scholarly journals Synthesis, Modification and Biological Activity of Diosgenyl β-d-Glycosaminosides: An Overview

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5433
Author(s):  
Daria Grzywacz ◽  
Beata Liberek ◽  
Henryk Myszka
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Protecting Groups ◽  
Pharmacological Properties ◽  
Amino Group ◽  
Reaction Conditions ◽  
Naturally Occurring ◽  
Anti Cancer ◽  
Wide Group ◽  
Derivatives Of

Saponins are a structurally diverse class of natural glycosides that possess a broad spectrum of biological activities. They are composed of hydrophilic carbohydrate moiety and hydrophobic triterpenoid or steroid aglycon. Naturally occurring diosgenyl glycosides are the most abundant steroid saponins, and many of them exhibit various pharmacological properties. Herein, we present an overview of semisynthetic saponins syntheses–diosgenyl β-d-glycosaminosides (d-gluco and d-galacto). These glycosides possess a 2-amino group, which creates great possibilities for further modifications. A wide group of glycosyl donors, different N-protecting groups and various reaction conditions used for their synthesis are presented. In addition, this paper demonstrates the possibilities of chemical modifications of diosgenyl β-d-glycosaminosides, associated with functionalisation of the amino group. These provide N-acyl, N-alkyl, N,N-dialkyl, N-cinnamoyl, 2-ureido and 2-thiosemicarbazonyl derivatives of diosgenyl β-d-glycosaminosides, for which the results of biological activity tests (antifungal, antibacterial, anti-cancer and hemolytic) are presented.

scholarly journals Insight into the Presence of Stilbenes in Medicinal Plants Traditionally Used in Croatian Folk Medicine

2016 ◽  
Vol 11 (6) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Ivana Generalić Mekinić ◽  
Danijela Skroza ◽  
Ivica Ljubenkov ◽  
Višnja Katalinić
Keyword(s):  
Biological Activity ◽  
Medicinal Plants ◽  
Biological Activities ◽  
Folk Medicine ◽  
Free Form ◽  
Naturally Occurring ◽  
Derivatives Of ◽  
Insight Into ◽  
Phenolic Extracts

Over the last years, great interest has arisen concerning plant stilbenes, especially resveratrol, which has a whole spectrum of positive biological activities. In this study, we investigated the presence of resveratrol monomers (trans- and cis- form) and naturally occurring derivatives of fraas-resveratrol (piceid, astringin and isorhapontin) in phenolic extracts of twenty medicinal plants traditionally used in Croatian folk medicine. The investigated compounds were present in the samples, in free form or as glucosides, and the highest share was found in immortelle, common yarrow and Lamiaceae plants. The obtained results indicate that biological activity of selected medicinal plants can be related to the presence of this valuable group of phytochemicals.

scholarly journals Synthetic Chiral Derivatives of Xanthones: Biological Activities and Enantioselectivity Studies

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 791 ◽  
Author(s):  
Carla Fernandes ◽  
Maria Carraro ◽  
João Ribeiro ◽  
Joana Araújo ◽  
Maria Tiritan ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Pharmacological Activities ◽  
Sar Studies ◽  
Naturally Occurring ◽  
Structure Activity ◽  
Wide Range ◽  
Synthetic Methodologies ◽  
Derivatives Of ◽  
Biological And Pharmacological Activities

Many naturally occurring xanthones are chiral and present a wide range of biological and pharmacological activities. Some of them have been exhaustively studied and subsequently, obtained by synthesis. In order to obtain libraries of compounds for structure activity relationship (SAR) studies as well as to improve the biological activity, new bioactive analogues and derivatives inspired in natural prototypes were synthetized. Bioactive natural xanthones compromise a large structural multiplicity of compounds, including a diversity of chiral derivatives. Thus, recently an exponential interest in synthetic chiral derivatives of xanthones (CDXs) has been witnessed. The synthetic methodologies can afford structures that otherwise could not be reached within the natural products for biological activity and SAR studies. Another reason that justifies this trend is that both enantiomers can be obtained by using appropriate synthetic pathways, allowing the possibility to perform enantioselectivity studies. In this work, a literature review of synthetic CDXs is presented. The structures, the approaches used for their synthesis and the biological activities are described, emphasizing the enantioselectivity studies.

Naphthoquinone Derivatives Isolated from Plants: Recent Advances in Biological Activity

2020 ◽  
Vol 20 (19) ◽  
pp. 2019-2035
Author(s):  
Esmaeil Sheikh Ahmadi ◽  
Amir Tajbakhsh ◽  
Milad Iranshahy ◽  
Javad Asili ◽  
Nadine Kretschmer ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Biological Activity ◽  
Small Molecules ◽  
Anticancer Activity ◽  
Clinical Significance ◽  
Phase Ii ◽  
Biological Activities ◽  
Phase Ii Clinical Trials ◽  
Naturally Occurring ◽  
The Subject

Naturally occurring naphthoquinones (NQs) comprising highly reactive small molecules are the subject of increasing attention due to their promising biological activities such as antioxidant, antimicrobial, apoptosis-inducing activities, and especially anticancer activity. Lapachol, lapachone, and napabucasin belong to the NQs and are in phase II clinical trials for the treatment of many cancers. This review aims to provide a comprehensive and updated overview on the biological activities of several new NQs isolated from different species of plants reported from January 2013 to January 2020, their potential therapeutic applications and their clinical significance.

scholarly journals Hemisynthesis and Biological Evaluation of Cinnamylated, Benzylated, and Prenylated Dihydrochalcones from a Common Bio-Sourced Precursor

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 620
Author(s):  
Anne Ardaillou ◽  
Jérôme Alsarraf ◽  
Jean Legault ◽  
François Simard ◽  
André Pichette
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Pharmacological Properties ◽  
Cytotoxic Potential ◽  
Naturally Occurring

Several families of naturally occurring C-alkylated dihydrochalcones display a broad range of biological activities, including antimicrobial and cytotoxic properties, depending on their alkylation sidechain. The catalytic Friedel–Crafts alkylation of the readily available aglycon moiety of neohesperidin dihydrochalcone was performed using cinnamyl, benzyl, and isoprenyl alcohols. This procedure provided a straightforward access to a series of derivatives that were structurally related to natural balsacones, uvaretin, and erioschalcones, respectively. The antibacterial and cytotoxic potential of these novel analogs was evaluated in vitro and highlighted some relations between the structure and the pharmacological properties of alkylated dihydrochalcones.

Identification of promising objects for the synthesis of thiosulphonate derivatives of benzoquinone and hydroquinone

2021 ◽  
Vol 4 (2) ◽  
pp. 47-53
Author(s):  
N. Y. Monka ◽  
◽  
N. E. Stadnytska ◽  
I. R. Buchkevych ◽  
K. O. Kaplia ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Experimental Studies ◽  
New Drugs ◽  
Reduced Form ◽  
Free Form ◽  
Wide Range ◽  
On Line ◽  
Living Organisms ◽  
Derivatives Of

Benzoquinone and its reduced form hydroquinone belong to phenolic compounds and are found in living organisms in free form or in glycosides. They are active substances of some medicinal plants and have a pharmacological effect on the human body. Accordingly, their derivatives are important objects for chemical synthesis and development of new drugs. This article presents the findings of the structural design of substances with benzoquinone or hydroquinone fragment and sulfur-containing compound. By use of appropriate on-line programs a predictive screening of the biological activity and cytotoxicity of thiosulfonate derivatives of benzoquinone and hydroquinone has been conducted. It has been found that they have immense methodological potential to be synthesized by substances with a wide range of biological activities and a high value of probable activity, which substantiates the feasibility of conducting experimental studies on their biological activity, particularly anticancer.

scholarly journals Essentials Oils from Brazilian Eugenia and Syzygium Species and Their Biological Activities

Biomolecules ◽  
2020 ◽  
Vol 10 (8) ◽  
pp. 1155
Author(s):  
Jamile S. da Costa ◽  
Ellen de Nazaré S. da Cruz ◽  
William N. Setzer ◽  
Joyce Kelly do R. da Silva ◽  
José Guilherme S. Maia ◽  
...  
Keyword(s):  
Biological Activity ◽  
South America ◽  
Biological Activities ◽  
Herbal Medicines ◽  
Chemical Diversity ◽  
Pharmacological Properties ◽  
Sesquiterpene Hydrocarbons ◽  
Leishmania Spp ◽  
Alternative Sources ◽  
Interspecific Diversity

The Eugenia and Syzygium genera include approximately 1000 and 1800 species, respectively, and both belong to the Myrtaceae. Their species present economic and medicinal importance and pharmacological properties. Due to their chemical diversity and biological activity, we are reporting the essential oils of 48 species of these two genera, which grow in South America and found mainly in Brazil. Chemically, a total of 127 oil samples have been described and displayed a higher intraspecific and interspecific diversity for both Eugenia spp. and Syzygium spp., according to the site of collection or seasonality. The main volatile compounds were sesquiterpene hydrocarbons and oxygenated sesquiterpenes, mainly with caryophyllane and germacrane skeletons and monoterpenes of mostly the pinane type. The oils presented many biological activities, especially antimicrobial (antifungal and antibacterial), anticholinesterase, anticancer (breast, gastric, melanoma, prostate), antiprotozoal (Leishmania spp.), antioxidant, acaricidal, antinociceptive and anti-inflammatory. These studies can contribute to the rational and economic exploration of Eugenia and Syzygium species once they have been identified as potent natural and alternative sources to the production of new herbal medicines.

scholarly journals Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

2019 ◽  
Vol 20 (17) ◽  
pp. 4238 ◽  
Author(s):  
Yaqi Ren ◽  
Chunlan Wang ◽  
Jiakun Xu ◽  
Shuaiyu Wang
Keyword(s):  
Furan Ring ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coffee Beans ◽  
Anti Cancer ◽  
Underlying Mechanisms ◽  
Target Alternative ◽  
Anti Inflammation

Cafestol and kahweol are natural diterpenes extracted from coffee beans. In addition to the effect of raising serum lipid, in vitro and in vivo experimental results have revealed that the two diterpenes demonstrate multiple potential pharmacological actions such as anti-inflammation, hepatoprotective, anti-cancer, anti-diabetic, and anti-osteoclastogenesis activities. The most relevant mechanisms involved are down-regulating inflammation mediators, increasing glutathione (GSH), inducing apoptosis of tumor cells and anti-angiogenesis. Cafestol and kahweol show similar biological activities but not exactly the same, which might due to the presence of one conjugated double bond on the furan ring of the latter. This review aims to summarize the pharmacological properties and the underlying mechanisms of cafestol-type diterpenoids, which show their potential as functional food and multi-target alternative medicine.

scholarly journals Recent study on the anticancer activity of nobiletin and its metabolites

2021 ◽  
Vol 14 ◽  
Author(s):  
Ke Lv ◽  
Lingling Zhang ◽  
Hui Zhao ◽  
Chi-Tang Ho ◽  
Shiming Li
Keyword(s):  
Cancer Prevention ◽  
Anticancer Activity ◽  
Promising Candidate ◽  
Naturally Occurring ◽  
Antitumor Potential ◽  
Anti Cancer ◽  
Citrus Peels ◽  
Derivatives Of ◽  
Cancer Activity

The exploration of naturally occurring phytochemicals with antitumor potential has been the focus of many studies. Nobiletin, a polymethoxyflavone (PMF) exclusively derived from citrus peels, has been reported as a promising candidate for the prevention and/or treatment of cancers. Additionally, multiple demethylated derivatives of nobiletin from in vivo biotransformation, including 3′-demethylnobiletin (3′-DMN), 4′-demethylnobiletin (4′-DMN), 3′,4′-didemethylnobiletin (3′,4′-DDMN) and 5-demethylnobiletin (5-DMN), among others, have been found to show anti-cancer activity. In this review, the anticancer activity of nobiletin and its derivatives in cancer prevention are comprehensively described.

scholarly journals A Review: Underutilized plant of Sabah and Its Potential Value

2021 ◽  
Vol 22 ◽  
Author(s):  
Nor Amirah Shamsudin ◽  
Lucky Poh Wah Goh ◽  
Mohd Khalizan Sabullah ◽  
Suraya Abdul Sani ◽  
Rahmath Abdulla ◽  
...  
Keyword(s):  
Additional Data ◽  
Biological Activities ◽  
Local Area ◽  
Pharmacological Properties ◽  
Health Product ◽  
Sustainable Resources ◽  
Potential Value ◽  
Medicinal Value ◽  
Anti Cancer ◽  
Pharmacological Studies

Abstract: Underutilized plants are referred to a plant species which their potential is not fully utilized yet and they are usually found abundantly in certain local area but globally rare. Sabah is known for a high biodiversity and contains many underutilized plants. To our knowledge, this is the first review is to provide an overview information of medicinal value and pharmacological properties of underutilized plant in Sabah. Extract and metabolites in different part of several underutilized plant contains multiple beneficial bioactive compounds and exploitation of these compounds was supported by additional data which plays various biological activities including anti-atherosclerotic, anti-cancer, antihypercholesterolemic and anti-ulcerogenic. A handful of pharmacological studies on the natural product these underutilized plants have conclusively outlined the mode of action in treatment of several diseases and in other health aspects. This paper limits its scope to reviewe and highlight the potential of using underutilized plants in Sabah only which could serve as reliable resource for health product development in pharmaceutical and nutraceutical through continuous discovering of more active and sustainable resources as well as ingredients for food and medicine.

scholarly journals Synthesis and Biological Activities of Pyrazino[1,2-a]indole and Pyrazino[1,2-a]indol-1-one Derivatives

2021 ◽  
Vol 14 (8) ◽  
pp. 779
Author(s):  
Kena Zhang ◽  
Christine Tran ◽  
Mouad Alami ◽  
Abdallah Hamze ◽  
Olivier Provot
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Metal Catalysts ◽  
Point Of View ◽  
Cyclization Reactions ◽  
Metal Free ◽  
Michael Reactions ◽  
Anti Cancer ◽  
Synthetic Routes ◽  
Metal Catalyzed

This review concerns the synthesis and biological activities of pyrazino[1,2-a]indoles and pyrazino[1,2-a]indol-1-ones reported since 1997 and the discovery of biological activity of pyrazinoindole derivatives. In the first part, we first presented the synthetic routes that have been reported from a methodological point of view to access the pyrazinoindole unit according to cyclization reactions using or not using metal catalysts. Then, syntheses and neuropsychiatric, auto-immune, anti-infectious and anti-cancer properties of pyrazinoindoles were detailed. In the second part, we first reported the main accesses to pyrazinoindol-1-one substrates according to Michael reactions, metal-catalyzed and metal-free cyclization reactions. The syntheses and anti-cancer, anti-infectious, anti-allergenic and neuropsychiatric properties of pyrazinoindolones were next described and discussed.

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