Natural Sesquiterpene Lactones as Potential Trypanocidal Therapeutic Agents: A Review

Chagas’ disease and Human African Trypanosomiasis are parasitic diseases that remain major health problems, mainly among the poorest and the most marginalized communities from Latin America and Africa. The scarcity of effective chemotherapy, due to the low investment in the research and development (R&D) of new drugs, together with a high incidence of side effects, and the emergence of drug resistance phenomena emphasize the urgent need for new prophylactic and therapeutic agents. Over the ages, humans have employed natural products to treat a wide spectrum of diseases. Recently, the pharmaceutical industry has focused on plant research and a large body of evidence has been collected to demonstrate the immense potential of medicinal plants as a source of bioactive compounds and lead molecules. In the field of parasitic diseases, drug development from plants has been successful for the sesquiterpene lactone (STL) artemisinin, which is employed as an antimalarial agent. STLs are a large group of naturally occurring terpenoids derived from plants that mostly belong to the Asteraceae family which exhibit a variety of skeletal arrangements and are the largest and most diverse category of natural products with an α-methylene-λ-lactone motif. STLs display a broad spectrum of biological activities such as antitumor, cytotoxic, antibacterial, anthelmintic, uterus contracting, antimalarial, neurotoxic, antiprotozoal and allergic (contact dermatitis) activities. In this context, the purpose of the present review is to provide an overview of the trypanocidal activity reported for STLs against Trypanosoma cruzi and T. brucei rhodesiense over the period 1993–2015.

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Natural Products Targeting the Mitochondria in Cancers

Molecules ◽

10.3390/molecules26010092 ◽

2020 ◽

Vol 26 (1) ◽

pp. 92

Author(s):

Yue Yang ◽

Ping-Ya He ◽

Yi Zhang ◽

Ning Li

Keyword(s):

Natural Products ◽

Anticancer Drugs ◽

Web Of Science ◽

Keyword Search ◽

Biological Activities ◽

Natural Compounds ◽

New Drugs ◽

Antitumor Effects ◽

Regulate Cell Growth ◽

Anticancer Drug Discovery

There are abundant sources of anticancer drugs in nature that have a broad prospect in anticancer drug discovery. Natural compounds, with biological activities extracted from plants and marine and microbial metabolites, have significant antitumor effects, but their mechanisms are various. In addition to providing energy to cells, mitochondria are involved in processes, such as cell differentiation, cell signaling, and cell apoptosis, and they have the ability to regulate cell growth and cell cycle. Summing up recent data on how natural products regulate mitochondria is valuable for the development of anticancer drugs. This review focuses on natural products that have shown antitumor effects via regulating mitochondria. The search was done in PubMed, Web of Science, and Google Scholar databases, over a 5-year period, between 2015 and 2020, with a keyword search that focused on natural products, natural compounds, phytomedicine, Chinese medicine, antitumor, and mitochondria. Many natural products have been studied to have antitumor effects on different cells and can be further processed into useful drugs to treat cancer. In the process of searching for valuable new drugs, natural products such as terpenoids, flavonoids, saponins, alkaloids, coumarins, and quinones cover the broad space.

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Effect of guaianolides in the meiosis reinitiation of amphibian oocytes

Zygote ◽

10.1017/s0967199416000265 ◽

2016 ◽

Vol 25 (1) ◽

pp. 10-16 ◽

Cited By ~ 2

Author(s):

J. Zapata-Martínez ◽

G. Sánchez-Toranzo ◽

F. Chaín ◽

C.A.N. Catalán ◽

M.I. Bühler

Keyword(s):

Biological Activities ◽

Wide Spectrum ◽

Sesquiterpene Lactones ◽

Inhibitory Effect ◽

Biological Molecules ◽

Plant Metabolites ◽

Major Mechanism ◽

Bufo Arenarum ◽

Asteraceae Family

SummarySesquiterpene lactones (STLs) are a large and structurally diverse group of plant metabolites generally found in the Asteraceae family. STLs exhibit a wide spectrum of biological activities and it is generally accepted that their major mechanism of action is the alkylation of the thiol groups of biological molecules. The guaianolides is one of various groups of STLs. Anti-tumour and anti-migraine effects, an allergenic agent, an inhibitor of smooth muscle cells and of meristematic cell proliferation are only a few of the most commonly reported activities of STLs. In amphibians, fully grown ovarian oocytes are arrested at the beginning of meiosis I. Under stimulus with progesterone, this meiotic arrest is released and meiosis progresses to metaphase II, a process known as oocyte maturation. There are previous records of the inhibitory effect of dehydroleucodin (DhL), a guaianolide lactone, on the progression of meiosis. It has been also shown that DhL and its 11,13-dihydroderivative (2H-DhL; a mixture of epimers at C-11) act as blockers of the resumption of meiosis in fully grown ovarian oocytes from the amphibian Rhinella arenarum (formerly classified as Bufo arenarum). The aim of this study was to analyze the effect of four closely related guaianolides, i.e., DhL, achillin, desacetoxymatricarin and estafietin as possible inhibitors of meiosis in oocytes of amphibians in vitro and discuss some structure–activity relationships. It was found that the inhibitory effect on meiosis resumption is greater when the lactone has two potentially reactive centres, either a α,β–α′,β′-diunsaturated cyclopentanone moiety or an epoxide group plus an exo-methylene-γ-lactone function.

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Neuroprotective Effects, Biological Activities and Therapeutic Potential of Phytochemicals: A Comprehensive Review

10.31487/j.ajmc.2020.01.04 ◽

2020 ◽

pp. 1-11

Author(s):

Xi-jun Wang ◽

Shi Qiu ◽

Aihua Zhang ◽

Jian-hua Miao ◽

Hui Sun ◽

...

Keyword(s):

Natural Products ◽

Neurological Disorders ◽

Chemical Biology ◽

Therapeutic Potential ◽

Biological Activities ◽

Therapeutic Agents ◽

Neuroprotective Effects ◽

Alternative Medicines ◽

Pharmacological Targets ◽

The World

The incidence of neurological disorders is growing in the world together with an increased lifespan. Nowadays, there are still no effective treatments for neurodegenerative pathology, which make necessary to search for new therapeutic agents. Natural products, most of them used in phytochemicals from herbal medicine, are considered promising alternatives for the treatment of neurodegenerative diseases. Numerous herbs have been applied to neurodegenerative disease treatments as complementary and alternative medicines. In the 21st century, omics-coupled functional pharmacology was developed for neurodegenerative drug discovery from natural products. In this article, we firstly provide the latest understanding of neurological disorders on risk factors, category, diagnosis and treatment, and then specially present an overview of natural products in neuroprotective effects research from chemical biology to pharmacological targets, and also discuss the natural products application and future challenge.

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In vitro and in vivo activities of flavonoids – apigenin, baicalin, chrysin, scutellarin – in regulation of hypertension – a review for their possible effects in pregnancy-induced hypertension

Herba Polonica ◽

10.2478/hepo-2019-0001 ◽

2019 ◽

Vol 65 (1) ◽

pp. 55-70 ◽

Cited By ~ 1

Author(s):

Marcin Ożarowski ◽

Radosław Kujawski ◽

Przemysław Ł. Mikołajczak ◽

Karolina Wielgus ◽

Andrzej Klejewski ◽

...

Keyword(s):

Ex Vivo ◽

Biological Activities ◽

Wide Spectrum ◽

Chemical Compounds ◽

New Drugs ◽

Future Application ◽

Mediators Of Inflammation ◽

And Function

Summary Flavonoids and their conjugates are the most important group of natural chemical compounds in drug discovery and development. The search for pharmacological activity and new mechanisms of activity of these chemical compounds, which may inhibit mediators of inflammation and influence the structure and function of endothelial cells, can be an interesting pharmacological strategy for the prevention and adjunctive treatments of hypertension, especially induced by pregnancy. Because cardiovascular diseases have multi-factorial pathogenesis these natural chemical compounds with wide spectrum of biological activities are the most interesting source of new drugs. Extracts from one of the most popular plant used in Traditional Chinese Medicine, Scutellaria baicalensis Georgi could be a very interesting source of flavonoids because of its exact content in quercetin, apigenin, chrysin and scutellarin as well as in baicalin. These flavonoids exert vasoprotective properties and many activities such as: anti-oxidative via several pathways, anti-in-flammatory, anti-ischaemic, cardioprotective and anti-hypertensive. However, there is lack of summaries of results of studies in context of potential and future application of flavonoids with determined composition and activity. Our review aims to provide a literature survey of in vitro, in vivo and ex vivo pharmacological studies of selected flavonoids (apigenin, chrysin and scutellarin, baicalin) in various models of hypertension carried out in 2008–2018.

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THE RED BLOOD CELLS CATALASE ACTIVITY IS INFLUENCED BY TARAXACUM OFFICINALE

InterConf ◽

10.51582/interconf.21-22.05.2021.020 ◽

2021 ◽

pp. 167-177

Author(s):

Ala Fulga ◽

Valeriana Pantea ◽

Svetlana Protopop ◽

Olga Tagadiuc ◽

Mihail Todiras ◽

...

Keyword(s):

Antioxidant Activity ◽

Catalase Activity ◽

Biological Activities ◽

Wide Spectrum ◽

Sesquiterpene Lactones ◽

Natural Antioxidants ◽

Taraxacum Officinale ◽

Biologically Active ◽

Ability To Act ◽

Leaves And Roots

Natural antioxidants protect cells against oxidative stress, which is directly involved in ageing processes and in the pathogenesis of cardiovascular, neurodegenerative and neoplastic diseases. Taraxacum officinale (TO) due to its rich content of biologically active ingredients has been commonly used in traditional medicine. It contains a wide spectrum of compounds with antioxidant activity. The content depends of parts of this plant. The roots are rich in phenolic and terpene compounds, sesquiterpene lactones, fructosans and inulin, while leaves are rich in substances belonging to flavonoids, phenolic acids, coumarins and vitamins, especially vitamin A. The literature results prove that antioxidant activity of TO depends on several factors including the plant part, the solvent used, as well as the duration of extraction. The aim of this study was to evaluate and to compare the action of alcoholic extracts of roots and leaves of TO on RBC’s catalase activity. Material and methods. Raw Taraxacum officinale plant material consisted of dried leaves and roots were harvested from a natural site. The extracts for analysis were prepared using 20, 25, 40, 50 and 80% (v/v) ethanol mixtures used as solvents. The catalase activity was established by using RBC of healthy persons. Conclusions. Phytotherapeutic herbs and plants continue to play an important role in the discovery and development of drugs. Leaves and roots of dandelion represent a rich source of bioactive compounds for potential exploitation in nutraceuticals and pharmacological sectors. Taraxacum officinale has a high ability to act as an antioxidant. The highest influence on RBC’s catalase activity was reported in case of roots ethanolic extracts of 25%. These actions are realized due to multiple substances, whose content probably depends of ethanol’s concentration. Additional studies are needed to characterize biological activities of these extracts.

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Dihydroresveratrol Type Dihydrostilbenoids: Chemical Diversity, Chemosystematics, and Bioactivity

Current Medicinal Chemistry ◽

10.2174/0929867324666170830112343 ◽

2018 ◽

Vol 25 (10) ◽

pp. 1194-1240 ◽

Cited By ~ 2

Author(s):

Sara Vitalini ◽

Serhat S. Cicek ◽

Sebastian Granica ◽

Christian Zidorn

Keyword(s):

Natural Products ◽

Anticancer Activity ◽

Biological Activities ◽

Wide Spectrum ◽

Pathogenic Fungi ◽

Chemical Diversity ◽

Limited Information ◽

Lead Compounds ◽

Naturally Occurring

Background: Dihydrostilbenoids, a diverse class of natural products differing from stilbenoids by the missing double bond in the ethylene chain linking the aromatic moieties, have been reported from fungi, mosses, ferns, and flowering plants. Objective: Occurrence, structure, and bioactivity of naturally occurring dihydroresveratrol type dihydrostilbenoids are discussed in this review. Method: A Reaxys database search for dihydroresveratrol derivatives with possible substitutions on all atoms, but excluding non-natural products and compounds featuring additional rings involving the ethyl connecting chain, was performed. Results: Structures include simple dihydroresveratrol derivatives, compounds substituted with complex side chains composed of acyl moieties and sugars, and compounds containing polycyclic cores attached to dihydrostilbenoid units. Dihydrostilbenoids have a wide spectrum of bioactivities ranging from expectable antioxidant and anti-inflammatory activities to interesting neuroprotective and anticancer activity. The anticancer activity in particular is very pronounced for some plant-derived dihydrostilbenoids and makes them interesting lead compounds for drug development. Apart from some reports on dihydroresveratrol derivatives as phytoalexins against plant-pathogenic fungi, only very limited information is available on the ecological role of these compounds for the organisms producing them. Conclusion: Dihydrostilbenoids are a class of natural products possessing significant biological activities; their scattered but not ubiquitous occurrence throughout the kingdoms of plants and fungi is not easily explained. We are convinced that future studies will identify new sources of dihydrostilbenoids, and we hope that the present review will inspire such studies and will help in directing such efforts to suitable source organisms and towards promising bioactivities.

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γ-Hydroxybutenolide Containing Marine Natural Products and Their Synthesis: A Review

Current Organic Chemistry ◽

10.2174/1385272823666191021122810 ◽

2020 ◽

Vol 23 (22) ◽

pp. 2436-2468

Author(s):

Supriya Tilvi ◽

Safia Khan ◽

Mahesh S. Majik

Keyword(s):

Natural Products ◽

Phospholipase A2 ◽

Marine Natural Products ◽

Biological Activities ◽

Therapeutic Agents ◽

Marine Sponges ◽

Molecular Structures ◽

Pharmacological Properties ◽

Secretory Phospholipase A2 ◽

Biological Studies

: γ-Hydroxybutenolides (γ-HB) is an important structural core found in many bioactive marine natural products (MNPS). The γ-HB core containing NPS served as an inspiration to medicinal chemists to undertake designing of the new synthetic strategies to construct γ-HB core. Subsequently, it further results in the development of novel physiological and therapeutic agents. The most notable example includes manoalides, cacospongionolides, petrosaspongioide M and dysidiolide from marine sponges possessing anti-inflammatory properties. γ-HB containing MNPS were known to possess various pharmacological properties such as antimicrobial (acantholide B), cytotoxic (acantholide A-E, spongianolide A), inhibitors of secretory phospholipase A2 (cladocorans A and B), BACE inhibitors (ianthellidone G), etc. Moreover, the γ-HB moiety was explored as antifouling agents as well. Owing to their numerous biological activities and attractive molecular structures, there are lots of advances in the synthetic methodology of these compounds. This review gives the account on isolation and biological studies of MNPS with γ-HB skeleton as a core unit. Furthermore, the synthesis of selective γ-HB containing bioactive MNPS like manoalide, secomanoalide, cacospongionolides, luffarielloide and dysidiolide were highlighted in the article.

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Fastidious Anatomization of Biota Procured Compounds on Cancer Drug Discovery

Current Pharmaceutical Biotechnology ◽

10.2174/1389201020666191128145015 ◽

2020 ◽

Vol 21 (5) ◽

pp. 354-363

Author(s):

Anand Thirupathi ◽

Chandra M. Shanmugavadivelu ◽

Sampathkumar Natarajan

Keyword(s):

Natural Products ◽

Side Effects ◽

Cancer Therapy ◽

Biological Activities ◽

Drug Approval ◽

Current Treatment ◽

New Drugs ◽

Cancer Drug ◽

Synthetic Drugs ◽

Wide Range

Background: Natural products are the rootstock for identifying new drugs since ancient times. In comparison with synthetic drugs, they have abounding beneficial effects in bestowing protection against many diseases, including cancer. Cancer has been observed as a major threat in recent decades, and its prevalence is expected to increase over the next decades. Also, current treatment methods in cancer therapy such as radiation therapy and chemotherapy cause severe adverse side effects among the cancer population. Therefore, it is exigent to find a remedy without any side effects. Methods: In recent years, research has focused on obtaining naturally derived products to encounter this complication. The current pace of investigations, such as gene identification and advancement in combinatorial chemistry, leads to the aberrant access to a wide range of new synthetic drugs. In fact, natural products act as templates in structure predictions and synthesis of new compounds with enhanced biological activities. Results: Recent developments in genomics have established the importance of polymorphism, which implies that patients require different drugs for their treatment. This demands the discovery of a large number of drugs, but limited sources restrict the pharmaceutical industry to overcome these major obstacles. The use of natural products and their semisynthetic and synthetic analogues could alleviate these problems. However, the lack of standardization in terms of developing methods for evaluating the chemical composition, efficacy, isolation and international approval is still a major limitation in this field. In the past few years, several drug-approval authorities, including the FDA and WHO have allowed using these naturally derived compounds in humans. Conclusion: In this review, we described the use of some natural products from plant and marine sources in cancer treatment and shed some light on semi-synthetic and synthetic compounds derived from natural sources used in cancer therapy.

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Coumarin sulfonamide derivatives: An emerging class of therapeutic agents

Heterocyclic Communications ◽

10.1515/hc-2020-0008 ◽

2020 ◽

Vol 26 (1) ◽

pp. 46-59 ◽

Cited By ~ 1

Author(s):

Ali Irfan ◽

Laila Rubab ◽

Mishbah Ur Rehman ◽

Rukhsana Anjum ◽

Sami Ullah ◽

...

Keyword(s):

Therapeutic Potential ◽

Biological Activities ◽

Wide Spectrum ◽

Structural Features ◽

Therapeutic Agents ◽

Review Article ◽

Structural Motif ◽

Structure Activity ◽

Anti Cancer ◽

Novel Therapeutic

AbstractCoumarin sulfonamide is a heterocyclic pharmacophore and an important structural motif which is a core and integral part of different therapeutic scaffolds and analogues. Coumarin sulfonamides are privileged and pivotal templates which have a broad spectrum of applications in the fields of medicine, pharmacology and pharmaceutics. Coumarin sulfonamide exhibited versatile and myriad biomedical activities such as anti-bacterial, antiviral, antifungal, anti-inflammatory and anti-cancer. This review article focuses on the structural features of coumarin sulfonamide derivatives in the treatment of different lethal diseases on the basis of structure-activity relationships (SAR). The plethora of research cited in this review article summarizes and discusses the various substitutions around the coumarin sulfonamide nucleus which have provided a wide spectrum of biological activities and therapeutic potential that has proved attractive to many researchers looking to exploit the coumarin sulfonamide skeleton for drug discovery and the development of novel therapeutic agents.

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Hydroalcoholic Extract of Myrcia bella Loaded into a Microemulsion System: A Study of Antifungal and Mutagenic Potential

Planta Medica ◽

10.1055/a-1323-3622 ◽

2021 ◽

Author(s):

Gabriel Davi Marena ◽

Luiza Girotto ◽

Luiz Leonardo Saldanha ◽

Matheus Aparecido dos Santos Ramos ◽

Rone Aparecido De Grandis ◽

...

Keyword(s):

Natural Products ◽

Mutagenic Activity ◽

Biological Activities ◽

Folk Medicine ◽

Antimicrobial Properties ◽

New Drugs ◽

Microemulsion System ◽

Mutagenic Potential ◽

Candida Sp ◽

Grape Seed Oil

Abstract Myrcia bella is a medicinal plant used for the treatment of diabetes, hemorrhages, and hypertension in Brazilian folk medicine. Considering that plant extracts are attractive sources of new drugs, the aim of the present study was to verify the influence of incorporating 70% hydroalcoholic of M. bella leaves in nanostructured lipid systems on the mutagenic and antifungal activities of the extract. In this work, we evaluated the antifungal potential of M. bella loaded on the microemulsion against Candida sp for minimum inhibitory concentration, using the microdilution technique. The system was composed of polyoxyethylene 20 cetyl ether and soybean phosphatidylcholine (10%), grape seed oil, cholesterol (10%: proportion 5/1), and purified water (80%). To investigate the mutagenic activity, the Ames test was used with the Salmonella Typhimurium tester strains. M. bella, either incorporated or free, showed an important antifungal effect against all tested strains. Moreover, the incorporation surprisingly inhibited the mutagenicity presented by the extract. The present study attests the antimicrobial properties of M. bella extract, contributing to the search for new natural products with biological activities and suggesting caution in its use for medicinal purposes. In addition, the results emphasize the importance of the use of nanotechnology associated with natural products as a strategy for the control of infections caused mainly by the genus Candida sp.

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