Metabolism of Rhaponticin and Activities of its Metabolite, Rhapontigenin: A Review

Rhaponticin is a stilbenoid glucoside compound, found in medicinal plant of rhubarb rhizomes. Rhapontigenin (RHAG), the stilbene aglycone metabolite of rhaponticin, has shown various biological activities including anticancer activities to act a potential human cytochrome P450 inhibitor, antihyperlipidemic effect, anti-allergic action, antioxidant and antibacterial activities. Moreover, it was reported to scavenge intracellular Reactive Oxygen Species (ROS), the 1,1-Diphenyl-2-Picrylliydrazyl (DPPH) radical, and Hydrogen Peroxide (H2O2). Meanwhile, RHAG exhibited the inhibitory activity for the synthesis of DNA, RNA and protein, and also presented the capacity of inducing morphological changes and apoptosis of C. albicans. Here, the structure, pharmacokinetics, pharmacological effects as well as underlying mechanisms of rhaponticin and its metabolite, RHAG, have been extensively reviewed. This review will provide a certain reference value for developing the therapeutic drug of rhaponticin or RHAG.

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Biological Properties of 6-Gingerol: A Brief Review

Natural Product Communications ◽

10.1177/1934578x1400900736 ◽

2014 ◽

Vol 9 (7) ◽

pp. 1934578X1400900 ◽

Cited By ~ 10

Author(s):

Shaopeng Wang ◽

Caihua Zhang ◽

Guang Yang ◽

Yanzong Yang

Keyword(s):

Fruits And Vegetables ◽

Biological Activities ◽

Zingiber Officinale ◽

Biological Properties ◽

Anticancer Activities ◽

Inhibition Of Angiogenesis ◽

Underlying Mechanisms ◽

Pharmacologically Active

Numerous studies have revealed that regular consumption of certain fruits and vegetables can reduce the risk of many diseases. The rhizome of Zingiber officinale (ginger) is consumed worldwide as a spice and herbal medicine. It contains pungent phenolic substances collectively known as gingerols. 6-Gingerol is the major pharmacologically-active component of ginger. It is known to exhibit a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation. 6-Gingerol has been found to possess anticancer activities via its effect on a variety of biological pathways involved in apoptosis, cell cycle regulation, cytotoxic activity, and inhibition of angiogenesis. Thus, due to its efficacy and regulation of multiple targets, as well as its safety for human use, 6-gingerol has received considerable interest as a potential therapeutic agent for the prevention and/or treatment of various diseases. Taken together, this review summarizes the various in vitro and in vivo pharmacological aspects of 6-gingerol and the underlying mechanisms.

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Targeting apoptosis via inactivation of PI3K/Akt/mTOR signaling pathway involving NF-κB by geraniin in HT-29 human colorectal adenocarcinoma cells

Progress in Drug Discovery & Biomedical Science ◽

10.36877/pddbs.a0000030 ◽

2019 ◽

Vol 2 (1) ◽

Author(s):

Chim Kei Chan ◽

Liu Ying Tang ◽

Bey Hing Goh ◽

Habsah Abdul Kadir

Keyword(s):

Colorectal Adenocarcinoma ◽

Therapeutic Potential ◽

Human Cancer ◽

Morphological Changes ◽

Biological Activities ◽

Mtor Pathway ◽

Human Cancer Cell Lines ◽

Adenocarcinoma Cells ◽

Underlying Mechanisms ◽

Ht 29

Dietary phytochemicals possess a variety of biological activities which can be widely discovered in fruits, vegetables and herbs. Geraniin, an ellagitannin is commonly found in fruits and herbs which possesses multitude of health benefits including anti-diabetic, hepatoprotective, anti-inflammatory and anticancer. However, the effects of geraniin on human colorectal adenocarcinoma cells have yet to be evaluated. This study aimed to investigate the apoptotic effects of geraniin against selected human cancer cell lines and elucidate its underlying mechanisms. Geraniin exhibited the strongest cytotoxic effect on HT-29 cells as determined by MTT assay. Events of apoptosis induced by geraniin in HT-29 cells was portrayed by apoptotic morphological changes, externalization of phosphatidylserine, DNA fragmentation and dissipation of mitochondrial membrane potential. Western blot analysis was then used to investigate the mechanisms underlying observed growth inhibition. Geraniin was found to initiate p53 activation further resulting in elevation of Bak/Bcl-xL ratio and caspase-3 activation. This eventually led to HT-29 cell death via apoptosis. Additionally, exposure of geraniin on HT-29 cells found to suppress the PI3K/Akt/mTOR pathway and suppression of NF-kB. Cumulative evidences in this study suggests that geraniin inhibited colorectal adenocarcinoma cell proliferation via apoptosis induction and suppression of PI3K/Akt/mTOR pathway. Thus, these findings provide novel mechanistic insight for the therapeutic potential of geraniin in the treatment of colorectal adenocarcinoma.

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Synthesis of Flavone Derivatives via N-Amination and Evaluation of Their Anticancer Activities

Molecules ◽

10.3390/molecules24152723 ◽

2019 ◽

Vol 24 (15) ◽

pp. 2723 ◽

Cited By ~ 1

Author(s):

Ni Zhang ◽

Jin Yang ◽

Ke Li ◽

Jun Luo ◽

Su Yang ◽

...

Keyword(s):

Cell Line ◽

Biological Activities ◽

Cancer Cell Line ◽

Prostate Cancer Cell Line ◽

Antibacterial Activities ◽

Anticancer Activities ◽

Structure Activity ◽

Ic50 Value ◽

Erythroleukemia Cell ◽

Flavone Derivatives

Seventeen new flavone derivatives substituted at the 4′-OH position were designed, synthesized and evaluated for their anticancer and antibacterial activities. Among them, compounds 3, 4, 6f, 6e, 6b, 6c and 6k demonstrated the most potent antiproliferative activities against a human erythroleukemia cell line (HEL) and a prostate cancer cell line (PC3). The results also showed that the IC50 value of compounds 3, 4, 6f, 6e, 6b, 6c and 6k were close to that of the anticancer drug cisplatin (DDP) and lower than that of apigenin. All of the derivatives did not present antibacterial activities. The structure–activity relationships evaluation showed that the configuration of methyl amino acid might affect their biological activities.

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Antioxidant and antibacterial activities of Opuntia ficus indica seed oil fractions and their bioactive compounds identification

Turkish Journal of Biochemistry ◽

10.1515/tjb-2016-0200 ◽

2017 ◽

Vol 42 (4) ◽

Cited By ~ 1

Author(s):

Olfa R’bia ◽

Chaker Chkioua ◽

Raoudha Hellal ◽

Wahid Herchi ◽

Samira Aschi Smiti

Keyword(s):

Bioactive Compounds ◽

Sulfonic Acid ◽

Seed Oil ◽

Biological Activities ◽

Antibacterial Activities ◽

Unsaponifiable Fraction ◽

Dpph Radical ◽

Inhibition Concentration ◽

Oil Fractions ◽

Β Carotene

AbstractAim:The twoMethods:Based on the inhibition concentration at 50 percent (ICResults:Results showed that antioxidant and antibacterial activities considerably varied depending on the fraction. In fact, unsaponifiable fraction has higher biological activities than the glyceridic ones. The unsaponifiable fraction has stronger effects of scavenging 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical and it is more efficient against bleaching of β-carotene than the saponifiable extract, unlike the experimental results of 2,2′-azino-bis3-ethylbenzthiazoline-6- sulfonic acid (ABTS) scavenging test. Furthermore, the unsaponifiable fraction was more efficient against all pathogenic strains speciallyConclusion:Informations provided through this work are important for the valorization and use of this cactus vegetable oil in cosmetic, pharmaceutical and nutraceutical industries.

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Antioxidant and Anticancer Activities and Protein Interaction of the Oxidovanadium(IV) Naringin Complex

Inorganics ◽

10.3390/inorganics10010013 ◽

2022 ◽

Vol 10 (1) ◽

pp. 13

Author(s):

Andrés Gonzalo Restrepo-Guerrero ◽

Helen Goitia-Semenco ◽

Luciana G. Naso ◽

Marilin Rey ◽

Pablo J. Gonzalez ◽

...

Keyword(s):

Reactive Oxygen Species ◽

Hydrophobic Interactions ◽

Biological Activities ◽

Physicochemical Characterization ◽

Reactive Oxygen ◽

Oxygen Species ◽

Anticancer Activities ◽

Apoptotic Pathway ◽

Synthetic Procedure

The complex of oxidovanadium(IV) with naringin (Narg) [VO(Narg)2] 8H2O (VONarg) was prepared according to the literature improving the synthetic procedure and physicochemical characterization. In addition, biological activities (cytotoxic, antioxidant, and BSA interaction) were determined. The metal coordinated through the 5-hydroxy and 4-carbonyl groups of rings A and C of naringin, respectively. The antioxidant activity of VONarg, determined in vitro, was higher than those of the flavonoid against superoxide and peroxyl reactive oxygen species (ROS) and DPPH radical. The cytotoxic properties were determined by a MTT assay on adenocarcinoma human alveolar basal epithelial cells (A549). VONarg exerted a 20% decrease in cancer cells viability at 24 h incubation, while naringin and oxidovanadium(IV) cation did not show cytotoxicity. Measurements with the normal HEK293 cell line showed that the inhibitory action of the complex is selective. VONarg generated intracellular reactive oxygen species (ROS), depletion of reduced glutathione and depolarization of mitochondrial membrane potential, typical for apoptotic pathway, producing cell death by oxidative stress mechanism. Moreover, naringin interacted with bovine serum albumin (BSA) through hydrophobic interactions in a spontaneous process, and VONarg showed greater affinity for the protein but can still be transported and delivered by it (Ka 104 L·mol−1 order).

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A Review on Anticancer Activities of Thiophene and Its Analogs

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557520666200715104555 ◽

2020 ◽

Vol 20 (19) ◽

pp. 1944-1965

Author(s):

Raghav Mishra ◽

Nitin Kumar ◽

Isha Mishra ◽

Neetu Sachan

Keyword(s):

Cancer Therapy ◽

Biological Activities ◽

Mortality Rates ◽

Oxygen Species ◽

Apoptosis Induction ◽

Significant Progress ◽

Anticancer Activities ◽

Structure Activity ◽

Thiophene Moiety

Cancer is the world's second-largest cause of mortality and one of the biggest global health concerns. The prevalence and mortality rates of cancer remain high despite significant progress in cancer therapy. The search for more effective, as well as less toxic treatment methods for cancer, is at the focus of current studies. Thiophene and its derivatives have surged as an influential scaffold, which, because of their appreciable diversity in biological activities, has drawn the concerned interest of the researchers in the field of medicinal chemistry. By the affluent introduction of its derivatives, which have antioxidant, anti-inflammatory, antimicrobial, and anticancer activities, the adaptability of the thiophene moiety has been displayed. The nature and positioning of the substitutions significantly impacted thiophene moiety activity. This decent array in the living response account about this moiety has picked plentiful researcher’s consideration to inquire about it to its peculiar potential across certain activities. In the field of cancer therapy against different cancer cells, the structure-activity relationship for each of the derivatives showed an excellent understanding of thiophene moiety. Information from the various articles revealed the key role of thiophene moiety and its derivatives to develop the vital lead compound. The essential anticancer mechanisms identified include inhibition of the topoisomerase, inhibition of tyrosine kinase, tubulin interaction and apoptosis induction through the activation of reactive oxygen species. This review is an endeavor to promote the anticancer potential of the derivatives, whether having thiophene or condensed thiophene as a core moiety or as a substituent that can lead in the future to synthesize varieties of chemotherapeutic entities in the field of cancer treatment.

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Anthocyanins As Modulators of Cell Redox-Dependent Pathways in Non-Communicable Diseases

Current Medicinal Chemistry ◽

10.2174/0929867325666181112093336 ◽

2020 ◽

Vol 27 (12) ◽

pp. 1955-1996 ◽

Cited By ~ 4

Author(s):

Antonio Speciale ◽

Antonella Saija ◽

Romina Bashllari ◽

Maria Sofia Molonia ◽

Claudia Muscarà ◽

...

Keyword(s):

Human Health ◽

Biological Activities ◽

Wide Spectrum ◽

Antioxidant Defenses ◽

Noncommunicable Diseases ◽

Protective Effects ◽

Pathological Conditions ◽

Chronic Pulmonary Diseases ◽

Underlying Mechanisms

: Chronic Noncommunicable Diseases (NCDs), mostly represented by cardiovascular diseases, diabetes, chronic pulmonary diseases, cancers, and several chronic pathologies, are one of the main causes of morbidity and mortality, and are mainly related to the occurrence of metabolic risk factors. Anthocyanins (ACNs) possess a wide spectrum of biological activities, such as anti-inflammatory, antioxidant, cardioprotective and chemopreventive properties, which are able to promote human health. Although ACNs present an apparent low bioavailability, their metabolites may play an important role in the in vivo protective effects observed. : This article directly addresses the scientific evidences supporting that ACNs could be useful to protect human population against several NCDs not only acting as antioxidant but through their capability to modulate cell redox-dependent signaling. In particular, ACNs interact with the NF-κB and AP-1 signal transduction pathways, which respond to oxidative signals and mediate a proinflammatory effect, and the Nrf2/ARE pathway and its regulated cytoprotective proteins (GST, NQO, HO-1, etc.), involved in both cellular antioxidant defenses and elimination/inactivation of toxic compounds, so countering the alterations caused by conditions of chemical/oxidative stress. In addition, supposed crosstalks could contribute to explain the protective effects of ACNs in different pathological conditions characterized by an altered balance among these pathways. Thus, this review underlines the importance of specific nutritional molecules for human health and focuses on the molecular targets and the underlying mechanisms of ACNs against various diseases.

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Structure and Activity of Pentacyclic Triterpenes Codrugs. A Review

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557521666210105110848 ◽

2021 ◽

Vol 21 ◽

Author(s):

Justyna Żwawiak ◽

Anna Pawełczyk ◽

Dorota Olender ◽

Lucjusz Zaprutko

Keyword(s):

Biological Activities ◽

Anticancer Activities ◽

Drug Molecule ◽

Pentacyclic Triterpene ◽

Formation Pathway ◽

Chemical Systems ◽

Drug Molecules ◽

Wide Range ◽

Anti Hiv ◽

Structure And Activity

: Triterpenes are a wide and important group of compounds that have several promising pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or anticancer activities. Such potent substances can be successfully incorporated in more complex chemical systems e.g. codrugs or pro-drugs that have better pharmacological profile. The codrug is connected with a drug formation pathway to chemically cohere at least two drug molecules to improve positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to generate effective compounds previously used as substrates. This article presents an overview of codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid codrugs are characterized by a wide range of biological activities. However, most of them have anticancer potency.

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Plant-Derived Nano and Microvesicles for Human Health and Therapeutic Potential in Nanomedicine

Pharmaceutics ◽

10.3390/pharmaceutics13040498 ◽

2021 ◽

Vol 13 (4) ◽

pp. 498

Author(s):

Mariaevelina Alfieri ◽

Antonietta Leone ◽

Alfredo Ambrosone

Keyword(s):

Therapeutic Potential ◽

Biological Activities ◽

Plant Biotechnology ◽

Bioactive Metabolites ◽

Anticancer Activities ◽

Long Distance ◽

In Vivo Models ◽

Therapeutic Tools

Plants produce different types of nano and micro-sized vesicles. Observed for the first time in the 60s, plant nano and microvesicles (PDVs) and their biological role have been inexplicably under investigated for a long time. Proteomic and metabolomic approaches revealed that PDVs carry numerous proteins with antifungal and antimicrobial activity, as well as bioactive metabolites with high pharmaceutical interest. PDVs have also been shown to be also involved in the intercellular transfer of small non-coding RNAs such as microRNAs, suggesting fascinating mechanisms of long-distance gene regulation and horizontal transfer of regulatory RNAs and inter-kingdom communications. High loading capacity, intrinsic biological activities, biocompatibility, and easy permeabilization in cell compartments make plant-derived vesicles excellent natural or bioengineered nanotools for biomedical applications. Growing evidence indicates that PDVs may exert anti-inflammatory, anti-oxidant, and anticancer activities in different in vitro and in vivo models. In addition, clinical trials are currently in progress to test the effectiveness of plant EVs in reducing insulin resistance and in preventing side effects of chemotherapy treatments. In this review, we concisely introduce PDVs, discuss shortly their most important biological and physiological roles in plants and provide clues on the use and the bioengineering of plant nano and microvesicles to develop innovative therapeutic tools in nanomedicine, able to encompass the current drawbacks in the delivery systems in nutraceutical and pharmaceutical technology. Finally, we predict that the advent of intense research efforts on PDVs may disclose new frontiers in plant biotechnology applied to nanomedicine.

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The biogenesis and biological function of PIWI-interacting RNA in cancer

Journal of Hematology & Oncology ◽

10.1186/s13045-021-01104-3 ◽

2021 ◽

Vol 14 (1) ◽

Author(s):

Silu Chen ◽

Shuai Ben ◽

Junyi Xin ◽

Shuwei Li ◽

Rui Zheng ◽

...

Keyword(s):

Cancer Diagnosis ◽

Precancerous Lesions ◽

Biological Activities ◽

Cancer Hallmarks ◽

Diagnosis And Prognosis ◽

Small Ncrnas ◽

Bioinformatics Databases ◽

Non Coding Rnas ◽

Underlying Mechanisms ◽

Proliferative Signaling

AbstractSmall non-coding RNAs (ncRNAs) are vital regulators of biological activities, and aberrant levels of small ncRNAs are commonly found in precancerous lesions and cancer. PIWI-interacting RNAs (piRNAs) are a novel type of small ncRNA initially discovered in germ cells that have a specific length (24–31 nucleotides), bind to PIWI proteins, and show 2′-O-methyl modification at the 3′-end. Numerous studies have revealed that piRNAs can play important roles in tumorigenesis via multiple biological regulatory mechanisms, including silencing transcriptional and posttranscriptional gene processes and accelerating multiprotein interactions. piRNAs are emerging players in the malignant transformation of normal cells and participate in the regulation of cancer hallmarks. Most of the specific cancer hallmarks regulated by piRNAs are involved in sustaining proliferative signaling, resistance to cell death or apoptosis, and activation of invasion and metastasis. Additionally, piRNAs have been used as biomarkers for cancer diagnosis and prognosis and have great potential for clinical utility. However, research on the underlying mechanisms of piRNAs in cancer is limited. Here, we systematically reviewed recent advances in the biogenesis and biological functions of piRNAs and relevant bioinformatics databases with the aim of providing insights into cancer diagnosis and clinical applications. We also focused on some cancer hallmarks rarely reported to be related to piRNAs, which can promote in-depth research of piRNAs in molecular biology and facilitate their clinical translation into cancer treatment.

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