Screening of flavonoids for antitubercular activity and their structure–activity relationships

Yadav, Akhilesh Kumar; Thakur, Jay Prakash; Prakash, Om; Khan, Feroz; Saikia, Dharmendra; Gupta, Madan M.

doi:10.1007/s00044-012-0268-7

Cited by 40 publications

(21 citation statements)

References 24 publications

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“…The variation in activity could not be verified in this study however it is thought that it could be linked to the number and positions of hydroxyl and methoxy groups on rings A and B. Previous studies have shown that the antimycobacterial activity of alkaloids is affected by the number and positions of functional groups [ 28 ].…”

Section: Discussionmentioning

confidence: 61%

Potential of Zanthoxylum leprieurii as a source of active compounds against drug resistant Mycobacterium tuberculosis

Bunalema

Fotso

Waako

et al. 2017

BMC Complement Altern Med

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BackgroundTuberculosis (TB) is still a global health problem mainly due to development of resistance and co-infection with the Human immune Virus (HIV). Treatment of multi and extensively drug resistant TB requires use of second line drugs which are less efficacious, expensive and very toxic. This has necessitated a need to search for new treatment regimens especially from medicinal plants. Zanthoxylum leprieurii, a plant species from Rutaceae is used locally in the treatment of tuberculosis in Uganda. The aim of the study was to isolate, identify and characterize bio active compounds from Z. leprieurii stem bark with antimycobacterial activity.MethodsCrude extracts, fractions and compounds from air dried stem bark of Z. leprieurii were tested against pan sensitive (H37rv), isoniazid resistant (TMC 301) and rifampicin resistant (TMC 331) strains of M. tuberculosis using micro plate alamar blue assay. Isolation of active compounds was done by using column chromatography and thin layer chromatography. They were analysed using nuclear magnetic resonance spectroscopy and mass spectroscopy.ResultsThe methanol extract had minimum inhibitory concentrations (MIC) of 47.5, 75.3 and 125.0 μg/ml on the pan sensitive strain, rifampicin resistant and isozianid resistant strains of M. tuberculosis respectively. The chloroform extract had MIC values of 260 μg/ml agnaist the pan sensitive strain and 156 μg/ml on the rifampicin resistant strain. Of the sixteen fractions from the methanol extract, fraction Za4 (MIC = 6.3 μg/mL, 23.0 μg/mL, 11.7 μg/mL) and Za6 (MIC = 11.7 μg/mL 31.2 μg/ml, 31.2 μg/ml) were the most active. Three acridone alkaloids; hydroxy-1, 3-dimethoxy-10-methyl-9-acridone (1), 1-hydroxy-3-methoxy-10-methyl-9-acridone (2) and 3-hydroxy-1, 5, 6-trimethoxy-9-acridone (3) were isolated from Za4 and Za6. The MIC of compound 3 was found to be 5.1 μg/ml, 4.5 μg/ml and 3.9 μg/ml on H37rv, TMC 331 and TMC 301 while that of 1 was found to be 1.5 μg/ml, 8.3 μg/ml and 3.5 μg/ml respectively.ConclusionThe results of this study suggest that Z. leprieurii is active on resistant strains of M. tuberculosis and could be a potential source of new leads against resistant tuberculosis. It also verifies the local use of the plant in treatment of tuberculosis.Electronic supplementary materialThe online version of this article (doi:10.1186/s12906-017-1602-x) contains supplementary material, which is available to authorized users.

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Section: Discussionmentioning

confidence: 61%

Potential of Zanthoxylum leprieurii as a source of active compounds against drug resistant Mycobacterium tuberculosis

Bunalema

Fotso

Waako

et al. 2017

BMC Complement Altern Med

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“…Antitubercular activity was recorded (MIC 50 µg/mL) after exposing Mycobacterium tuberculosis to myricetin [ 202 ]. A structure-activity relationship analysis left no doubt that the hydroxy groups in the structure are responsible for this activity.…”

Section: Pharmacological Applicationsmentioning

confidence: 99%

Myricetin: A Dietary Molecule with Diverse Biological Activities

et al. 2016

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Myricetin is a common plant-derived flavonoid and is well recognised for its nutraceuticals value. It is one of the key ingredients of various foods and beverages. The compound exhibits a wide range of activities that include strong anti-oxidant, anticancer, antidiabetic and anti-inflammatory activities. It displays several activities that are related to the central nervous system and numerous studies have suggested that the compound may be beneficial to protect against diseases such as Parkinson’s and Alzheimer’s. The use of myricetin as a preserving agent to extend the shelf life of foods containing oils and fats is attributed to the compound’s ability to protect lipids against oxidation. A detailed search of existing literature revealed that there is currently no comprehensive review available on this important molecule. Hence, the present work includes the history, synthesis, pharmaceutical applications and toxicity studies of myricetin. This report also highlights structure-activity relationships and mechanisms of action for various biological activities.

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“…The compound myricetin revealed curlidependent E. coli biofilm formation inhibition (IC 50 = 46.2 μM), curli contributes to the robustness of E. coli biofilms [45]. Yadav et al [47] demonstrated the anti-tubercular activity of 15 selected flavonoids including myricetin and their structure-activity relationships were evaluated against Mycobacterium tuberculosis H37Rv strain radiometrically. Myricetin was found to be active against M. tuberculosis, with a MIC of 50 μg/mL, and structure-activity relationships authenticated their anti-tubercular potential due to the presence of hydroxy groups in their structure.…”

Section: Antimicrobial Activitiesmentioning

confidence: 99%

Myricetin bioactive effects: moving from preclinical evidence to potential clinical applications

Taheri

Suleria

Martins

et al. 2020

BMC Complement Med Ther

150

111

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Several flavonoids have been recognized as nutraceuticals, and myricetin is a good example. Myricetin is commonly found in plants and their antimicrobial and antioxidant activities is well demonstrated. One of its beneficial biological effects is the neuroprotective activity, showing preclinical activities on Alzheimer, Parkinson, and Huntington diseases, and even in amyotrophic lateral sclerosis. Also, myricetin has revealed other biological activities, among them as antidiabetic, anticancer, immunomodulatory, cardiovascular, analgesic and antihypertensive. However, few clinical trials have been performed using myricetin as nutraceutical. Thus, this review provides new insights on myricetin preclinical pharmacological activities, and role in selected clinical trials.

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Screening of flavonoids for antitubercular activity and their structure–activity relationships

Cited by 40 publications

References 24 publications

Potential of Zanthoxylum leprieurii as a source of active compounds against drug resistant Mycobacterium tuberculosis

Potential of Zanthoxylum leprieurii as a source of active compounds against drug resistant Mycobacterium tuberculosis

Myricetin: A Dietary Molecule with Diverse Biological Activities

Myricetin bioactive effects: moving from preclinical evidence to potential clinical applications

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