scholarly journals Cellular Defensive Mechanisms of Tea Polyphenols: Structure-Activity Relationship

2021 ◽  
Vol 22 (17) ◽  
pp. 9109
Author(s):  
Van-Long Truong ◽  
Woo-Sik Jeong

Tea is particularly rich in polyphenols, including catechins and theaflavins, thearubigins, flavonols, and phenolic acids, which are believed to contribute to the health benefits of tea. The health-promoting effects of tea polyphenols are believed to be related to their cellular defensive properties. This review is intended to briefly summarize the relationship between the chemical structures of tea polyphenols and their biological activities. Tea polyphenols appear as direct antioxidants by scavenging reactive oxygen/nitrogen species; chelating transition metals; and inhibiting lipid, protein, and DNA oxidations. They also act directly by suppressing “pro-oxidant” enzymes, inducing endogenous antioxidants, and cooperating with vitamins. Moreover, tea polyphenols regulate cellular signaling transduction pathways, importantly contributing to the prevention of chronic diseases and the promotion of physiological functions. Apparently, the features in the chemical structures of tea polyphenols are closely associated with their antioxidant potentials.

2019 ◽  
Vol 19 (7) ◽  
pp. 555-568 ◽  
Author(s):  
Yang Li ◽  
Yan-peng Li ◽  
Jun He ◽  
Ding Liu ◽  
Qi-zhi Zhang ◽  
...  

Chrysin is a natural product of a flavonoid compound. Chemically, chrysin consists of two phenyl rings (A and B) and a heterocyclic ring (C). Biologically, chrysin exerts many different physiological activities. In recent years, with the in-depth development for more active drugs, the synthesis and biological activities of chrysin derivatives have been well studied. Besides, structure-activity relationship of chrysin revealed that the chemical construction meets the critical chemical structural necessities of flavonoids for numerous pharmacological activities. It is generally believed that modified chrysin could be more potent than unmodified chrysin. Different modification in the rings of chrysin could possess various degrees of biological activities. This review aims to summarize the mechanism for the activities of chrysin and its derivatives in different rings. We also explored the relationship between biological function and structure-activity of substituted chrysin derivatives with different functional groups. The influence of chrysin derivatives on the proliferation and apoptosis of cancer cells is also investigated. Development of novel drugs based on the biological functions of chrysin could better improve clinical outcomes of affected population, especially for tumor patients and diabetic patients.


1986 ◽  
Vol 51 (1) ◽  
pp. 241-248 ◽  
Author(s):  
Miroslav Polster ◽  
Bohuslav Rittich ◽  
Renata Žaludová

The present work deals with the relationship between biological activities of differently substituted phenols and their physico-chemical parameters expressing the influence of hydrophobic, electronic and steric factors. The testing was performed with the fungi Trychophyton gypseum and Trychophyton gypseum var. Kaufman-Wolf and the yeast Candida albicans. Significant relationship between biological activity and pKA values was calculated. The interactions between individual factors as well as the influence of the position of substituents on quantitative structure-activity relationships are discussed.


2021 ◽  
Vol 22 (2) ◽  
pp. 959
Author(s):  
Ruihong Zheng ◽  
Shoujie Li ◽  
Xuan Zhang ◽  
Changqi Zhao

Secondary metabolites isolated from plant endophytic fungi have been getting more and more attention. Some secondary metabolites exhibit high biological activities, hence, they have potential to be used for promising lead compounds in drug discovery. In this review, a total of 134 journal articles (from 2017 to 2019) were reviewed and the chemical structures of 449 new metabolites, including polyketides, terpenoids, steroids and so on, were summarized. Besides, various biological activities and structure-activity relationship of some compounds were aslo described.


Marine Drugs ◽  
2020 ◽  
Vol 18 (7) ◽  
pp. 368
Author(s):  
Hanan I. Althagbi ◽  
Walied M. Alarif ◽  
Khalid O. Al-Footy ◽  
Ahmed Abdel-Lateff

The curiosity and attention that researchers have devoted to alkaloids are due to their bioactivities, structural diversity, and intriguing chemistry. Marine-derived macrocyclic alkaloids (MDMAs) are considered to be a potential source of drugs. Trabectedin, a tetrahydroisoquinoline derivative, has been approved for the treatment of metastatic soft tissue sarcoma and ovarian cancers. MDMAs displayed potent activities that enabled them to be used as anticancer, anti-invasion, antimalarial, antiplasmodial, and antimicrobial. This review presents the reported chemical structures, biological activities, and structure–activity relationships of macrocyclic alkaloids from marine organisms that have been published since their discovery until May 2020. This includes 204 compounds that are categorized under eight subclasses: pyrroles, quinolines, bis-quinolizidines, bis-1-oxaquinolizidines, 3-alkylpiperidines, manzamines, 3-alkyl pyridinium salts, and motuporamines.


Marine Drugs ◽  
2020 ◽  
Vol 18 (11) ◽  
pp. 569
Author(s):  
Zhaoming Liu ◽  
Hongxin Liu ◽  
Weimin Zhang

Natural polypropionates (PPs) are a large subgroup of polyketides with diverse structural features and bioactivities. Most of the PPs are discovered from marine organisms including mollusks, fungi and actinomycetes, while some of them are also isolated from terrestrial resources. An increasing number of studies about PPs have been carried out in the past two decades and an updated review is needed. In this current review, we summarize the chemical structures and biological activities of 164 natural PPs reported in 67 research papers from 1999 to 2020. The isolation, structural features and bioactivities of these PPs are discussed in detail. The chemical diversity, bioactive diversity, biodiversity and the relationship between chemical classes and the bioactivities are also concluded.


1979 ◽  
Vol 07 (02) ◽  
pp. 103-141 ◽  
Author(s):  
Shoji Shibata

Some herbal drugs commonly used in Chinese medicine have been studied chemically in correlation with their biological activities. In many cases it has been recognized that some characteristic chemical constituents could represent the therapeutical actions of the drugs. It is noted that elucidation of their chemical structures in view of the structure-activity relationship provides scientific evidence for the beneficial uses of traditional drugs in health care and, furthermore, promotes the discovering of new therapeutics from them. The principles of Chinese drugs are distributed widely among almost all the chemical groups of natural products, for example, simple phenolics, lignan, flavonoid, quinonoid, lower terpenes, triterpenoid, steroid, true alkaloid, protoalkaloid or amines and simple and polymolecular carbonhydrates. In the present article, the chemical principles of some important Chinese drugs currently used are discussed mainly on the basis of our own investigations, and we refer to other works for a general understanding of the present status on the chemical approach to studies of Chinese drugs and medicines.


2017 ◽  
Author(s):  
Mohit S. Verma ◽  
Michael J. Fink ◽  
Gabriel L Salmon ◽  
Nadine Fornelos ◽  
Takahiro E. Ohara ◽  
...  

Two biological activities of butyrate in the colon (suppression of proliferation of colonic epithelial stem cells and inflammation) correlate with inhibition of histone deacetylases. Cellular and biochemical studies of molecules similar in structure to butyrate, but different in molecular details (functional groups, chain-length, deuteration, oxidation level, fluorination, or degree of unsaturation) demonstrated that these activities were sensitive to molecular structure, and were compatible with the hypothesis that butyrate acts by binding to the Zn<sup>2+</sup> in the catalytic site of histone deacetylases. Structure-activity relationships drawn from a set of 36 compounds offer a starting point for the design of new compounds targeting the inhibition of histone deacetylases. The observation that butyrate was more potent than other short-chain fatty acids is compatible with the hypothesis that crypts evolved (at least in part), to separate stem cells at the base of crypts from butyrate produced by commensal bacteria.


2014 ◽  
Vol 14 (12) ◽  
pp. 963-977 ◽  
Author(s):  
Andrea Milelli ◽  
Carmela Fimognari ◽  
Nicole Ticchi ◽  
Paolo Neviani ◽  
Anna Minarini ◽  
...  

2020 ◽  
Vol 20 (10) ◽  
pp. 908-920 ◽  
Author(s):  
Su-Min Wu ◽  
Xiao-Yang Qiu ◽  
Shu-Juan Liu ◽  
Juan Sun

Inhibitors of monoamine oxidase (MAO) have shown therapeutic values in a variety of neurodegenerative diseases such as depression, Parkinson’s disease and Alzheimer’s disease. Heterocyclic compounds exhibit a broad spectrum of biological activities and vital leading compounds for the development of chemical drugs. Herein, we focus on the synthesis and screening of novel single heterocyclic derivatives with MAO inhibitory activities during the past decade. This review covers recent pharmacological advancements of single heterocyclic moiety along with structure- activity relationship to provide better correlation among different structures and their receptor interactions.


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