scholarly journals Secondary metabolites of a marine-derived Penicillium ochrochloron

2021 ◽  
Vol 13 (3) ◽  
pp. 11020
Author(s):  
Peter M. EZE ◽  
Ying GAO ◽  
Yang LIU ◽  
Lasse Van GEELEN ◽  
Chika P. EJIKEUGWU ◽  
...  

Extremophilic fungi have received considerable attention recently as new promising sources of biologically active compounds with potential pharmaceutical applications. This study investigated the secondary metabolites of a marine-derived Penicillium ochrochloron isolated from underwater sea sand collected from the North Sea in St. Peter-Ording, Germany. Standard techniques were used for fungal isolation, taxonomic identification, fermentation, extraction, and isolation of fungal secondary metabolites. Chromatographic separation and spectroscopic analyses of the fungal secondary metabolites yielded eight compounds: talumarin A (1), aspergillumarin A (2), andrastin A (3), clavatol (4), 3-acetylphenol (5), methyl 2,5-dihydro-4-hydroxy-5-oxo-3-phenyl-2-furanpropanoate (6), emodin (7) and 2-chloroemodin (8). After co-cultivation with Bacillus subtilis, the fungus was induced to express (-)-striatisporolide A (9). Compound 1 was evaluated for antibacterial activity against Staphylococcus aureus, Acinetobacter baumannii, Mycobacterium smegmatis, and M. tuberculosis, as well as cytotoxicity against THP-1 cells. The compound, however, was not cytotoxic to THP-1 cells and had no antibacterial activity against the microorganisms tested. The compounds isolated from P. ochrochloron in this study are well-known compounds with a wide range of beneficial biological properties that can be explored for pharmaceutical, agricultural, or industrial applications. This study highlights the bioprospecting potential of marine fungi and confirms co-cultivation as a useful strategy for the discovery of new natural products.

2019 ◽  
Vol 3 (2) ◽  
pp. 105-111
Author(s):  
Peter M. Eze ◽  
Dominic O. Abonyi ◽  
Chika C. Abba ◽  
Peter Proksch ◽  
Festus B. C. Okoye ◽  
...  

Abstract Fungi remain a promising source of novel biologically active compounds with potentials in drug discovery and development. This study was aimed at investigating the secondary metabolites from endophytic Fusarium equiseti and Epicoccum sorghinum associated with leaves of Carica papaya collected from Agulu, Anambra State, Nigeria. Isolation of the endophytic fungi, taxonomic identification, fermentation, extraction and isolation of fungal secondary metabolites were carried out using standard procedures. Chromatographic separation and spectroscopic analyses of the fungal secondary metabolites yielded three toxigenic compounds - equisetin and its epimer 5’- epiequisetin from F. equiseti and tenuazonic acid from E. sorghinum These compounds are known to possess several beneficial biological properties that can be explored for pharmaceutical, agricultural or industrial purposes.


Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3579
Author(s):  
Svetlana A. Popova ◽  
Evgenia V. Pavlova ◽  
Oksana G. Shevchenko ◽  
Irina Yu. Chukicheva ◽  
Aleksandr V. Kutchin

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.


2007 ◽  
Vol 2 (6) ◽  
pp. 1934578X0700200 ◽  
Author(s):  
Liva Harinantenaina ◽  
Yoshinori Asakawa

The phytochemical investigation of eight Jungermaniales liverwort species: Bazzania decrescens, B. madagassa (Lepidoziaceae), Plagiochila barteri, P. terebrans (Plagiochilaceae), Isotachis aubertii (Isotachidaceae), Mastigophora diclados (Lepicoleaceae), Radula appressa (Radulaceae), and Thysananthus spathulistipus (Lejeuneaceae), collected from Madagascar, has been carried out to afford new and structurally interesting terpenoids and aromatic compounds. The biological activities of the isolated secondary metabolites were determined and the herbertene-type sesquiterpenoids were shown to have antibacterial activity. A new ent-clerodane diterpene from Thysananthus spathulistipus and bis-bibenzyls-type aromatic compounds exhibited strong inhibition of NO production in RAW 264.7 cells, while marchantin C produced moderate α-glucosidase inhibition. The chemosystematics of the studied species are discussed.


2021 ◽  
Vol 16 (3) ◽  
Author(s):  
Asifa Mushtaq ◽  
Musharaf Gul ◽  
Seema Rawat ◽  
Jay Krishan Tiwari

Actinomycetes are prolific producers of secondary metabolites majority of which have phenomenal industrial applications. Actinomycetes recovered from cave habitats have generated a considerable interest among the scientific community with respect to their adaptability under such unique environmental conditions. Garhwal Himalaya, Uttarakhand abodes several pristine caves which have not been previously explored for the presence of actinomycetes. The present study has been undertaken to assess the in vitro antibacterial properties of actinomycetes recovered from some of the caves located in Garhwal Himalayan region. In the present study, a total of 127 actinomycetes were isolated from three distinct caves. Majority of the isolates exhibited antibacterial activity against gram-positive bacteria. Actinomycetes isolates RCM1 and SCMM1 were observed to evince promising antibacterial activities. Members of Streptomyces genus were found to be predominant in all the samples.


2020 ◽  
Vol 82 (5) ◽  
pp. 3-10
Author(s):  
L.D. Varbanets ◽  
◽  
O.V. Gudzenko ◽  
V.A. Ivanytsia ◽  
◽  
...  

In recent years researchers have attracted their attention to such glycosidases as α-L-rhamnosidase (α-L-rhamnoside-rhamnohydrolase – EC 3.2.1.40). The substrates of their action are widespread in the plant world glycosides such as naringin, quercetrin, hesperidin, neohesperidin, and rutin, from which α-L-rhamnosidases cleave the terminal unreduced L-rhamnose residues. This specificity of α-L-rhamnosidases can be used in various industries: food – to improve the quality of drinks (reducing bitterness in citrus juices, enhancing the aroma of wines), as well as production of food additives; in the pharmaceutical industry – to improve the biological properties of bioflavonoids, in particular anti-inflammatory. A number of them are characterized by cardio- and radioprotective effects, have antioxidant, cytotoxic, antibacterial, antisclerotic properties, and are used in the complex treatment of coronary heart disease, including angina pectoris. The use of α-L-rhamnosidases in the chemical industry is associated with a reduction in the cost of rhamnose production as well as various plant glycosides and rutinosides. In the literature available to us, no data were found on the producers of α-L-rhamnosidases among the representatives of actinobacteria, which are known to synthesize a wide range of biologically active compounds, including antibiotics and enzymes. Purpose. To study the ability of actinobacteria isolated from water and bottom sediments of the Black Sea, to produce a-L-rhamnosidase, and also to study the properties of the most active producer. Methods. Glycosidase activity was determined by the Romero and Davis methods, protein – by the Lowry method. Results. The study of 12 glycosidase activities in 10 strains of actinobacteria isolated from bottom sediments of the Black Sea indicated that 6 investigated strains showed the ability to synthesize an enzyme with a-L-rhamnosidase and b-D-glucosidase activity. Studies have shown that the highest α-L-rhamnosidase activity (0.14 U/mg protein) was manifested by Acty 5 isolate with an optimum pH of 7.0 and a temperature optimum of 38°C. The enzyme preparation showed substrate specificity both for natural (rutin, naringin, neohesperidin) and synthetic (p-nitrophenyl derivatives of L-rhamnose and D-glucose) substrates. Conclusions. Promising Acty 5 isolate with high a-L-rhamnosidase and low b-Dglucosidase activity was found among marine actinobacteria. Bacteria with two enzymes activity expand the possibilities of their practical use.


2019 ◽  
Vol 65 (2) ◽  
pp. 99-102 ◽  
Author(s):  
Yu.V. Butina ◽  
T.V. Kudayarova ◽  
E.A. Danilova ◽  
M.K. Islyaikin

The work is devoted to predicting and studying biological properties of N-substituted analogs of 3,5-diamino-1,2,4-thiadiazole, which, in their turn, include in the composition of many drugs that exhibit a wide range of pharmacological actions. For searching of new alternative drugs with an antibacterial activity, but lacking resistance of microorganism strains to them, a computer screening of 2N-alkyl-substituted 5-amino-3-imino-1,2,4-thiadiazolines previously synthesized by us was carried out. The prediction of the spectrum of biological activity, as well as the determination of the probable toxicity of these compounds, was performed using the freely available computer programs PASS, Anti-Bac-Pred, and GUSAR. The study of the antibacterial activity in vitro against gram-positive (Staphylococcus aureus, Staphylococcus saprophyticus, Staphylococcus epidermidis) and gram-negative (Escherichia coli, Pseudomonas aeruginosae) bacterial strains was performed by the disco-diffusion method. Experimental data roughly correspond to the predictions.


2018 ◽  
Vol 15 (1) ◽  
pp. 84-104 ◽  
Author(s):  
Andre F. Constantino ◽  
Carla S. Francisco ◽  
Diana C. Cubides-Roman ◽  
Valdemar Lacerda

Background: The Hetero-Diels-Alder reaction (HDAR) is a method extensively used in organic chemistry as a tool in the synthesis of innumerous polycyclic compounds in particular nitrogen compounds, presents in many natural products, medicinally relevant substances and organic materials. The literature describes innumerable studies of HDAR using classic methods and modern developments such as reactions on the solid phase, the use of catalysts, transformations in aqueous solution and under microwaves. Objective: This review describes a variety of HDAR focused on obtaining nitrogen-containing compounds of considerable chemical and biological interest, and highlighting reported biological activity. Conclusion: This review has shown the importance of the HDA reaction as a tool of organic chemistry in the synthesis of nitrogen compounds. This type of reaction presents important properties including bond-forming economy, high regio- and stereoselectivities and thus provides highly efficient routes to access a wide range of polycyclic compounds. In addition to the variety of nitrogen compounds synthetized successfully by this method, they present relevant biological properties.


Author(s):  
Manal Selim Mohamed Selim ◽  
Sayeda Abdelrazek Abdelhamid ◽  
Sahar Saleh Mohamed

Abstract Background The ability to produce microbial bioactive compounds makes actinobacteria one of the most explored microbes among prokaryotes. The secondary metabolites of actinobacteria are known for their role in various physiological, cellular, and biological processes. Main body Actinomycetes are widely distributed in natural ecosystem habitats such as soil, rhizosphere soil, actinmycorrhizal plants, hypersaline soil, limestone, freshwater, marine, sponges, volcanic cave—hot spot, desert, air, insects gut, earthworm castings, goat feces, and endophytic actinomycetes. The most important features of microbial bioactive compounds are that they have specific microbial producers: their diverse bioactivities and their unique chemical structures. Actinomycetes represent a source of biologically active secondary metabolites like antibiotics, biopesticide agents, plant growth hormones, antitumor compounds, antiviral agents, pharmacological compounds, pigments, enzymes, enzyme inhibitors, anti-inflammatory compounds, single-cell protein feed, and biosurfactant. Short conclusions Further highlight that compounds derived from actinobacteria can be applied in a wide range of industrial applications in biomedicines and the ecological habitat is under-explored and yet to be investigated for unknown, rare actinomycetes diversity.


2020 ◽  
Vol 5 (1) ◽  
Author(s):  
Himayat Ullah ◽  
Muhammad Hubaib ◽  
Muhammad Israr ◽  
Muhammad Mushtaq ◽  
Muhammad Zeeshan ◽  
...  

Every plant available in the universe is not produced to be the part of biodiversity, but is also produced to obtain medicinal purposes. The medicinal value of the plant is due to the availability of various chemical compounds [1]. Since prehistoric time, the crude extract of plant is used to cure various diseases, although the biologically active components of the plant were unidentified [2]. In the present study the antibacterial activity is performed for various extracts of cerastium glomeratum. The plant cerastium glomeratum was collected from near kalpani river Mardan, Pakistan and was identified by lecturer Israr department of botany GPGC Mardan, Pakistan. The plant was dried under shade and grinded into powder form. The extraction process was done by using soxhlet apparatus, reflux condenser and maceration process using ethanol as a solvent. The extract was divided into different fractions of n-hexane, DCM, ethyl acetate and water. These four extracts were tested against gram positive (staphylococcus aureus) and gram negative (E.coli) bacteria using well diffusion technique. The water extract show a wide range inhibition zone against both gram positive and gram negative bacteria while n-hexane, DCM and ethyl acetate fractions show no zone of inhibition against bacteria. In effort to find new antibacterial compounds cerastium glomeratum seems to be a good plant for additional phytochemical studies.


2021 ◽  
Author(s):  
Lali Tabatadze ◽  
Neli Sidamonidze ◽  
Darejan Gulbani ◽  
Darejan Iremashvili

Carbohydrate derivatives are distinguished with wide range of biological activity which is proven by successful usage of preparations made of Carbohydrate based in different branches of pharmaceutical chemistry. As a result of research of Carbohydrate compounde, the relationship between unique structure and its chemical and biological properties has been studied. Input of bulk liphophilic adamantine moiety in the proved medications or biologically active molecule in most cases is improved molecule’s biological characteristic, drug’s lipopilycity and prolonged actin is enhanced, and at the same time toxicity and side negative effects is reduced.We studied the reactions of acetylaryl glycosides with phenylsulfonyl chloride in the presence of a benzoyl peroxide catalyst. A new sulfur-containing glucoside was synthesized: Hepta-O-acetyl-1-O-(2-chloro-3-phenyl thio propyl)-β-D-maltose. The bactericidal properties of β-O-(2-chloro-3-phenyl thio propyl)-D-maltose of the obtained product after deacetylation were studied. With the help of the com­­pu­ter program PASS (Prediction of Activity Spectra for Substance) onlaines were able to predict the range of activity of substances. The obtained result established correlations on bactericidal properties between biological activity and the intended biological activity. The structure of the synthesized compounds was determined by physico-chemical research methods.


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