scholarly journals Ursolic Acid-Based Derivatives as Potential Anti-Cancer Agents: An Update

2020 ◽  
Vol 21 (16) ◽  
pp. 5920 ◽  
Author(s):  
Vuyolwethu Khwaza ◽  
Opeoluwa O. Oyedeji ◽  
Blessing A. Aderibigbe
Keyword(s):  
Ursolic Acid ◽  
Clinical Medicine ◽  
Biological Activities ◽  
Therapeutic Effects ◽  
Pharmacological Activities ◽  
Pentacyclic Triterpenoid ◽  
Anti Cancer ◽  
Pharmacologically Active ◽  
Derivatives Of ◽  
Cell Signaling Pathways

Ursolic acid is a pharmacologically active pentacyclic triterpenoid derived from medicinal plants, fruit, and vegetables. The pharmacological activities of ursolic acid have been extensively studied over the past few years and various reports have revealed that ursolic acid has multiple biological activities, which include anti-inflammatory, antioxidant, anti-cancer, etc. In terms of cancer treatment, ursolic acid interacts with a number of molecular targets that play an essential role in many cell signaling pathways. It suppresses transformation, inhibits proliferation, and induces apoptosis of tumor cells. Although ursolic acid has many benefits, its therapeutic applications in clinical medicine are limited by its poor bioavailability and absorption. To overcome such disadvantages, researchers around the globe have designed and developed synthetic ursolic acid derivatives with enhanced therapeutic effects by structurally modifying the parent skeleton of ursolic acid. These structurally modified compounds display enhanced therapeutic effects when compared to ursolic acid. This present review summarizes various synthesized derivatives of ursolic acid with anti-cancer activity which were reported from 2015 to date.

Ursolic Acid in Cancer Treatment and Metastatic Chemoprevention: From Synthesized Derivatives to Nanoformulations in Preclinical Studies

2019 ◽  
Vol 19 (4) ◽  
pp. 245-256 ◽  
Author(s):  
Junjie Zou ◽  
Juanfang Lin ◽  
Chao Li ◽  
Ruirui Zhao ◽  
Lulu Fan ◽  
...  
Keyword(s):  
Ursolic Acid ◽  
Cancer Metastasis ◽  
Biological Activities ◽  
Inhibitory Effect ◽  
Cancer Drug ◽  
Therapeutic Effects ◽  
Candidate Drug ◽  
Wide Range ◽  
Anti Cancer ◽  
Tumor Growth And Metastasis

Background:Cancer metastasis has emerged as a major public health threat that causes majority of cancer fatalities. Traditional chemotherapeutics have been effective in the past but suffer from low therapeutic efficiency and harmful side-effects. Recently, it has been reported ursolic acid (UA), one of the naturally abundant pentacyclic triterpenes, possesses a wide range of biological activities including anti-inflammatory, anti-atherosclerotic, and anti-cancer properties. More importantly, UA has the features of low toxicity, liver protection and the potential of anti-cancer metastasis.Objective:This article aimed at reviewing the great potential of UA used as a candidate drug in the field of cancer therapy relating to suppression of tumor initiation, progression and metastasis.Methods:Selective searches were conducted in Pubmed, Google Scholar and Web of Science using the keywords and subheadings from database inception to December 2017. Systemic reviews are summarized here.Results:UA has exhibited chemopreventive and therapeutic effects of cancer mainly through inducing apoptosis, inhibiting cell proliferation, preventing tumor angiogenesis and metastatic. UA nanoformulations could enhance the solubility and bioavailability of UA as well as exhibit better inhibitory effect on tumor growth and metastasis.Conclusion:The information presented in this article can provide useful references for further studies on making UA a promising anti-cancer drug, especially as a prophylactic metastatic agent for clinical applications.

Jaceosidin: a natural flavone with versatile pharmacological and biological activities

2020 ◽  
Vol 26 ◽  
Author(s):  
Bushra Nageen ◽  
Azhar Rasul ◽  
Ghulam Hussain ◽  
Muhammad Ajmal Shah ◽  
Haseeb Anwar ◽  
...  
Keyword(s):  
Biological Activities ◽  
Review Article ◽  
Therapeutic Action ◽  
Health Issues ◽  
Pharmacological Activities ◽  
Terrestrial Vertebrates ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Reported Data ◽  
Cell Signaling Pathways

: Nature always remains an inexhaustible source of treasures for mankind. It remains a mystery for every challenge until the completion of the challenge. While we talk about the complicated health issues, nature offers us a great variety of chemical scaffolds and their various moieties packed in the form of natural products e.g., plants, microorganisms (fungi, algae, protozoa), and terrestrial vertebrates and invertebrates. This review article is an update about jaceosidin, a bioactive flavone, from genus Artemisia. This potentially active compound exhibits a variety of pharmacological activities including antiinflammatory, anti-oxidant, anti-bacterial, anti-allergic and anti-cancer. The bioactivities and the therapeutic action of jaceosidin, especially the modulation of different cell signaling pathways (ERK1/2, NF-κB, PI3K/Akt and ATM-Chk1/2) which become deregulated in various pathological disorders, have been focused here. The reported data suggest that the bioavailability of this anti-cancer compound should be enhanced by utilizing various chemical biology and medicinal chemistry techniques. Moreover, it is recommended that researchers and scientists should work on the mode of action of this particular flavone to precede it further as a potent anti-cancer compound.

Structure-Bioactivity Relationship Study of Xanthene Derivatives: A Brief Review

2020 ◽  
Vol 16 (8) ◽  
pp. 1071-1077
Author(s):  
Aref G. Ghahsare ◽  
Zahra S. Nazifi ◽  
Seyed M.R. Nazifi
Keyword(s):  
Biological Activities ◽  
Cyclic Compound ◽  
Research Field ◽  
Pharmaceutical Chemistry ◽  
Therapeutic Effects ◽  
Main Research ◽  
Research Fields ◽  
Xanthene Derivatives ◽  
Anti Cancer ◽  
Heterocyclic Derivatives

: Over the last decades, several heterocyclic derivatives compounds have been synthesized or extracted from natural resources and have been tested for their pharmaceutical activities. Xanthene is one of these heterocyclic derivatives. These compounds consist of an oxygen-containing central heterocyclic structure with two more cyclic structures fused to the central cyclic compound. It has been shown that xanthane derivatives are bioactive compounds with diverse activities such as anti-bacterial, anti-fungal, anti-cancer, and anti-inflammatory as well as therapeutic effects on diabetes and Alzheimer. The anti-cancer activity of such compounds has been one of the main research fields in pharmaceutical chemistry. Due to this diverse biological activity, xanthene core derivatives are still an attractive research field for both academia and industry. This review addresses the current finding on the biological activities of xanthene derivatives and discussed in detail some aspects of their structure-activity relationship (SAR).

scholarly journals Anti-Cancer Potential of Synthetic Oleanolic Acid Derivatives and Their Conjugates with NSAIDs

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4957
Author(s):  
Wanda Baer-Dubowska ◽  
Maria Narożna ◽  
Violetta Krajka-Kuźniak
Keyword(s):  
Signaling Pathways ◽  
Oleanolic Acid ◽  
Short Review ◽  
Therapeutic Effects ◽  
Pentacyclic Triterpenoid ◽  
Anti Cancer ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Synthetic Derivatives ◽  
Cancer Activity

Naturally occurring pentacyclic triterpenoid oleanolic acid (OA) serves as a good scaffold for additional modifications to achieve synthetic derivatives. Therefore, a large number of triterpenoids have been synthetically modified in order to increase their bioactivity and their protective or therapeutic effects. Moreover, attempts were performed to conjugate synthetic triterpenoids with non-steroidal anti-inflammatory drugs (NSAIDs) or other functional groups. Among hundreds of synthesized triterpenoids, still the most promising is 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO), which reached clinical trials level of investigations. The new group of synthetic triterpenoids are OA oximes. The most active among them is 3-hydroxyiminoolean-12-en-28-oic acid morpholide, which additionally improves the anti-cancer activity of standard NSAIDs. While targeting the Nrf2 and NF-κB signaling pathways is the main mechanism of synthetic OA derivatives′ anti-inflammatory and anti-cancer activity, most of these compounds exhibit multifunctional activity, and affect cross-talk within the cellular signaling network. This short review updates the earlier data and describes the new OA derivatives and their conjugates in the context of modification of signaling pathways involved in inflammation and cell survival and subsequently in cancer development.

scholarly journals PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

2017 ◽  
Vol 10 (6) ◽  
pp. 237 ◽  
Author(s):  
Ishwar Bhat K ◽  
Abhishek Kumar
Keyword(s):  
Acetic Acid ◽  
Cytotoxic Activity ◽  
Glacial Acetic Acid ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

scholarly journals Ursolic Acid—A Pentacyclic Triterpenoid with a Wide Spectrum of Pharmacological Activities

Molecules ◽  
2015 ◽  
Vol 20 (11) ◽  
pp. 20614-20641 ◽  
Author(s):  
Łukasz Woźniak ◽  
Sylwia Skąpska ◽  
Krystian Marszałek
Keyword(s):  
Ursolic Acid ◽  
Wide Spectrum ◽  
Pharmacological Activities ◽  
Pentacyclic Triterpenoid

Phytochemical composition and biological activity of Physalis spp.: A mini-review

2020 ◽  
Vol 3 (1) ◽  
pp. 56
Author(s):  
Venelina Popova ◽  
Albena Stoyanova ◽  
Nadezhda Mazova
Keyword(s):  
Functional Foods ◽  
Biological Activities ◽  
Metabolite Profile ◽  
Sucrose Esters ◽  
Nutritional Properties ◽  
Pharmacological Activities ◽  
Future Studies ◽  
Phytochemical Composition ◽  
Anti Cancer ◽  
Biological And Pharmacological Activities

The main objective of this mini-review was to synthesize recent data about the phytochemical composition, the nutritional properties, and the biological and pharmacological activities of a now cosmopolitan genus, Physalis (Solanaceae), being in the focus of intensive research over the last two decades. Six Physalis species with nutritional and pharmacological promise are considered in particular – P. peruviana L., P. philadelphica Lam., P. ixocarpa Brot. ex Horm., P. angulata L., P. pubescens L., and P. alkekengi L. Summarized contemporary data on the metabolite profile and the biological activities of Physalis species support their century-long use in traditional medicine and human nutrition. The fruit represent a rich source of minerals, vitamins, fibers, carotenoids, proteins, fructose, sucrose esters, pectins, flavonoids, polyphenols, polyunsaturated fatty acids, phytosterols and many other beneficial nutrients. Individual phytochemicals and complex fractions isolated from Physalis plants demonstrate various biological and pharmacological activities, the most promising of which include antimicrobial, antioxidant, anti-diabetic, hepato-renoprotective, anti-cancer, anti-inflammatory, immunomodulatory and others. Most of these activities are associated with the presence of flavonoids, phenylpropanoids, alkaloids, physalins, withanolides, and other bioactive compounds. The accumulated data disclose the potential of Physalis spp. as highly functional foods, as profitable crops for many regions over the world, and as sources of valuable secondary metabolites for phytopharmacy, novel medicine and cosmetics. Information provided by this review is also important for a more intensive promotion of Physalis species in Bulgaria and for future studies on their composition and benefits.

Synthesis and Reactions of Perimidines and Their Fused Systems

2020 ◽  
Vol 24 (15) ◽  
pp. 1669-1716 ◽  
Author(s):  
Thoraya A. Farghaly ◽  
Sami A. Al-Hussain ◽  
Zeinab A. Muhammad ◽  
Magda A. Abdallah ◽  
Magdi E. A. Zaki
Keyword(s):  
Chemical Reactions ◽  
Heterocyclic Compounds ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Lone Pair ◽  
Pharmacological Activities ◽  
Synthetic Analogs ◽  
Interesting Class ◽  
Derivatives Of

Perimidines are peri-naphtho-fused derivatives of pyrimidine. They are of particular interest as they are a rare example of an azine in which the lone pair of electrons of pyrrole-like nitrogen participates in the π-system of the molecule. Perimidine is an interesting class of heterocyclic compounds. Various synthetic analogs of perimidines have been prepared and evaluated for many pharmacological activities in different models with desired findings. They exhibit biological activities as antitumor, antiulcer, antimicrobial, and antifungal agents. This review is an attempt to organize the synthesis and chemical reactions of perimidine analogs reported to date systematically since 1955. It should be noted that this review is the first one that includes the preparation and reactions of the perimidine ring.

Anti-Angiogenic Activity of Curcumin in Cancer Therapy: A Narrative Review

2019 ◽  
Vol 17 (3) ◽  
pp. 262-269 ◽  
Author(s):  
Abolfazl Shakeri ◽  
Natalie Ward ◽  
Yunes Panahi ◽  
Amirhossein Sahebkar
Keyword(s):  
Curcuma Longa ◽  
Tumour Microenvironment ◽  
Pharmacological Activities ◽  
Angiogenic Activity ◽  
Tumour Metastasis ◽  
Naturally Occurring ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Apoptotic Pathways ◽  
Cell Signaling Pathways

Curcumin is a naturally occurring polyphenol isolated from Curcuma longa that has various pharmacological activities, including, anti-inflammatory, anti-oxidant and anti-cancer properties. The anticancer effect of curcumin is attributed to activation of apoptotic pathways in cancer cells, as well as inhibition of inflammation and angiogenesis in the tumour microenvironment and suppression of tumour metastasis. Angiogenesis, which is the formation of new blood vessels from pre-existing ones, is a fundamental step in tumour growth and expansion. Several reports have demonstrated that curcumin inhibits angiogenesis in a wide variety of tumour cells through the modulation of various cell signaling pathways which involve transcription factors, protein kinases, growth factors and enzymes. This review provides an updated summary of the various pathways and molecular targets that are regulated by curcumin to elicit its anti-angiogenic activity.

Heterocyclic Compounds Bearing Triazine Scaffold and Their Biological Significance: A Review

2020 ◽  
Vol 20 (1) ◽  
pp. 4-28
Author(s):  
Tarawanti Verma ◽  
Manish Sinha ◽  
Nitin Bansal
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Significance ◽  
Resonance Energy ◽  
Weak Bases ◽  
Anti Cancer ◽  
Interesting Class ◽  
Synthetic Derivatives ◽  
Derivatives Of

Benzene is a six-membered hydrocarbon ring system and if three carbon-hydrogen units of benzene ring are replaced by nitrogen atoms then triazine is formed. Triazines are present in three isomeric forms 1,2,3- triazine, 1,2,4-triazine, and 1,3,5-triazine according to the position of the nitrogen atom. These are weak bases having weaker resonance energy than benzene, so nucleophilic substitution is preferred than electrophilic substitution. Triazine is an interesting class of heterocyclic compounds in medicinal chemistry. Numerous synthetic derivatives of triazine have been prepared and evaluated for a wide spectrum of biological activities in different models with desired findings such as antibacterial, antifungal, anti-cancer, antiviral, antimalarial, antiinflammatory, antiulcer, anticonvulsant, antimicrobial, insecticidal and herbicidal agents. Triazine analogs have exposed potent pharmacological activity. So, triazine nucleus may be considered as an interesting core moiety for researchers for the development of future drugs.

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