scholarly journals In Vitro Antibacterial and Antifungal Potential of Amyrin-Type Triterpenoid Isolated from Datura metel Linnaeus

2021 ◽  
Vol 2021 ◽  
pp. 1-5
Author(s):  
Sami Bawazeer ◽  
Abdur Rauf

The aim of the present investigation was to evaluate the effect of the combined crude extract, fractions, and compound 1 isolated from the fruits of Datura metel against selected microbial (bacteria and fungi) strains. Results of antibacterial screening indicated marked susceptibility of the extract and its fractions against tested bacterial strains. Among the extract and various fractions, the chloroform fraction exhibited a significant effect against different bacterial strains including Escherichia coli, Staphylococcus aureus, and Bacillus subtilis with an inhibitory zone ranging from 18 to 24 mm. Similarly, results of antifungal activity revealed that the chloroform fraction displays a promising effect against various fungal strains. The chloroform fraction was subjected to repeated chromatography analysis, which yielded compound 1 (daturaolone). Daturaolone exhibited potent activity against selected bacterial strains including Klebsiella pneumoniae, B. subtilis, S. epidermidis, and S. aureus with an inhibitory zone ranging from 12 to 30 mm. In addition, the extracts and daturaolone exhibited significant sensitivity against T. longifusus, C. albicans, A. flavus, M. canis, F. solani, and C. glabrata. Taken all together, it is concluded that our findings validated the traditional use of D. metel to treat various infectious diseases, which is supported by daturaolone.

2020 ◽  
Vol 1 (3) ◽  
pp. 116-125
Author(s):  
Hadis Tavafi ◽  
Maryam- sadat Sadrzadeh-Afshar ◽  
Soroush Niroomand

Periodontal disease is one of the most prevalent infectious oral conditions in the present century, and it is necessary to conduct research to find a solution to overcome these diseases. A variety of microbial strains of bacteria and fungi are involved in the pathogenesis of periodontal disease. The use of chemical agents such as mouthwashes is one of the strategies to control these diseases. The purpose of the present study was to compare the antimicrobial effects of propolis and chlorhexidine gluconate (CHX) on the bacterial strains of Streptococcus mutans, Streptococcus pyogenes, Staphylococcus aureus, Enterococcus faecalis, Pseudomonas aeruginosa, and the yeast strain of Candida albicans using the broth microdilution method. The results showed the inhibitory and microbicidal activities of the two substances against the tested microbial strains. The antibacterial and antifungal effects of CHX were more effective reported in this study than that of propolis against the studied pathogens. The results of this study also indicated that the propolis was less effective in inhibiting bacterial growth than the CHX. In addition, the combination of these two solutions had a synergistic effect on inhibition of other studied strains, with the exception of C. albicans and S. aureus. There is a need for further research on strains isolated from oral biofilm to achieve complementary results.


2020 ◽  
Vol 13 (4) ◽  
pp. 2003-2014
Author(s):  
Arun Kumar ◽  
Yashika Garg

Background:Calophylluminophyllum is an evergreen tree with ethno-medical value growing along the seashores and islands of the Pacific and Indian Ocean. All parts of the plant such as bark, seeds and leaves have diverse medicinal uses such as an antiseptic, analgesic in wound healing, astringent, diuretic, purgative and expectorant. Although many species of calophyllum have been studied phytochemically for pharmacological properties, reports on inophyllum species are scanty. Aim of the study:Keeping inview it’s medical importance and availability in India as well as the rapid development of resistance by pathogens to the commonly used synthetic antibiotics,the pharmacological effects of C. inophyllum leaf extract (CIE) on HIV, bacteria and fungi causative of many human diseases was assessed in this study. Material and Methods: Isolation of the pure compounds from the ethanolic CIE was performed by gross column chromatography and tested against lyophilized forms of 8 fungal and 14 bacterial strains grown on Sabouraud’s dextrose agar and nutrient agar media respectively. Fractions and pure compounds isolated from CIE were evaluated against HIV by the HIV-RT inhibition assay by using the RT assay kit(Roche). The results were tabulated and analysed. Results: Among the purified compounds, Inophyllum C & E exhibited significant antibacterial and antifungal properties. Moreover, Inophyllum E was more potent than Inophyllum C in inhibiting the tested strains of bacteria and fungi whereasInophyllum B shows highest antiretroviral activity. Conclusion:We conclude that CIEis aneffective antimicrobial agent against common human pathogens tested in this in-vitro pharmacological evaluation of CIE.


2019 ◽  
Vol 16 (3) ◽  
pp. 245-248
Author(s):  
Hummera Rafique ◽  
Aamer Saeed ◽  
Ehsan Ullah Mughal ◽  
Muhammad Naveed Zafar ◽  
Amara Mumtaz ◽  
...  

Background: (±)-6,8-Dihydroxy-3-undecyl-3,4-dihydroisochromen-1-one is one of the structural analog of several substituted undecylisocoumarins isolated from Ononis natrix (Fabaceae), has been successfully synthesized by direct condensation of homopthalic acid (1) with undecanoyl chloride yields isochromen-1-one (2). Methods: Alkaline hydrolysis of (2) gave the corresponding keto-acid (3), which is then reduced to hydroxy acid (4) then its cyclodehydration was carried out with acetic anhydride to afford 3,4- dihydroisochromen-1-one (5). Followed by demethylation step, the synthesis of target 6,8- dihydroxy-7-methyl-3-undecyl-3,4-dihydroisocoumarin (6) was achieved. Results: In vitro antibacterial screening of all the synthesized compounds were carried out against ten bacterial strains by agar well diffusion method. Conclusion: Newly synthesized molecules exhibited moderate antibacterial activity and maximum inhibition was observed against Bacillus subtilus and Salmonella paratyphi.


2016 ◽  
Vol 11 (2) ◽  
pp. 248 ◽  
Author(s):  
Kathirvel Poonkodi ◽  
Subban Ravi

<p class="Abstract">The present study was aimed to evaluate the phytochemical screening and antimicrobial activity of the petroleum ether and methanol extracts from the mature leaves of <em>Richardia scabra</em> from India. Disc diffusion method was used to determine the zone inhibition of the tested samples for antibacterial and agar plug method was used to determine the antifungal activity, while the microtube-dilution technique was used to determine the minimum inhibitory concentration. Both extracts showed significant antibacterial and antifungal activities when tested against 10 bacterial and four fungal strains. The minimum inhibitory concentrations of the methanol extract of<em> R. scabra</em> ranged between 12.5–100 μg/mL for bacterial strains. Alkaloids, steroids, flavonoids, fatty acids, terpenoids and simple sugar were detected as phytoconstituents of extracts. To the best of our knowledge, this is the first report against antimicrobial activity of common weed species <em>R. scabra</em> found in India.</p><p> </p>


2010 ◽  
Vol 76 (15) ◽  
pp. 4969-4976 ◽  
Author(s):  
Kerstin Engelhardt ◽  
Kristin F. Degnes ◽  
Michael Kemmler ◽  
Harald Bredholt ◽  
Espen Fj�rvik ◽  
...  

ABSTRACT Twenty-seven marine sediment- and sponge-derived actinomycetes with a preference for or dependence on seawater for growth were classified at the genus level using molecular taxonomy. Their potential to produce bioactive secondary metabolites was analyzed by PCR screening for genes involved in polyketide and nonribosomal peptide antibiotic synthesis. Using microwell cultures, conditions for the production of antibacterial and antifungal compounds were identified for 15 of the 27 isolates subjected to this screening. Nine of the 15 active extracts were also active against multiresistant Gram-positive bacterial and/or fungal indicator organisms, including vancomycin-resistant Enterococcus faecium and multidrug-resistant Candida albicans. Activity-guided fractionation of fermentation extracts of isolate TFS65-07, showing strong antibacterial activity and classified as a Nocardiopsis species, allowed the identification and purification of the active compound. Structure elucidation revealed this compound to be a new thiopeptide antibiotic with a rare aminoacetone moiety. The in vitro antibacterial activity of this thiopeptide, designated TP-1161, against a panel of bacterial strains was determined.


2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Sonja Ž. Đurić ◽  
Sandra Vojnovic ◽  
Tina P. Andrejević ◽  
Nevena Lj Stevanović ◽  
Nada D. Savić ◽  
...  

1,2-Bis(4-pyridyl)ethane (bpa) and 1,2-bis(4-pyridyl)ethene (bpe) were used for the synthesis of polynuclear silver(I) complexes, {[Ag(bpa)]NO3}n (1), {[Ag(bpa)2]CF3SO3.H2O}n (2) and {[Ag(bpe)]CF3SO3}n (3). In complexes 1–3, the corresponding nitrogen-containing heterocycle acts as a bridging ligand between two Ag(I) ions. In vitro antimicrobial activity of these complexes, along with the ligands used for their synthesis, was evaluated against the broad panel of Gram-positive and Gram-negative bacteria and fungi. The silver(I) complexes 1–3 showed selectivity towards Candida spp. and Gram-negative Escherichia coli in comparison to the other investigated bacterial strains, effectively inhibiting the growth of four different Candida species with minimal inhibitory concentrations (MICs) between 2.5 and 25 μg/mL and the growth of E. coli, with MIC value being 12.5 μg/mL. Importantly, complex 2 significantly reduced C. albicans filamentation, an essential process for its pathogenesis. Antiproliferative effect on the normal human lung fibroblast cell line MRC-5 was also evaluated with the aim of determining the therapeutic potential of the complexes 1–3. The interactions of these complexes with calf thymus DNA (ctDNA) and bovine serum albumin (BSA) were studied to evaluate their binding activities towards these biomolecules for possible insights on their mode of action.


Author(s):  
Sarkar M.A. Kawsar ◽  
Khaleda Mymona ◽  
Refat Asma ◽  
Mohammad A. Manchur ◽  
Yasuhiro Koide ◽  
...  

This study was carried out to regioselective myristoylation of methyl α-D-glucopyranoside (1) using the direct acylation method gave the corresponding methyl 6-O-myristoyl-α-D-glucopyranoside (2) in fair yield. A number of 2,3,4-tri-O-acyl derivatives (3-15) of this 6-O-substitution product using a wide variety of acylating agents were also prepared in order to obtain newer derivatives of synthetic and biological importance. The reaction conditions are reasonably simple and yields were very good. The structures of the title compounds (2-15) were established by using analytical, physicochemical techniques and spectroscopic data (IR and 1H-NMR). All the synthesized compounds were employed as test chemicals for in vitro antimicrobial functionality test against Gram-positive Bacillus subtilis, Staphylococcus aureus, Gram-negative Escherichia coli, Pseudomonas aeruginosa bacteria and plant pathogenic fungi Aspergillus niger and Candida albicans. For comparative studies, antimicrobial activity of standard antibiotics, Ampicillin and Nystatin were also carried out against these microorganisms. The study revealed that the tested samples exhibited moderate to good antibacterial and antifungal activities. It was also observed that the test substances were more effective against fungal phytopathogens than those of the human bacterial strains. Encouragingly, a number of tested chemicals showed nearest antibacterial and antifungal activities with the standard antibiotics employed.


2019 ◽  
Vol 4 (4) ◽  
pp. 209-215
Author(s):  
D. Joshi ◽  
R. Narigara ◽  
G. Jani ◽  
K. Parikh

A new class of fluorobenzimidazole derivatives (IIIa-j)was synthesized to investigate their antimicrobial potential. All the compounds were prepared by multiple step synthesis, initiating from the synthesis of 5-(difluoromethoxy)-1H-benzimidazole-2-thiol (I). The compound I was further reacted with different derivatives of 2-chloro-N-phenylacetamide (IIa-j) prepared by reacting differently substituted anilines with chloroacetylchloride and triethylamine in DMF (solvent); resulting in formation of fluorobenzimidazoles IIIa-j. The compounds IIIa-j were characterized by spectral analysis viz. 1H NMR, 13C NMR, mass spectra, elemental analysis and IR. All these compounds were screened in vitro for their antimicrobial activity against Gram-positive (S. aureus and E. faecalis) and Gram-negative bacterial (E. coli and P.aeruginosa) strains as well as fungi (A. niger and C. albicans). Some of the compounds exhibited promising results (in MIC) against Gram-negative bacterial strains.


2020 ◽  
Vol 5 (2) ◽  
pp. 138-148
Author(s):  
Macchindra S. Tambe ◽  
Sonali Gadhe ◽  
Amit Choudhari ◽  
Dhiman Sarkar ◽  
Jaiprakash N. Sangshetti ◽  
...  

A series of side chain modified structurally diverse 3,4-dihydro-2H-benzo[b][1,4]-oxazine-2-carboxylic acid derivatives were synthesized and characterized by IR, 1H NMR, 13C NMR and mass spectral study. All the newly synthesized compounds were examined for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra. The synthesized compounds exhibited minimum inhibitory concentration (IC50) ranging from 5.98 to >30 (μg/mL) against MtbH37Ra. Among the screened compounds, compounds 5a, 5c, 5d, 5f, 5g, 5h, 5I, 5j exhibited IC50 as 10.42, 11.81, 18.79, 5.98, 19.21, 24.81 and 14.81 μg/mL, respectively. The antibacterial screening study of these compounds was conducted against four different bacteria to asses there selectivity towards MTB. The antibacterial screening of all the synthesized compounds was conducted against four bacterial strains (Gram-negative strains: E.coli and S.aureus; Gram-positive strains: P. aeruginosa and B.subtilis. The compounds 5a, 5b, 5c, 5e and 5j showed higher antibacterial activity up to 7-25 μg/mL. Furthermore, molecular docking studies revealed the binding modes of the compounds in the binding site of the good agreement with the in vitro antitubercular screening. The compounds 5a, 5c and 5f with free energy of binding lower than -9.0 Kcal/mol binds more favourably at the binding site of panC as compared to other compounds. Specifically, the compound 5f with free energy of binding -9.6 Kcal/mol is indeed found more active in docking study as well as in the in vitro antitubercular screening. These findings open the possibility for potential lead for antituberculosis chemotherapy.


2018 ◽  
Vol 17 (2) ◽  
pp. 221-226
Author(s):  
BC Revanasiddappa ◽  
MS Jisha ◽  
M Vijay Kumar ◽  
Hemanth Kumar

A new series of chalcones (2a-j) were prepared by reacting substituted aldehydes and substituted ketones in alcohol medium in presence of NaOH. The chalcones underwent selective cyclization with guanicol hydrazide (1) in glacial acetic acid medium to yield the title compounds 1,3,5-trisubstituted pyrazolines (3a-j). The new compounds were characterized on the basis of 1H-NMR, IR and mass spectral data. All the newly synthesized compounds were evaluated for their in-vitro antibacterial and antifungal activities. Some of the tested compounds 3a and 3e showed good activity against bacterial strains and compounds 3d and 3h revealed good activity against fungal strains. Dhaka Univ. J. Pharm. Sci. 17(2): 221-226, 2018 (December)


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