Synthesis, antioxidant and anticancer screenings of berberine–indole conjugates

Mistry, Bhupendra M.; Keum, Young‐Soo; Kim, Doo Hwan

doi:10.1007/s11164-015-2208-x

Cited by 18 publications

(11 citation statements)

References 54 publications

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“…The inclusion of antioxidants to the conducted radical cation decreases it to ABTS, identifying a decolourization. In this technique, an antioxidant is included in a pre-formed ABTS radical solution, and after a set period, the staying ABTS _ + is quantified spectrophotometrically at 734 nm [ 42 , 43 ]. In the current study, all extract/fractions except petroleum ether fraction and positive control (ascorbic acid) exhibited a significant, dose-dependent radical scavenging activity ( p < 0.05).…”

Section: Resultsmentioning

confidence: 99%

Assessment of free radical scavenging and anti-proliferative activities of Tinospora cordifolia Miers (Willd)

Polu

Nayanbhirama

Khan

et al. 2017

BMC Complement Altern Med

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Background Tinospora cordifolia (Guduchi or Amrita) is an important drug of Ayurvedic System of Medicine and found mention in various classical texts for the treatment of diseases such as jaundice, fever, diabetes, cancer and skin disease etc. In view of its traditional claims, antioxidant and anti-proliferative activities were evaluated in the present study.MethodsEthanol extract (TCE) and subsequent petroleum ether (TCP), dichloromethane (TCD), n-Butanol (TCB) and aqueous (TCA) fractions of were prepared from stems of T cordifolia. Total phenolic, flavonoid content and anti-oxidant activity was assessed by different methods. Anti-proliferative activity was assessed in cervical carcinoma (HeLa) cell lines by MTT and SRB assay.ResultsEthanol extract and n-butanol fractions shown to be superior in their scavenging activity in all the tested methods. n-butanol fractions shown antioxidant activity with an IC50 of 14.81 ± 0.53, 29.48 ± 2.23, 58.20 ± 0.70 and 21.17 ± 1.19 μg/mL by DPPH, ABTS, Nitric oxide and iron chelating activities respectively. Anti-proliferative activity results demonstrates that the TCD and ethanol extract of T cordifolia exhibits potent cytotoxic effect against HeLa with an IC50 of 54.23 ± 0.94 μg/mL and 101.26 ± 1.42 μg/mL respectively by MTT assay; and with an IC50 of 48.91 ± 0.33 μg/mL and 87.93 ± 0.85 μg/mL respectively by SRB assay.ConclusionThe outcomes of the present study support the fact that T Cordifolia is a promising source of antioxidant agent and propose its further investigation. Moreover, dichloromethane fraction of T cordifolia shown to be the most potent anti-proliferative fraction and further mechanistic and phytochemical investigations are under way to identify the active principles.

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Section: Resultsmentioning

confidence: 99%

Assessment of free radical scavenging and anti-proliferative activities of Tinospora cordifolia Miers (Willd)

Polu

Nayanbhirama

Khan

et al. 2017

BMC Complement Altern Med

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“…Two controls were applied for this test: a negative control (blank) containing of methanol (20 μL) and the DPPH radical solution (180 μL) and a positive control including the referrals anti-oxidant (Ascorbic acid) in methanol and DPPH radical solution. The results of this bioassay, RSA% (the radical scavenging activity in percentage) was determined according to Mensor et al (Mensor et al, 2001, Mistry et al, 2015) as described in the below equation:%Scavenging=Absorbance of blank-Absorbance of testAbsorbance of blank×100…”

Section: Methodsmentioning

confidence: 99%

“…The inclusion of anti-oxidants to the conducted radical cation decreases it to ABTS, identifying a decolourization. In this technique, an antioxidant is included in a pre-formed ABTS radical solution, and after a set period, the staying ABTS •+ is quantified spectrophotometrically at 734 nm (Molyneux, 2004, Mistry et al, 2015). The ABTS •+ was created by responding 7 mM ABTS in H 2 O with 2.45 mM potassium persulfate (K 2 S 2 O 8 ), saved in the dark at room temperature for 12–16 h before use (the radical was constant for more than two days under these conditions).…”

Section: Methodsmentioning

confidence: 99%

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Synthesis of N-Mannich bases of berberine linking piperazine moieties revealing anticancer and antioxidant effects

Mistry

Patel

Keum

et al. 2017

Saudi Journal of Biological Sciences

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A new Mannich base series of piperazine linked berberine analogues was furnished in this study to screen the antioxidant and anticancer potential of the resultant analogues. Alkoxy group at a C-9 position of berberine was converted to hydroxyl functionality to enhance the ability of final scaffolds binding to the target of drug action mainly through hydrophobic effect, conjugation effect, whereas Mannich base functionality was introduced on the C-12 position of berberine. Scaffolds were investigated for their free radical scavenging antioxidant potential in FRAP and DPPH assay, whereas tested to check their Fe reducing power in ABTS assay. The radical scavenging potential of the final derivatives - was found excellent with ICs, <13 μg/mL and < 8 μg/mL in DPPH and ABTS assay, respectively, whereas some analogues showed significant Fe reducing power with absorption at around 2 nm in the FRAP assay. Anticancer effects of titled compounds were inspected against cervical cancer cell line Hela and Caski adapting SRB assay, in which analogues - presented <6 μg/mL of ICs, and >30 of therapeutic indices, thus exerting low cytotoxic values against Malin-Darby canine kidney (MDCK) cell lines at CCs >125 μg/mL. Hence, from the bioassay outcomes it can be stated that these analogues are dual active agents as the scavengers of reactive oxygen species and inhibitors of the cancerous cells as compounds with halogen functional group have overall good pharmacological potential in assays studied in this research. Correct structure of the final compounds was adequately confirmed on the basis of FT-IR and H NMR as well as elemental analyses.

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“…BBR derivates, containing phenolic hydroxy groups, have been reported with enhanced antioxidant activity. At the same time, 8-oxocoptisine, 16 indole, 17 piperazine 18 and benzothiazole 19 derivatives of berberine have also been developed in recent years, while the C-9 position modification of benzoic acid was seldom reported. In our previous work, we designed and synthesized a series of berberine derivatives, and demonstrated that the introduction of an aromatic nucleus on the C-9 position of berberine had important influences on hypoglycemic 20 and anti-inflammatory activities, 21 which were closely related with oxidative stress.…”

Section: Introductionmentioning

confidence: 99%