scholarly journals General Toxicity screening of Royleanone derivatives using an Artemia salina model

2021 ◽  
Vol 18 (1) ◽  
pp. 114
Author(s):  
Epole Ntungwe ◽  
Vera M. S. Isca ◽  
Ana María Díaz-Lanza ◽  
Carlos A. M. Afonso ◽  
Patrícia Rijo

Cancer is the second leading cause of death globally. World Health Organization recorded an estimated 9.6 million deaths attributed to cancer in 2018. There is an urgent need for new anticancer drugs with novel modes of action. Natural products remain a valuable source for the identification and development of novel treatment options for cancer. Plectranthus species are well-known medicinal species used extensively for the treatment of different illnesses. These species are rich in diterpenoids which are reported to be responsible for various pharmacological activities including cytotoxic activities. Brine shrimp (Artemia salina) is broadly used in lethality studies and this model is a convenient starting point for cytotoxicity study when screening for general toxicity of natural products. This assay is based on their ability to kill a laboratory cultured nauplii. In this work, we report the general toxicity of some derivatives from 6,7-dehydroroyleanone (1) and 7α-acetoxy-6β-hydroxyroyleanone (2) compounds. The A. salina bioassay is a simple, rapid, and low-cost test, and is very useful for preliminary assessment of general toxicity in natural products thereby guiding the determination of possible biological activities.

2019 ◽  
Vol 18 (4) ◽  
pp. 406-412
Author(s):  
Hoang Kim Chi ◽  
Tran Thi Hong Ha ◽  
Le Huu Cuong ◽  
Tran Thi Nhu Hang ◽  
Nguyen Dinh Tuan ◽  
...  

In the context of sources for natural products discovery are going scarcer, exploiting biotechnologically potential compounds from marine microbial symbionts is considered a relatively new trend. In our study a total of fifteen fungal strains were isolated from marine algal samples belonging to species Kappaphycus cottonii, K. striatus, Gracilaria eucheumatoides and Betaphycus gelatinus collected in Nha Trang in 2017. The in vitro biological activities, including antimicrobial, cytotoxic and hemolytic activities of ethyl acetate extracts of the fungal strains were determined. From fifteen fungal extracts, six displayed antimicrobial activity against at least one test strain. At 20 μg.ml-1, four fungal extracts were found to express cytotoxic activity on two human cancer cell lines hepatocellular carcinoma (Hep-G2) and breast adenocarcinoma (MCF-7), with G. eucheumatoides being the source of the highest number of producer strains. Hemolytic activity was observed in rabbit erythrocytes under almost all fungal extracts’ effect. No apparent relationship was observed between the biological activities of fungal isolates. The biological assessments uncovered several fungal candidates, such as Bge-1.1, Kco-2.1 and Geu-1.1 with relatively potent antimicrobial and cytotoxic activities while expressing less hemolytic effect at concentrations from 20 μg.ml-1 to 200 μg.ml-1. The results evidenced the potential of exploiting natural products from associated marine microorganisms, especially those for the purpose of pharmaceutical applications.


2014 ◽  
Vol 60 (01) ◽  
pp. 9-18 ◽  
Author(s):  
Mentor R. Hamidi ◽  
Blagica Jovanova ◽  
Tatjana Kadifkova Panovska

Many natural products could serve as the starting point in the development of modern medicines because of their numerous biological and pharmacological activities. However, some of them are known to carry toxicological properties as well. In order to achieve a safe treatment with plant products, numerous research studies have recently been focused on both pharmacology and toxicity of medicinal plants. Moreover, these studies employed efforts for alternative biological assays. Brine Shrimp Lethality Assay is the most convenient system for monitoring biological activities of various plant species. This method is very useful for preliminary assessment of toxicity of the plant extracts. Rapidness, simplicity and low requirements are several advantages of this assay. However, several conditions need to be completed, especially in the means of standardized experimental conditions (temperature, pH of the medium, salinity, aeration and light). The toxicity of herbal extracts using this assay has been determined in a concentration range of 10, 100 and 1000 µg/ml of the examined herbal extract. Most toxicity studies which use the Brine Shrimp Lethality Assay determine the toxicity after 24 hours of exposure to the tested sample. The median lethal concentration (LC50) of the test samples is obtained by a plot of percentage of the dead shrimps against the logarithm of the sample concentration. LC50 values are estimated using a probit regression analysis and compared with either Meyer’s or Clarkson’s toxicity criteria. Furthermore, the positive correlation between Meyer’s toxicity scale for Artemia salina and Gosselin, Smith and Hodge’s toxicity scale for higher animal models confirmed that the Brine Shrimp Lethality Assay is an excellent predictive tool for the toxic potential of plant extracts in humans.


2020 ◽  
Vol 23 (9) ◽  
pp. 862-876
Author(s):  
Hayrettin O. Gulcan ◽  
Ilkay E. Orhan

With respect to the unknowns of pathophysiology of Alzheimer’s Disease (AD)-, and Parkinson’s Disease (PD)-like neurodegenerative disorders, natural product research is still one of the valid tools in order to provide alternative and/or better treatment options. At one hand, various extracts of herbals provide a combination of actions targeting multiple receptors, on the other hand, the discovery of active natural products (i.e., secondary metabolites) generally offers alternative chemical structures either ready to be employed in clinical studies or available to be utilized as important scaffolds for the design of novel agents. Regarding the importance of certain enzymes (e.g. cholinesterase and monoamine oxidase B), for the treatment of AD and PD, we have surveyed the natural product research within this area in the last decade. Particularly novel natural agents discovered within this period, concomitant to novel biological activities displayed for known natural products, are harmonized within the present study.


2018 ◽  
Vol 16 (1) ◽  
pp. 26-34 ◽  
Author(s):  
Sunil Kumar ◽  
Ranjana Aggarwal

Marine natural products have proven to be a rich source of drugs and drug leads. These natural products are secondary metabolites and show biological activity against bacteria, fungi and viruses. Natural products containing thiazole ring occur often in marine sources. They exhibit diverse and remarkable biological activities, including antitumor, antibacterial, anti-inflammatory and cytotoxic activities, to name a few. This review surveys the natural thiazole derivatives that have been isolated from marine microorganisms, with emphasis on biological implications in last three decades.


2019 ◽  
Vol 44 (4) ◽  
pp. 85 ◽  
Author(s):  
Paulo Roberto Barros Gomes ◽  
Marlucy Bezerra Oliveira ◽  
Dionney Andrade De Sousa ◽  
Jeremias Caetano Da Silva ◽  
Romer Pessôa Fernandes ◽  
...  

In this present work, we tested the larvicidal activity, molluscicide and toxicity of the oil extracted from Citrus limon peels, respectively against third stage larvae of Aedes aegypti, snail Biomphalaria glabrata, and Artemia salina. For this, we extract the essential oil by hydrodistillation. Then, we identified and quantified the components by gas chromatography coupled to mass spectrometry (GC-MS). We tested the larvicidal and molluscicidal activity, respectively, using the method adopted by the Brazilian Ministry of Health and the World Health Organization. We calculated the lethal concentration (LC50) from the Probit method for the three biological activities with 95 %. The results of the chromatographic analysis showed that the oil has 58.81% of Limonene (major constituent) and 0.11% α-Mulene (minority component). The essential oil presented lethal concentration (LC50) for larvicidal activity, molluscicide and toxicity, respectively at 15.48, 13.05 and 743.35 mg∙L-1. Therefore, the essential oil is active against larvae of A. aegypti and snail B. glabrata and non-toxic against larvae of A. salina.


2017 ◽  
Vol 12 (9) ◽  
pp. 1934578X1701200
Author(s):  
Abdelhak Neghra ◽  
Marylin Lecsö ◽  
Marie-José Butel ◽  
Laila S. Espindola ◽  
Brigitte Deguin ◽  
...  

Numerous natural products having a 2,2-dimethylchromene (2,2-dimethylbenzopyrane) structural element present interesting biological activities that may, therefore, be considered as privileged pharmacophore. Nine aliphatic and aromatic amides were synthesized from the 5-amino-7-methoxy-2,2-dimethyl-2 H-chromene synthon. The antibacterial, antifungal, antileishmanial and cytotoxic activities of all amidochromenes were evaluated. No antibacterial or antifungal activity was observed. Nevertheless, three aromatic amides compounds shown significant antileishmanial activity with an excellent selectivity index.


Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 314 ◽  
Author(s):  
Joana Araújo ◽  
Carla Fernandes ◽  
Madalena Pinto ◽  
Maria Tiritan

According to the World Health Organization, the exacerbated use of antibiotics worldwide is increasing multi-resistant infections, especially in the last decade. Xanthones are a class of compounds receiving great interest in drug discovery and development that can be found as natural products or obtained by synthesis. Many derivatives of xanthones are chiral and associated with relevant biological activities, including antimicrobial. The aim of this review is to compile information about chiral derivatives of xanthones from natural sources and their synthesized examples with antimicrobial activity.


2020 ◽  
pp. 20-25
Author(s):  
Denise Sackett ◽  
Tala Dajani ◽  
David Shoup ◽  
Uzoma Ikonne

The benefits of breastfeeding are well established. The World Health Organization and the Centers for Disease Control and Prevention recommend that mothers breastfeed infants for at least one year, but most children are not breastfed that long because of many factors. Breastfeeding mothers face many challenges to continued breastfeeding, including medical conditions that arise during this period, such as postpartum depression and lactational mastitis. Because of a perceived lack of consistent guidance on medication safety, it can be difficult for the family physician to treat these conditions while encouraging mothers to continue breastfeeding. The purpose of the current review is to summarize and clarify treatment options for the osteopathic family physician treating lactating mothers. We specifically focus on the pharmacological management of contraception, postpartum depression, and lactational mastitis.


2017 ◽  
Author(s):  
Mohit S. Verma ◽  
Michael J. Fink ◽  
Gabriel L Salmon ◽  
Nadine Fornelos ◽  
Takahiro E. Ohara ◽  
...  

Two biological activities of butyrate in the colon (suppression of proliferation of colonic epithelial stem cells and inflammation) correlate with inhibition of histone deacetylases. Cellular and biochemical studies of molecules similar in structure to butyrate, but different in molecular details (functional groups, chain-length, deuteration, oxidation level, fluorination, or degree of unsaturation) demonstrated that these activities were sensitive to molecular structure, and were compatible with the hypothesis that butyrate acts by binding to the Zn<sup>2+</sup> in the catalytic site of histone deacetylases. Structure-activity relationships drawn from a set of 36 compounds offer a starting point for the design of new compounds targeting the inhibition of histone deacetylases. The observation that butyrate was more potent than other short-chain fatty acids is compatible with the hypothesis that crypts evolved (at least in part), to separate stem cells at the base of crypts from butyrate produced by commensal bacteria.


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