-)-epicatechin, caftaric acid, caffeic acid and p-coumaric acid, which were determined as 1.05-1.83 mg/100 g, 5.40-7.83 mg/100 g, 6.35-9.21 mg/100 g, 3.01-5.18 mg/100 g, 0- 1.95 mg/100 g, 2.33-3.54 mg/100 g, 12.40-37.60 mg/100 g, 1.44-2.26 mg/100 g and 0.27-0.44 mg/100 g, respectively. Ferulic, sinapic acids and quercetin were only detected at concentrate step of the sour grape juice processing and were found as 0.18 mg/100 g, 0.28 mg/100 g and 0.76 mg/100 g, respectively.

scholarly journals Function of Green Tea Catechins in the Brain: Epigallocatechin Gallate and its Metabolites

2019 ◽  
Vol 20 (15) ◽  
pp. 3630 ◽  
Author(s):  
Monira Pervin ◽  
Keiko Unno ◽  
Akiko Takagaki ◽  
Mamoru Isemura ◽  
Yoriyuki Nakamura
Keyword(s):  
Green Tea ◽  
Epigallocatechin Gallate ◽  
Systemic Circulation ◽  
Brain Parenchyma ◽  
Neuroprotective Effects ◽  
Tea Catechins ◽  
Green Tea Catechins ◽  
Ring Fission ◽  
The Brain

Over the last three decades, green tea has been studied for its beneficial effects, including anti-cancer, anti-obesity, anti-diabetes, anti-inflammatory, and neuroprotective effects. At present, a number of studies that have employed animal, human and cell cultures support the potential neuroprotective effects of green tea catechins against neurological disorders. However, the concentration of (−)-epigallocatechin gallate (EGCG) in systemic circulation is very low and EGCG disappears within several hours. EGCG undergoes microbial degradation in the small intestine and later in the large intestine, resulting in the formation of various microbial ring-fission metabolites which are detectable in the plasma and urine as free and conjugated forms. Recently, in vitro experiments suggested that EGCG and its metabolites could reach the brain parenchyma through the blood–brain barrier and induce neuritogenesis. These results suggest that metabolites of EGCG may play an important role, alongside the beneficial activities of EGCG, in reducing neurodegenerative diseases. In this review, we discuss the function of EGCG and its microbial ring-fission metabolites in the brain in suppressing brain dysfunction. Other possible actions of EGCG metabolites will also be discussed.

Recent Progress of Benzimidazole Hybrids for Anticancer Potential

2020 ◽  
Vol 27 (35) ◽  
pp. 5970-6014 ◽  
Author(s):  
Md. Jawaid Akhtar ◽  
Mohammad Shahar Yar ◽  
Vinod Kumar Sharma ◽  
Ahsan Ahmed Khan ◽  
Zulphikar Ali ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Alkylating Agents ◽  
American Chemical Society ◽  
Chemical Society ◽  
Benzimidazole Derivatives ◽  
Progressive Development ◽  
Anticancer Properties ◽  
Naturally Occurring ◽  
Nitrogenous Base

This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researchers all over the world in both developed and developing countries are in a continuous effort to tackle this serious concern. Benzimidazole and its derivatives showed a broad range of biological activities due to their resemblance with naturally occurring nitrogenous base i.e. purine. The review discussed benzimidazole derivatives showing anticancer properties through a different mechanism viz. intercalation, alkylating agents, topoisomerases, DHFR enzymes, and tubulin inhibitors. Benzimidazole derivatives act through a different mechanism and the substituents reported from the earlier and recent research articles are prerequisites for the synthesis of targeted based benzimidazole derivatives as anticancer agents. The review focuses on an easy comparison of the substituent essential for potency and selectivity through SAR presented in figures. This will further provide a better outlook or fulfills the challenges faced in the development of novel benzimidazole derivatives as anticancer.

Flavonoids as Potential Therapeutic Agents for the Management of Diabetic Neuropathy

2020 ◽  
Vol 26 (42) ◽  
pp. 5468-5487 ◽  
Author(s):  
Ankita Sood ◽  
Bimlesh Kumar ◽  
Sachin Kumar Singh ◽  
Pankaj Prashar ◽  
Anamika Gautam ◽  
...  
Keyword(s):  
Neuropathic Pain ◽  
Diabetic Neuropathy ◽  
Glucose Utilization ◽  
Antioxidant Properties ◽  
Therapeutic Agents ◽  
Secondary Complications ◽  
Naturally Occurring ◽  
Glycation End Products ◽  
Treatment Of Diabetes ◽  
Pharmaceutical Industries

Flavonoids are secondary metabolites that are widely distributed in plants. These phenolic compounds are classified into various subgroups based on their structures: flavones, flavonols, isoflavones, flavanones, and anthocyanins. They are known to perform various pharmacological actions like antioxidant, anti-inflammatory, anticancer, antimicrobial, antidiabetic and antiallergic, etc. Diabetes is a chronic progressive metabolic disorder that affects several biochemical pathways and leads to secondary complications such as neuropathy, retinopathy, nephropathy, and cardiomyopathy. Among them, the management of diabetic neuropathy is one of the major challenges for physicians as well as the pharmaceutical industries. Naturally occurring flavonoids are extensively used for the treatment of diabetes and its related complications due to their antioxidant properties. Moreover, flavonoids inhibit various pathways that are involved in the progression of diabetic neuropathy like the reduction of oxidative stress, decrease in glycogenolysis, increase glucose utilization, decrease in the formation of advanced glycation end products, and inhibition of the α-glucosidase enzyme. This review entails current updates on the therapeutic perspectives of flavonoids in the treatment of neuropathic pain. This manuscript explains the pathological aspects of neuropathic pain, the chemistry of flavonoids, and their application in amelioration of neuropathic pain through preclinical studies either alone or in combination with other therapeutic agents.

Anticancer Properties of Essential Oils: An Overview

2018 ◽  
Vol 18 (10) ◽  
pp. 957-966 ◽  
Author(s):  
Milene Aparecida Andrade ◽  
Mariana Aparecida Braga ◽  
Pedro Henrique Souza Cesar ◽  
Marcus Vinicius Cardoso Trento ◽  
Mariana Araújo Espósito ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Essential Oils ◽  
Public Health Problem ◽  
Mechanisms Of Action ◽  
Low Molecular Weight ◽  
Anticancer Properties ◽  
Anti Cancer ◽  
Different Types ◽  
Antitumor Properties ◽  
Pharmaceutical Properties

Background: Essential oils are complex mixtures of low molecular weight compounds extracted from plants. Their main constituents are terpenes and phenylpropanoids, which are responsible for their biological and pharmaceutical properties, such as insecticidal, parasiticidal, antimicrobial, antioxidant, anti-inflammatory, analgesic, antinociceptive, anticarcinogenic, and antitumor properties. Cancer is a complex genetic disease considered as a serious public health problem worldwide, accounting for more than 8 million deaths annually. Objective: The activities of prevention and treatment of different types of cancer and the medicinal potential of essential oils are addressed in this review. Conclusion: Several studies have demonstrated anti-carcinogenic and antitumor activity for many essential oils obtained from various plant species. They may be used as a substitution to or in addition to conventional anti-cancer therapy. Although many studies report possible mechanisms of action for essential oils compounds, more studies are necessary in order to apply them safely and appropriately in cancer therapy.

scholarly journals The Potential Effects of Phytoestrogens: The Role in Neuroprotection

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 2954
Author(s):  
Justyna Gorzkiewicz ◽  
Grzegorz Bartosz ◽  
Izabela Sadowska-Bartosz
Keyword(s):  
Neuroprotective Effect ◽  
Antioxidant Properties ◽  
Estrogen Therapy ◽  
Neuroprotective Effects ◽  
Potential Health ◽  
Naturally Occurring ◽  
Epigenetic Effects ◽  
Estrogen Synthesis ◽  
Health Promoting ◽  
The Brain

Phytoestrogens are naturally occurring non-steroidal phenolic plant compounds. Their structure is similar to 17-β-estradiol, the main female sex hormone. This review offers a concise summary of the current literature on several potential health benefits of phytoestrogens, mainly their neuroprotective effect. Phytoestrogens lower the risk of menopausal symptoms and osteoporosis, as well as cardiovascular disease. They also reduce the risk of brain disease. The effects of phytoestrogens and their derivatives on cancer are mainly due to the inhibition of estrogen synthesis and metabolism, leading to antiangiogenic, antimetastatic, and epigenetic effects. The brain controls the secretion of estrogen (hypothalamus-pituitary-gonads axis). However, it has not been unequivocally established whether estrogen therapy has a neuroprotective effect on brain function. The neuroprotective effects of phytoestrogens seem to be related to both their antioxidant properties and interaction with the estrogen receptor. The possible effects of phytoestrogens on the thyroid cause some concern; nevertheless, generally, no serious side effects have been reported, and these compounds can be recommended as health-promoting food components or supplements.

scholarly journals Sustainable Processing of Floral Bio-Residues of Saffron (Crocus sativus L.) for Valuable Biorefinery Products

Plants ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 523
Author(s):  
Stefania Stelluti ◽  
Matteo Caser ◽  
Sonia Demasi ◽  
Valentina Scariot
Keyword(s):  
Phenolic Compounds ◽  
Vitamin C ◽  
Antioxidant Properties ◽  
Crocus Sativus ◽  
Extraction Technique ◽  
Ultrasound Assisted Extraction ◽  
Average Value ◽  
Assisted Extraction ◽  
High Yields ◽  
Crocus Sativus L

Tepals constitute the most abundant bio-residues of saffron (Crocus sativus L.). As they are a natural source of polyphenols with antioxidant properties, they could be processed to generate valuable biorefinery products for applications in the pharmaceutical, cosmetic, and food industries, becoming a new source of income while reducing bio-waste. Proper storage of by-products is important in biorefining and dehydration is widely used in the herb sector, especially for highly perishable harvested flowers. This study aimed to deepen the phytochemical composition of dried saffron tepals and to investigate whether this was influenced by the extraction technique. In particular, the conventional maceration was compared with the Ultrasound Assisted Extraction (UAE), using different solvents (water and three methanol concentrations, i.e., 20%, 50%, and 80%). Compared to the spice, the dried saffron tepals showed a lower content of total phenolics (average value 1127.94 ± 32.34 mg GAE 100 g−1 DW) and anthocyanins (up to 413.30 ± 137.16 mg G3G 100 g−1 DW), but a higher antioxidant activity, which was measured through the FRAP, ABTS, and DPPH assays. The HPLC-DAD analysis detected some phenolic compounds (i.e., ferulic acid, isoquercitrin, and quercitrin) not previously found in fresh saffron tepals. Vitamin C, already discovered in the spice, was interestingly detected also in dried tepals. Regarding the extraction technique, in most cases, UAE with safer solvents (i.e., water or low percentage of methanol) showed results of phenolic compounds and vitamin C similar to maceration, allowing an improvement in extractions by halving the time. Thus, this study demonstrated that saffron tepals can be dried maintaining their quality and that green extractions can be adopted to obtain high yields of valuable antioxidant phytochemicals, meeting the requirement for a sustainable biorefining.

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