Marine Algae as Source of Novel Antileishmanial Drugs: A Review

Yamthé, Lauve Rachel Tchokouaha; Appiah–Opong, Regina; Fokou, Patrick Valère Tsouh; Tsabang, Nolé; Boyom, Fabrice Fekam; Nyarko, Alexander Kwadwo; Wilson, Michael D.

doi:10.3390/md15110323

Cited by 30 publications

(17 citation statements)

References 75 publications

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“…L. donovani is a neglected tropical disease spread by sandflies affecting millions of people per year and can be fatal in its visceral form if left untreated . Intravenous amphotericin is the only currently approved treatment for visceral leishmaniasis in the US, though interest in new treatments is strong. − The bis(methyl acetal) membranoid scaffold seen in membranoids B–E ( 6 – 9 ) represents an intriguing model in functionality that could serve as the basis of future studies to enhance their therapeutic potential.…”

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confidence: 99%

Spongian Diterpenoids Derived from the Antarctic Sponge Dendrilla antarctica Are Potent Inhibitors of the Leishmania Parasite

et al. 2020

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From the CH 2 Cl 2 extract of the Antarctic sponge Dendrilla antarctica we found spongian diterpenes, including previously reported aplysulphurin (1), tetrahydroaplysulphurin-1 (2), membranolide (3), and darwinolide (4), utilizing a CH 2 Cl 2 / MeOH extraction scheme. However, the extracts also yielded diterpenes bearing one or more methyl acetal functionalities (5−9), two of which are previously unreported, while others are revised here. Further investigation of diterpene reactivity led to additional new metabolites (10−12), which identified them as well as the methyl acetals as artifacts from methanolysis of aplysulphurin. The bioactivity of the methanolysis products, membranoids A−H (5−12), as well as natural products 1−4, were assessed for activity against Leishmania donovani-infected J774A.1 macrophages, revealing insights into their structure/activity relationships. Four diterpenes, tetrahydroaplysulphurin-1 (2) as well as membranoids B (6), D (8), and G (11), displayed low micromolar activity against L. donovani with no discernible cytotoxicity against uninfected J774A.1 cells. Leishmaniasis is a neglected tropical disease that affects one million people every year and can be fatal if left untreated.

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confidence: 99%

Spongian Diterpenoids Derived from the Antarctic Sponge Dendrilla antarctica Are Potent Inhibitors of the Leishmania Parasite

et al. 2020

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“…These compounds include diterpenes, halogenated triterpenes, sulfated polysaccharides, acetogenins, polyphenols and others (Figure 6). A recent review estimated that 151 extracts from up to 30,000 macroalgae species identified worldwide have proven antileishmanial activity [287]. From these, 48 extracts were obtained from brown Phaeophyceae macroalgae, 80 from Rhodophyceae and 23 from green Chlorophytes.…”

Section: Algae-derived Compoundsmentioning

confidence: 99%

Screening Marine Natural Products for New Drug Leads against Trypanosomatids and Malaria

et al. 2020

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Neglected Tropical Diseases (NTD) represent a serious threat to humans, especially for those living in poor or developing countries. Almost one-sixth of the world population is at risk of suffering from these diseases and many thousands die because of NTDs, to which we should add the sanitary, labor and social issues that hinder the economic development of these countries. Protozoan-borne diseases are responsible for more than one million deaths every year. Visceral leishmaniasis, Chagas disease or sleeping sickness are among the most lethal NTDs. Despite not being considered an NTD by the World Health Organization (WHO), malaria must be added to this sinister group. Malaria, caused by the apicomplexan parasite Plasmodium falciparum, is responsible for thousands of deaths each year. The treatment of this disease has been losing effectiveness year after year. Many of the medicines currently in use are obsolete due to their gradual loss of efficacy, their intrinsic toxicity and the emergence of drug resistance or a lack of adherence to treatment. Therefore, there is an urgent and global need for new drugs. Despite this, the scant interest shown by most of the stakeholders involved in the pharmaceutical industry makes our present therapeutic arsenal scarce, and until recently, the search for new drugs has not been seriously addressed. The sources of new drugs for these and other pathologies include natural products, synthetic molecules or repurposing drugs. The most frequent sources of natural products are microorganisms, e.g., bacteria, fungi, yeasts, algae and plants, which are able to synthesize many drugs that are currently in use (e.g. antimicrobials, antitumor, immunosuppressants, etc.). The marine environment is another well-established source of bioactive natural products, with recent applications against parasites, bacteria and other pathogens which affect humans and animals. Drug discovery techniques have rapidly advanced since the beginning of the millennium. The combination of novel techniques that include the genetic modification of pathogens, bioimaging and robotics has given rise to the standardization of High-Performance Screening platforms in the discovery of drugs. These advancements have accelerated the discovery of new chemical entities with antiparasitic effects. This review presents critical updates regarding the use of High-Throughput Screening (HTS) in the discovery of drugs for NTDs transmitted by protozoa, including malaria, and its application in the discovery of new drugs of marine origin.

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“…In addition, other sources should also be examined to look for novel, effective leishmanicidal agents. For instance, marine organisms have been considered as promising suppliers of compounds with novel structures and noteworthy antiparasitic activity [40][41][42], including antileishmanial properties [43][44][45]. In this sense, it may be worthwhile considering marine specimens in future studies, especially marine microorganisms, whose chemical composition and biological activity-to our knowledge-remain to be deeply explored.…”

Section: General Findingsmentioning

confidence: 99%

Colombian Contributions Fighting Leishmaniasis: A Systematic Review on Antileishmanials Combined with Chemoinformatics Analysis

2020

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Leishmaniasis is a parasitic morbid/fatal disease caused by Leishmania protozoa. Twelve million people worldwide are appraised to be currently infected, including ca. two million infections each year, and 350 million people in 88 countries are at risk of becoming infected. In Colombia, cutaneous leishmaniasis (CL) is a public health problem in some tropical areas. Therapeutics is based on traditional antileishmanial drugs, but this practice has several drawbacks for patients. Thus, the search for new antileishmanial agents is a serious need, but the lack of adequately funded research programs on drug discovery has hampered its progress. Some Colombian researchers have conducted different research projects focused on the assessment of the antileishmanial activity of naturally occurring and synthetic compounds against promastigotes and/or amastigotes. Results of such studies have separately demonstrated important hits and reasonable potential, but a holistic view of them is lacking. Hence, we present the outcome from a systematic review of the literature (under PRISMA guidelines) on those Colombian studies investigating antileishmanials during the last thirty-two years. In order to combine the general efforts aiming at finding a lead against Leishmania panamensis (one of the most studied and incident parasites in Colombia causing CL) and to recognize structural features of representative compounds, fingerprint-based analyses using conventional machine learning algorithms and clustering methods are shown. Abstraction from such a meta-description led to describe some function-determining molecular features and simplify the clustering of plausible isofunctional hits. This systematic review indicated that the Colombian efforts for the antileishmanials discovery are increasingly intensified, though improvements in the followed pathways must be definitively pursued. In this context, a brief discussion about scope, strengths and limitations of such advances and relationships is addressed.

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Marine Algae as Source of Novel Antileishmanial Drugs: A Review

Cited by 30 publications

References 75 publications

Spongian Diterpenoids Derived from the Antarctic Sponge Dendrilla antarctica Are Potent Inhibitors of the Leishmania Parasite

Spongian Diterpenoids Derived from the Antarctic Sponge Dendrilla antarctica Are Potent Inhibitors of the Leishmania Parasite

Screening Marine Natural Products for New Drug Leads against Trypanosomatids and Malaria

Colombian Contributions Fighting Leishmaniasis: A Systematic Review on Antileishmanials Combined with Chemoinformatics Analysis

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