Galangin: A metabolite that suppresses anti-neoplastic activities through modulation of oncogenic targets

2021 ◽  
pp. 153537022110625
Author(s):  
Hardeep Singh Tuli ◽  
Katrin Sak ◽  
Shubham Adhikary ◽  
Ginpreet Kaur ◽  
Diwakar Aggarwal ◽  
...  
Keyword(s):  
Cancer Incidence ◽  
Natural Compound ◽  
Biological Activities ◽  
Chemotherapeutic Drugs ◽  
Lead Compounds ◽  
Molecular Oncology ◽  
Wide Range ◽  
Anti Cancer ◽  
The World

With the dramatic increase in cancer incidence all over the world in the last decades, studies on identifying novel efficient anti-cancer agents have been intensified. Historically, natural products have represented one of the most important sources of new lead compounds with a wide range of biological activities. In this article, the multifaceted anti-cancer action of propolis-derived flavonoid, galangin, is presented, discussing its antioxidant, anti-inflammatory, antiproliferative, pro-apoptotic, anti-angiogenic, and anti-metastatic effects in various cancer cells. In addition, co-effects with standard chemotherapeutic drugs as well as other natural compounds are also under discussion, besides highlighting modern nanotechnological advancements for overcoming the low bioavailability issue characteristic of galangin. Although further studies are needed for confirming the anti-cancer potential of galangin in vivo malignant systems, exploring this natural compound might open new perspectives in molecular oncology.

scholarly journals A Review on Daphnane-Type Diterpenoids and Their Bioactive Studies

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1842 ◽  
Author(s):  
Yue-Xian Jin ◽  
Lei-Ling Shi ◽  
Da-Peng Zhang ◽  
Hong-Yan Wei ◽  
Yuan Si ◽  
...  
Keyword(s):  
Biological Activities ◽  
Structural Diversity ◽  
Cytotoxic Activities ◽  
Hydroxyl Groups ◽  
Substitution Pattern ◽  
In Vivo Experiments ◽  
Wide Range ◽  
Anti Cancer

Natural daphnane diterpenoids, mainly distributed in plants of the Thymelaeaceae and Euphorbiaceae families, usually include a 5/7/6-tricyclic ring system with poly-hydroxyl groups located at C-3, C-4, C-5, C-9, C-13, C-14, or C-20, while some special types have a characteristic orthoester motif triaxially connectedat C-9, C-13, and C-14. The daphnane-type diterpenoids can be classified into five types: 6-epoxy daphnane diterpenoids, resiniferonoids, genkwanines, 1-alkyldaphnanes and rediocides, based on the oxygen-containing functions at rings B and C, as well as the substitution pattern of ring A. Up to now, nearly 200 daphnane-type diterpenoids have been isolated and elucidated from the Thymelaeaceae and Euphorbiaceae families. In-vitro and in-vivo experiments of these compounds have shown that they possess a wide range of biological activities, including anti-HIV, anti-cancer, anti-leukemic, neurotrophic, pesticidal and cytotoxic effects. A comprehensive account of the structural diversity is given in this review, along with the cytotoxic activities of daphnane-type diterpenoids, up to April 2019.

scholarly journals Recent Developments on the Synthetic and Biological Applications of Chalcones-A Review

2021 ◽  
Vol 12 (1) ◽  
pp. 180-195
Keyword(s):  
Physical Properties ◽  
Scientific Community ◽  
Biological Activities ◽  
Critical Discussion ◽  
Biological Applications ◽  
Wide Range ◽  
Anti Cancer ◽  
The World ◽  
Recent Developments ◽  
Optical Fluorescence

Chalcones are precursors of the biosynthesis of flavonoids present in plants. These motifs serve a wide range of applications, from synthetic to pharmacological to physical spheres. Chalcone derivatives attracted the scientific community all over the world in recent times due to their diversified applications. The presence of reactive α,β-unsaturated carbonyl moiety in chalcones makes them a versatile intermediate in synthesizing various classes of compounds of biological and physical interest. More importantly, the chalcones themselves have been known to possess enormous biological activities and physical properties like semiconductor, non-linear optical, fluorescence, and electronic properties. In this context, the present review summarises the overall developments in the synthetic, pharmacological, and physical applications of chalcones in recent fast. The critical discussion was attempted on the synthetic applications and biological potencies as anti-cancer, antidiabetic, antimicrobial, antioxidant, and anti-inflammatory.

Potential Triazole-based Molecules for the Treatment of Neglected Diseases

2019 ◽  
Vol 26 (23) ◽  
pp. 4403-4434 ◽  
Author(s):  
Susimaire Pedersoli Mantoani ◽  
Peterson de Andrade ◽  
Talita Perez Cantuaria Chierrito ◽  
Andreza Silva Figueredo ◽  
Ivone Carvalho
Keyword(s):  
Effective Treatment ◽  
Chagas Disease ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Neglected Diseases ◽  
Triazole Derivatives ◽  
Wide Range ◽  
The World ◽  
Great Relevance ◽  
The Moment

Neglected Diseases (NDs) affect million of people, especially the poorest population around the world. Several efforts to an effective treatment have proved insufficient at the moment. In this context, triazole derivatives have shown great relevance in medicinal chemistry due to a wide range of biological activities. This review aims to describe some of the most relevant and recent research focused on 1,2,3- and 1,2,4-triazolebased molecules targeting four expressive NDs: Chagas disease, Malaria, Tuberculosis and Leishmaniasis.

Ethnomedicinal uses, Phytochemistry and Pharmacological Aspects of the Genus Berberis Linn: A Comprehensive Review

2020 ◽  
Vol 23 ◽  
Author(s):  
Roohi Mohi-ud-din ◽  
Reyaz Hassan Mir ◽  
Prince Ahad Mir ◽  
Saeema Farooq ◽  
Syed Naiem Raza ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Pharmacological Activities ◽  
Traditional Use ◽  
Comprehensive Review ◽  
Wide Range ◽  
Anti Cancer ◽  
Comprehensive Survey ◽  
Ethnomedicinal Uses

Background: Genus Berberis (family Berberidaceae), which contains about 650 species and 17 genera worldwide, has been used in folklore and various traditional medicine systems. Berberis Linn. is the most established group among genera with around 450-500 species across the world. This comprehensive review will not only help researchers for further evaluation but also provide substantial information for future exploitation of species to develop novel herbal formulations. Objective: The present review is focussed to summarize and collect the updated review of information of Genus Berberis species reported to date regarding their ethnomedicinal information, chemical constituents, traditional/folklore use, and reported pharmacological activities on more than 40 species of Berberis. Conclusion: A comprehensive survey of the literature reveals that various species of the genus possess various phytoconstituents mainly alkaloids, flavonoid based compounds isolated from different parts of a plant with a wide range of pharmacological activities. So far, many pharmacological activities like anti-cancer, anti-hyperlipidemic, hepatoprotective, immunomodulatory, anti-inflammatory both in vitro & in vivo and clinical study of different extracts/isolated compounds of different species of Berberis have been reported, proving their importance as a medicinal plant and claiming their traditional use.

Associated microflora of medicinal ferns: biotechnological potentials and possible applications

2016 ◽  
Vol 5 (03) ◽  
pp. 4927 ◽  
Author(s):  
Shubhi Srivastava ◽  
Paul A. K.
Keyword(s):  
Secondary Metabolites ◽  
Growth Promotion ◽  
Biological Activities ◽  
Hydrolytic Enzymes ◽  
In Vitro Production ◽  
Wide Range ◽  
Negative Effect ◽  
Bacteria And Fungi

Plant associated microorganisms that colonize the upper and internal tissues of roots, stems, leaves and flowers of healthy plants without causing any visible harmful or negative effect on their host. Diversity of microbes have been extensively studied in a wide variety of vascular plants and shown to promote plant establishment, growth and development and impart resistance against pathogenic infections. Ferns and their associated microbes have also attracted the attention of the scientific communities as sources of novel bioactive secondary metabolites. The ferns and fern alleles, which are well adapted to diverse environmental conditions, produce various secondary metabolites such as flavonoids, steroids, alkaloids, phenols, triterpenoid compounds, variety of amino acids and fatty acids along with some unique metabolites as adaptive features and are traditionally used for human health and medicine. In this review attention has been focused to prepare a comprehensive account of ethnomedicinal properties of some common ferns and fern alleles. Association of bacteria and fungi in the rhizosphere, phyllosphere and endosphere of these medicinally important ferns and their interaction with the host plant has been emphasized keeping in view their possible biotechnological potentials and applications. The processes of host-microbe interaction leading to establishment and colonization of endophytes are less-well characterized in comparison to rhizospheric and phyllospheric microflora. However, the endophytes are possessing same characteristics as rhizospheric and phyllospheric to stimulate the in vivo synthesis as well as in vitro production of secondary metabolites with a wide range of biological activities such as plant growth promotion by production of phytohormones, siderophores, fixation of nitrogen, and phosphate solubilization. Synthesis of pharmaceutically important products such as anticancer compounds, antioxidants, antimicrobials, antiviral substances and hydrolytic enzymes could be some of the promising areas of research and commercial exploitation.

scholarly journals Designer Oncolytic Adenovirus: Coming of Age

Cancers ◽  
2018 ◽  
Vol 10 (6) ◽  
pp. 201 ◽  
Author(s):  
Alexander Baker ◽  
Carmen Aguirre-Hernández ◽  
Gunnel Halldén ◽  
Alan Parker
Keyword(s):  
Checkpoint Inhibitors ◽  
Coming Of Age ◽  
Oncolytic Adenovirus ◽  
Detailed Knowledge ◽  
Immunomodulatory Agents ◽  
Double Stranded Dna ◽  
Wide Range ◽  
Anti Cancer ◽  
Targeting Ability

The licensing of talimogene laherparepvec (T-Vec) represented a landmark moment for oncolytic virotherapy, since it provided unequivocal evidence for the long-touted potential of genetically modified replicating viruses as anti-cancer agents. Whilst T-Vec is promising as a locally delivered virotherapy, especially in combination with immune-checkpoint inhibitors, the quest continues for a virus capable of specific tumour cell killing via systemic administration. One candidate is oncolytic adenovirus (Ad); it’s double stranded DNA genome is easily manipulated and a wide range of strategies and technologies have been employed to empower the vector with improved pharmacokinetics and tumour targeting ability. As well characterised clinical and experimental agents, we have detailed knowledge of adenoviruses’ mechanisms of pathogenicity, supported by detailed virological studies and in vivo interactions. In this review we highlight the strides made in the engineering of bespoke adenoviral vectors to specifically infect, replicate within, and destroy tumour cells. We discuss how mutations in genes regulating adenoviral replication after cell entry can be used to restrict replication to the tumour, and summarise how detailed knowledge of viral capsid interactions enable rational modification to eliminate native tropisms, and simultaneously promote active uptake by cancerous tissues. We argue that these designer-viruses, exploiting the viruses natural mechanisms and regulated at every level of replication, represent the ideal platforms for local overexpression of therapeutic transgenes such as immunomodulatory agents. Where T-Vec has paved the way, Ad-based vectors now follow. The era of designer oncolytic virotherapies looks decidedly as though it will soon become a reality.

Combinatorial Synthesis of Novel 3/5(3,5)-(Di)nitro/chloropaeonol Carbonyl Hydrazone Derivatives as Nematicidal Agents

2021 ◽  
Vol 24 ◽  
Author(s):  
Genqiang Chen ◽  
Lina Zhu ◽  
Yanfei Xia ◽  
Jinming Yang ◽  
Song Zhang ◽  
...  
Keyword(s):  
High Efficiency ◽  
Biological Activities ◽  
Science Research ◽  
Nematicidal Activity ◽  
Effective Control ◽  
Root Bark ◽  
Naturally Occurring ◽  
Whole Plant ◽  
Wide Range

Background: Developing the high-efficiency and low-risk small-molecule green-nematocide is the key of effective control of the nematodes. Paeonol, is a naturally occurring phenolic compound, isolated from the root bark of Paeonia suffruticosa and the whole plant of Cynanchum paniculatum. Due to its crucial phenolic ketone skeleton, modern biological science research has indicated that paeonol has a wide range of biological activities. The structural modification of paeonol into paeonol carbonyl hydrazone derivatives is a potential approach for the development of novel nematodes, which showed more toxicity than paeonol. However, there are no reports on the nematicidal activity of paeonol carbonyl hydrazone derivatives to control Heterodera glycines. Results: We always endeavor to discover and develop biorational natural products-based pesticidal agents, 4 significant intermediates and 21 novel 3/5(3,5)-(di)nitro/chloropaeonol carbonyl hydrazone derivatives were prepared, and their structures well characterized by 1H NMR, HRMS, MS, and mp. Due to the steric hindrance, the substituents on the C=N double bond of all hydrazine compounds adopted E configuration. Results of nematicidal activity revealed that, among all compounds, especially 5-nitropaeonol (5) and 3,5-dinitropaeonol (7) displayed the most potent nematicidal activity H. glycines in vivo with LC50 values of 0.0323 and 0.0367 mg/mL, respectively. Conclusion: It suggested that for the 3/5(3,5)-(di)nitro/chloropaeonol carbonyl hydrazone derivatives, a nitro group introduced at C5 position of 1 was necessary for obtaining the potent compound as nematicidal agents. These preliminary results will pave the way for further modification of paeonol in the development of potential new nematicides.

Sixty Years Young: The Diverse Biological Activities of Metal Polypyridyl Complexes Pioneered by Francis P. Dwyer

2012 ◽  
Vol 65 (9) ◽  
pp. 1325 ◽  
Author(s):  
Nathan L. Kilah ◽  
Eric Meggers
Keyword(s):  
Inorganic Chemistry ◽  
Biological Activities ◽  
Biologically Active ◽  
Ruthenium Polypyridyl ◽  
Polypyridyl Complexes ◽  
Anti Cancer ◽  
Ruthenium Polypyridyl Complexes ◽  
Medicinal Inorganic Chemistry ◽  
Sixtieth Anniversary

Sixty years ago, the Australian chemist Francis P. Dwyer pioneered the use of ruthenium polypyridyl complexes as biologically active compounds. These chemically inert and configurationally stable complexes revealed an astonishing range of interesting biological activities, such as the inhibition of the enzyme acetylcholinesterase, anti-cancer activity in vivo, and bacteriostatic/bacteriocidal action. This review commemorates the sixtieth anniversary of Dwyer and co-workers’ landmark 1952 publication, summarises their broader achievements in biological inorganic chemistry, and discusses the contribution of this work to the development of modern biological and medicinal inorganic chemistry.

Ethnic Use, Phytochemistry, and Pharmacology of Cyperus rotundus

2022 ◽  
pp. 431-453
Author(s):  
Mohammed Rahmatullah ◽  
Khoshnur Jannat ◽  
Gerald R. Reeck ◽  
Rownak Jahan ◽  
Taufiq Rahman ◽  
...  
Keyword(s):  
Wound Healing ◽  
Skin Diseases ◽  
Cyperus Rotundus ◽  
Invasive Weed ◽  
Lead Compounds ◽  
Traditional Uses ◽  
Novel Drugs ◽  
Anti Cancer ◽  
The World ◽  
Scientific Validation

Cyperus rotundus (nut grass in English) is a perennial erect sedge plant and is distributed in over 90 countries of the world, where it has been mostly classified as a highly invasive weed. Despite this classification, the plant has been considered from traditional times to be medicinally important. The traditional uses of the plant in various countries include uses against various gastrointestinal tract disorders, skin diseases, leprosy, fever, and neurological disorders. Evaluation of the plant and especially its rhizomes in a scientific manner has revealed the presence of numerous phytochemicals and wide-ranging pharmacological activities, which include anti-microbial, gastrointestinal, wound healing, anti-diabetic, anti-cancer, anti-malarial, anti-obesity, hepatoprotective, and anti-pyretic activity. The scientific validation of a number of traditional uses strongly indicates that the plant may prove useful in the discovery of a number of lead compounds and novel drugs.

scholarly journals Andrographolide, A Natural Antioxidant: An Update

Antioxidants ◽  
2019 ◽  
Vol 8 (12) ◽  
pp. 571 ◽  
Author(s):  
Eugenie Mussard ◽  
Annabelle Cesaro ◽  
Eric Lespessailles ◽  
Brigitte Legrain ◽  
Sabine Berteina-Raboin ◽  
...  
Keyword(s):  
Signaling Pathway ◽  
Herbal Remedy ◽  
Biological Activities ◽  
Lung Infection ◽  
Andrographis Paniculata ◽  
Natural Antioxidant ◽  
Nuclear Factor ◽  
Wide Range ◽  
Anti Cancer ◽  
Antioxidant Mechanisms

Traditionally, Andrographis paniculata has been used as an herbal remedy for lung infection treatments. Its leaves contain a diterpenoid labdane called andrographolide responsible for a wide range of biological activities such as antioxidant, anti-inflammatory, and anti-cancer properties. This manuscript is a brief review of the antioxidant mechanisms and the regulation of the Nrf2 (nuclear factor (erythroid-derived 2)-like 2) signaling pathway by andrographolide.

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