Preliminary investigation of the chemo diversity of bioactive molecules produced by endophytic fungi isolated from Manihot utilisima leaf

Endophytic fungi have demonstrated a harmless relationship living within the internal tissues of several plant hosts and at the same time produce diverse important bioactive compounds having a wide range of pharmaceutical applicability. In this study, nine endophytic fungi, eight from Cassava leaf: Clg1, Clg2, Clr4, Clr5, Clr6, Clr7, Clr9 and one from Cassava mid-rib: CRs3 with distinct cultural features were isolated from healthy leaves of Manihot utilisima and axenic cultures were fermented on sterile rice medium for 21 days. The antimicrobial and antioxidant activities of the fungal crude extracts were evaluated. Chemical analyses of the metabolic profiles of each fungal extract revealed the presence of nine known compounds with established biological activities. Each fungal extract exhibited antimicrobial activities against at least one Gram positive and Gram negative bacteria with an inhibition zone that ranged from 2 – 6 mm. Clg2 and CRs3 fungal extracts demonstrated moderate potential to scavenge free radical with an inhibition of 58 and 60% respectively. Septicine, cyclo(prolylvalyl), pentenedioc acid, neurolenin B, rubrofusarin, p-Hydroxybenzoic acid, protocatechuic acid, citreoisocoumarin, palitantin and pestalio pyrone were the compounds detected in the fungal fermentation products. Our findings reveal that M. utilisima leaves harbor endophytic fungi with unique chemodiversity of bioactive secondary metabolites needed for development of new drugs.

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Antibacterial and antioxidant activities of endophytic fungi and nettle (Urtica dioica L.) leaves as their host

Cellular and Molecular Biology ◽

10.14715/cmb/2021.67.3.33 ◽

2021 ◽

Vol 67 (3) ◽

pp. 204-211

Author(s):

Djouza Salmi ◽

Catherine Riou ◽

Mohammad Issawi ◽

Yacine Titouche ◽

Veronica Ambrosini ◽

...

Keyword(s):

Endophytic Fungi ◽

Antioxidant Activities ◽

Radical Scavenging ◽

Antimicrobial Activities ◽

Urtica Dioica ◽

Biologically Active ◽

Bioactive Metabolites ◽

Wide Range ◽

Thiol Content ◽

Pharmaceutical Industries

Nettle (Urtica dioica L), as a plant rich in biologically active compounds, is one of the most important plants used in herbal medicine. Studies have shown that this plant has antioxidant, antiplatelet, hypoglycemic and hypocholesterolemia effects. In this study, we characterized three Alternaria endophytic fungi isolated from their host U. dioica. We hypothesized that these endophytic fungi can produce new bioactive metabolites, which may possess the bioactive property with potential application in the medical and pharmaceutical industries. The antibacterial activity was evaluated against reference and isolated strains, including Methicillin-Resistant Staphylococcus aureus. A wide range of antimicrobial activities similar to those measured in nettle leaves was detected especially for Alternaria sorghi. Furthermore, the highest antioxidant activity detected with DPPH free radical scavenging was measured for A. sorghi and nettle leaves ethyl acetate extracts. In addition, whereas catalase activity was similar in the three isolated fungi and nettle leaves, total thiol content and superoxide dismutase activity were significantly higher in leaves. A. sorghi showed the best activities compared to other isolated fungi. The characterization and further production of bioactive compounds produced by this endophyte should be investigated to fight bacteria and especially those that develop drug multi-resistance.

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Advances in Triazole Synthesis from Copper-catalyzed Azide-alkyne Cycloadditions (CuAAC) Based on Eco-friendly Procedures

Current Organic Synthesis ◽

10.2174/1570179416666190104141454 ◽

2019 ◽

Vol 16 (2) ◽

pp. 244-257 ◽

Cited By ~ 2

Author(s):

Marcus Vinicius Nora de Souza ◽

Cristiane França da Costa ◽

Victor Facchinetti ◽

Claudia Regina Brandão Gomes ◽

Paula Mázala Pacheco

Keyword(s):

Biological Activities ◽

Reaction Times ◽

Water Extract ◽

Fish Bone ◽

New Drugs ◽

Bone Powder ◽

Wide Range ◽

Recoverable Catalysts ◽

Egg Shell ◽

Work Up

Background: 1,2,3-triazoles are an important class of organic compounds and because of their aromatic stability, they are not easily reduced, oxidized or hydrolyzed in acidic and basic environments. Moreover, 1,2,3-triazole derivatives are known by their important biological activities and have drawn considerable attention due to their variety of properties. The synthesis of this nucleus, based on the click chemistry concept, through the 1,3-dipolar addition reaction between azides and alkynes is a well-known procedure. This reaction has a wide range of applications, especially on the development of new drugs. Methods: The most prominent eco-friendly methods for the synthesis of triazoles under microwave irradiation published in articles from 2012-2018 were reviewed. Results: In this review, we cover some of the recent eco-friendly CuAAC procedures for the click synthesis of 1,2,3-triazoles with remarks to new and easily recoverable catalysts, such as rhizobial cyclic β-1,2 glucan; WEB (water extract of banana); biosourced cyclosophoraose (CyS); egg shell powder (ESP); cyclodextrin (β- CD); fish bone powder; nanoparticle-based catalyst, among others. Conclusion: These eco-friendly procedures are a useful tool for the synthesis of 1,2,3-triazoles, providing many advantages on the synthesis of this class, such as shorter reaction times, easier work-up and higher yields when compared to classical procedures. Moreover, these methodologies can be applied to the industrial synthesis of drugs and to other areas.

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

Chemistry, Technology and Application of Substances ◽

10.23939/ctas2021.02.047 ◽

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.

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Steroidal pyrazolines as a promising scaffold in drug discovery

Future Medicinal Chemistry ◽

10.4155/fmc-2019-0325 ◽

2020 ◽

Vol 12 (10) ◽

pp. 949-959

Author(s):

Ranju Bansal ◽

Ranjit Singh

Keyword(s):

Drug Discovery ◽

Broad Spectrum ◽

Chemical Reactivity ◽

Biological Activities ◽

Antimicrobial Activities ◽

Review Article ◽

Pharmacological Activities ◽

Neuroprotective Effects ◽

Wide Range

Steroidal pyrazolines constitute an interesting and promising scaffold for drug discovery as they display diverse chemical reactivity and a wide range of biological activities. Literature reports indicate potent anticancer potential of steroidal pyrazolines along with broad-spectrum antimicrobial activities. Strong neuroprotective effects with steroids possessing pyrazoline moiety have also been observed. Among all the therapeutically active steroidal pyrazolines, D-ring-substituted derivatives are highly potent and the least toxic. The current and futuristic research approaches in this area are focused towards the exploration of this promising scaffold to develop molecules with widespread pharmacological activities. This review article mainly covers the synthetic and pharmacological aspects of steroidal pyrazolines, which will assist the medicinal chemists working in this area in their scientific endeavors.

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Nutraceutical Activity in Osteoarthritis Biology: A Focus on the Nutrigenomic Role

Cells ◽

10.3390/cells9051232 ◽

2020 ◽

Vol 9 (5) ◽

pp. 1232

Author(s):

Stefania D’Adamo ◽

Silvia Cetrullo ◽

Veronica Panichi ◽

Erminia Mariani ◽

Flavio Flamigni ◽

...

Keyword(s):

Signaling Pathways ◽

Antioxidant Activities ◽

Synergistic Effects ◽

National Health System ◽

Bioactive Molecules ◽

Joint Disease ◽

In Vivo Studies ◽

Wide Range

Osteoarthritis (OA) is a disease associated to age or conditions that precipitate aging of articular cartilage, a post-mitotic tissue that remains functional until the failure of major homeostatic mechanisms. OA severely impacts the national health system costs and patients’ quality of life because of pain and disability. It is a whole-joint disease sustained by inflammatory and oxidative signaling pathways and marked epigenetic changes responsible for catabolism of the cartilage extracellular matrix. OA usually progresses until its severity requires joint arthroplasty. To delay this progression and to improve symptoms, a wide range of naturally derived compounds have been proposed and are summarized in this review. Preclinical in vitro and in vivo studies have provided proof of principle that many of these nutraceuticals are able to exert pleiotropic and synergistic effects and effectively counteract OA pathogenesis by exerting both anti-inflammatory and antioxidant activities and by tuning major OA-related signaling pathways. The latter are the basis for the nutrigenomic role played by some of these compounds, given the marked changes in the transcriptome, miRNome, and methylome. Ongoing and future clinical trials will hopefully confirm the disease-modifying ability of these bioactive molecules in OA patients.

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Compositions and Biological Activities of Essential Oils of Kadsura longepedunculata and Schisandra sphenanthera

The American Journal of Chinese Medicine ◽

10.1142/s0192415x07004874 ◽

2007 ◽

Vol 35 (02) ◽

pp. 353-364 ◽

Cited By ~ 13

Author(s):

Lei Song ◽

Jie-Ying Ding ◽

Cui Tang ◽

Chun-Hua Yin

Keyword(s):

Essential Oils ◽

Antioxidant Activities ◽

Biological Activities ◽

Liver Homogenate ◽

Reducing Power ◽

Antimicrobial Activities ◽

Dilution Method ◽

Chemical Compositions ◽

Dependent Manner ◽

Schisandra Sphenanthera

The chemical compositions, antimicrobial activities, antioxidant activities and cytotoxicities of the essential oils isolated from the root of Kadsura longepedunculata Finet et Gagnep (KLREO) and the fruit of Schisandra sphenanthera Rehd. et Wills. (SSFEO) were investigated.The analyses of gas chromatography-mass spectrometry (GC-MS) showed that cadinane type compounds and their derivatives were rich in both oils (54.2% and 39.7%, respectively) and δ-cadinene was the major component of both oils (13.8% and 25.6%, respectively). The antimicrobial activities of both oils were evaluated against five microorganisms with the disc diffusion and the broth micro-dilution method. Results showed that Gram-positive bacteria were more sensitive to both oils than Gram-negative bacteria and the yeast. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the oil of KLREO were lower than those of SSFEO, indicating that the former possessed slightly stronger antibacterial capability than the latter. The reducing power and lipid peroxidation assays were employed to study the potential antioxidant activities of both oils. Both oils remarkably decreased the content of malondialdehyde (MDA) in rat liver homogenate in a dose dependent manner. The antioxidant activities of KLREO appeared to be more potent than that of SSFEO. The oils of KLREO and SSFEO exhibited concentration-dependent cytotoxicities and were proved to be toxic to HepG2 cells with IC50 of 147 and 189 μg/ml, respectively.

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Diversity and Biological Activities of Endophytic Fungi at Al-Qassim Region

Journal of Molecular Biology Research ◽

10.5539/jmbr.v9n1p160 ◽

2019 ◽

Vol 9 (1) ◽

pp. 160

Author(s):

Nahla Tharwat Elazab

Keyword(s):

Endophytic Fungi ◽

Extracellular Enzymes ◽

Biological Activities ◽

Trichoderma Viride ◽

Pathogenic Fungi ◽

Phytopathogenic Fungi ◽

Antagonistic Effect ◽

Wild Plants ◽

Dual Culture ◽

Wide Range

In recent year’s endophytic fungi has become a major concern on their host plants by enhancing their growth, increasing their fitness, strengthening their tolerances to abiotic and biotic stresses, and promoting their accumulation of secondary metabolites. Kingdom of Saudi Arabia has a wide range of flora which may be a rich source of endophytic fungi so that, the present study involves diversity and bioactivity of the endophytic fungal community in Al-Qassim region from 15 wild plants 162 isolates were obtained and identified. Among them, the most common isolates were Aspergillus niger, Aspergillus terreus, Aspergillus ochraceous and Trichoderma viride, these four endophytic isolates were examined for its antagonistic effect against six phytopathogenic fungi using two different assays, Dual-culture and Culture filtrate. Trichoderma viride recorded the most significant growth inhibition of almost pathogenic fungi followed by the three endophytic Aspergillus spp. In addition, these four endophytic fungi were screened for the production of some extracellular enzymes such as protease, cellulose, amylase, pectinase and xylanase. Our results show the ability of these isolates to produce these extracellular enzymes so this indicated the possible role of endophytic fungi as a biocontrol agent of plant disease.

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LC-MS Based Analysis and Biological Properties of Pseudocedrela kotschyi (Schweinf.) Harms Extracts: A Valuable Source of Antioxidant, Antifungal, and Antibacterial Compounds

Antioxidants ◽

10.3390/antiox10101570 ◽

2021 ◽

Vol 10 (10) ◽

pp. 1570

Author(s):

Kouadio Ibrahime Sinan ◽

Stefano Dall’Acqua ◽

Irene Ferrarese ◽

Adriano Mollica ◽

Azzurra Stefanucci ◽

...

Keyword(s):

Antioxidant Activities ◽

Stem Bark ◽

Antimicrobial Activities ◽

Biological Properties ◽

Bioactive Molecules ◽

Total Phenolic ◽

E Coli ◽

Methanolic Extracts ◽

Therapeutic Value ◽

The Impact

The impact of two extraction solvents on the phenolic composition, antioxidant, and enzymes inhibitory and antimicrobial activities of two parts (leaves and stem bark) of P. kotschyi was studied. Two different LC-DAD-MSn approaches were used to identify and quantify the bioactive compounds in the different extracts. A total of thirty-two compounds were quantified, being the procyanidin the most abundant in stem bark while catechin and flavonoids are most abundant in leaves. Overall, the stem bark extraction using methanol showed higher amounts of total phenolic (131.83 ± 1.81 mg GAE/g) and flavanol (14.14 ± 0.11 mg CE/g) while the leaves extraction using water exhibited stronger levels of total flavonoid (44.95 ± 0.38 mg RE/g) and phenolic acid (63.58 ± 2.00 mg CAE/g). As regards the antioxidant assays, methanol stem bark extracts were characterized by the highest antioxidant activities (DPPH: 1.94 ± 0.01 mmol TE/g, ABTS: 3.31 ± 0.01 mmol TE/g, FRAP: 2.86 ± 0.02 mmol TE/g, CUPRAC: 5.09 ± 0.08 mmol TE/g, phosphomolybdenum: 5.16 ± 0.23 mmol TE/g and metal chelating: 17.12 ± 0.46 mg EDTAE/g). In addition, the methanolic extracts of stem bark had highest impact on acetylcholinesterase (2.54 mg GALAE/g), butyrylcholinesterase (5.48 mg GALAE/g). In contrast, the methanolic extracts of leaves was potent against tyrosinase (77.39 ± 0.21 mg KAE/g) and α-glucosidase (0.97 ± 0.01 mmol ACAE/g), while a higher anti-α–amylase (0.97 ± 0.01 mmol ACAE/g) was observed for water extracts of the same part. All of the tested extracts showed inhibitory effects on elastase, except methanolic leaves extracts. Additionally, the extracts exhibited appreciable antifungal toward A. ochraceus, A. fumigatus, P. ochrochloron, T. viride, and P. funiculosum and promising antibacterial activity against M. flavus, S. aureus, L. monocytogenes, E. coli, P. aeruginosa, E. cloacae, and S. typhimurium. Taken together, the outcomes demonstrated P. kotschyi as a novel source of bioactive molecules of interest with an evident therapeutic value.

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PHYTOCHEMICAL SCREENING, ANTIOXIDANT AND ANTIMICROBIAL ASSESSMENT OF PLUCHEA INDICA (L.) LESS EXTRACT AS AN ACTIVE INGREDIENT IN NATURAL LOTION BAR

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2021v13i2.41555 ◽

2021 ◽

pp. 51-57

Author(s):

SIRIKHWAN TINRAT

Keyword(s):

Broad Spectrum ◽

Antioxidant Activities ◽

Biological Activities ◽

Radical Scavenging ◽

Ethanolic Extract ◽

Antimicrobial Activities ◽

Dilution Method ◽

Reducing Ability ◽

Phytochemical Compounds ◽

Antioxidant And Antimicrobial Activities

Objective: To screen phytochemical compounds and study antioxidant and antimicrobial activities of Pluchea indica (L.) Less (PI) leaves extracts for assessment the moisturizing lotion bar formulation containing it’s as a bioactive ingredient. Methods: PI leaves were extracted in different solvents. Crude extracts were screened phytochemical compounds and evaluated antioxidant and antimicrobial activities before formulating to antibacterial moisturizing lotion bar. Results: 95% ethanolic extract displayed high antioxidant activities. DPPH radical scavenging capacity with IC50 was 6.80±0.04 mg/ml (61.37±0.41%) and the ferric reducing ability power was 381.20±0.10 mg AAE/100 gDW. Additionally, 95% ethanolic extract served as a broad spectrum bacteriostatic agents against gram-positive and gram-negative species with an inhibition zone of 6.50±0.00-46.67±0.58 mm. It also was simultaneously as a broad spectrum bactericidal agents (MIC and MBC value of 25-200 mg/ml) by broth micro-dilution method. The screened phytochemical constituents (saponins, tannins, flavonoids, terpenoids, steroids, and alkaloids) in PI leaves extract may be responsible for high biological activities. Thus, 95% ethanolic extract was the most appropriate bioactive ingredient for formulated the product development. Conclusion: The developed moisturizing lotion bar with 0.0041% of 95% ethanolic extract was the most eligible formula that showed good appearance, odor, color, homogeneity, after feel and stability. This extract-containing lotion bar formulation achieved a high level of customer satisfaction by sensory evaluation and development of this specific formulation should be subject to further clinical investigation.

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Synthesis, Characterization and Study of Antimicrobial Activities of Mannich Bases Incorporating 1,2,4-Triazole Nucleus

Amrit Research Journal ◽

10.3126/arj.v2i01.39894 ◽

2021 ◽

Vol 2 (01) ◽

pp. 19-27

Author(s):

Rhambus Rawat ◽

Prem Shankar Deo ◽

Bhushan Shakya

Keyword(s):

Schiff Base ◽

Heterocyclic Compounds ◽

Environmental Science ◽

Biological Activities ◽

Antimicrobial Activities ◽

Mannich Bases ◽

New Drugs ◽

Spectroscopic Techniques ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal

Heterocyclic compounds containing triazole moiety have great importance in the field of medicine, pharmaceuticals, biochemistry, biology, therapeutics, environmental science, and industry. Triazoles and their derivatives have been extensively used in the development of new drugs. Biological activities of Schiff bases are highly investigated, but Mannich bases are on the verge of their development, and they are being synthesized in large number nowadays. In this work, Mannich bases are synthesized by incorporation 1,2,4-triazole moiety through Schiff base using different amines. Mannich bases are found to exhibit highly effective antibacterial and antifungal activities. The formation of synthesized compounds - 1,2,4-triazole-5-thione, Schiff base (4) and Mannich bases (5a and 5b) - are confirmed and characterized by spectroscopic techniques like UV, FTIR 1H-NMR and 13C-NMR. The activity of the synthesized compounds was tested against bacterial and fungal strain.

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