Rare Phenanthroindolizidine Alkaloids and a Substituted Phenanthrene, Tyloindane, from Tylophora indica

The antimicrobial efficacy of two phenanthroindolizidine alkaloids, tylophorinidine hydrochloride (TdnH) and tylophorinine hydrochloride (TnnH), isolated from the plant Tylophora indica (local name, Antamul) was evaluated. These were screened for in vitro antifungal and antibacterial activities. Both compounds exhibited potent antifungal activity displaying minimum inhibitory concentrations (MIC) in the range of 2-4 μg/mL for TdnH and 0.6-2.5 μg/mL for TnnH against Candida species.

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Assessing the Antimalarial Potentials of Phytochemicals: Virtual Screening, Molecular Dynamics and In-Vitro Investigations

Letters in Drug Design & Discovery ◽

10.2174/1570180815666180604085626 ◽

2019 ◽

Vol 16 (3) ◽

pp. 291-300

Author(s):

Saumya K. Patel ◽

Mohd Athar ◽

Prakash C. Jha ◽

Vijay M. Khedkar ◽

Yogesh Jasrai ◽

...

Keyword(s):

Molecular Dynamics ◽

Structural Integrity ◽

Md Simulations ◽

Tylophora Indica ◽

Multidrug Resistance Protein 1 ◽

Receptor Complexes ◽

Resistance Protein ◽

Dynamics Simulations ◽

Stable Trajectory

Background: Combined in-silico and in-vitro approaches were adopted to investigate the antiplasmodial activity of Catharanthus roseus and Tylophora indica plant extracts as well as their isolated components (vinblastine, vincristine and tylophorine). Methods: We employed molecular docking to prioritize phytochemicals from a library of 26 compounds against Plasmodium falciparum multidrug-resistance protein 1 (PfMDR1). Furthermore, Molecular Dynamics (MD) simulations were performed for a duration of 10 ns to estimate the dynamical structural integrity of ligand-receptor complexes. Results: The retrieved bioactive compounds viz. tylophorine, vinblastin and vincristine were found to exhibit significant interacting behaviour; as validated by in-vitro studies on chloroquine sensitive (3D7) as well as chloroquine resistant (RKL9) strain. Moreover, they also displayed stable trajectory (RMSD, RMSF) and molecular properties with consistent interaction profile in molecular dynamics simulations. Conclusion: We anticipate that the retrieved phytochemicals can serve as the potential hits and presented findings would be helpful for the designing of malarial therapeutics.

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ChemInform Abstract: Iron(III) Chloride-Based Mild Synthesis of Phenanthrene (II) and Its Application to Total Synthesis of Phenanthroindolizidine Alkaloids (V).

ChemInform ◽

10.1002/chin.200848097 ◽

2008 ◽

Vol 39 (48) ◽

Author(s):

Kai-Liang Wang ◽

Mao-Yun Lue ◽

Qing-Min Wang ◽

Run-Qiu Huang

Keyword(s):

Total Synthesis ◽

Phenanthroindolizidine Alkaloids

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Can herbal extracts serve as antibacterial root canal irrigating solutions? Antimicrobial efficacy of Tylophora indica, Curcumin longa, Phyllanthus amarus, and sodium hypochlorite on Enterococcus faecalis biofilms formed on tooth substrate: In vitro study

Journal of Pharmacy And Bioallied Sciences ◽

10.4103/jpbs.jpbs_127_20 ◽

2020 ◽

Vol 12 (5) ◽

pp. 423

Author(s):

Sivadas Ganapathy ◽

Shan Sainudeen ◽

VeenaS Nair ◽

Mohammad Zarbah ◽

AnshadMohamed Abdulla ◽

...

Keyword(s):

Enterococcus Faecalis ◽

Sodium Hypochlorite ◽

Root Canal ◽

In Vitro Study ◽

Vitro Study ◽

Antimicrobial Efficacy ◽

Phyllanthus Amarus ◽

Herbal Extracts ◽

Tylophora Indica

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Antimicrobial potential of Tylophora indica and its future considerations in health and food industry

Pharmacognosy Reviews ◽

10.4103/phrev.phrev_24_17 ◽

2018 ◽

Vol 12 (23) ◽

pp. 72

Author(s):

Shalini Singh ◽

Charu Khanna ◽

Manish Vyas

Keyword(s):

Food Industry ◽

Tylophora Indica ◽

Antimicrobial Potential

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Thymidylate synthase activity in leukocytes from patients with chronic myelocytic leukemia and acute lymphocytic leukemia and its inhibition by phenanthroindolizidine alkaloids pergularinine and tylophorinidine

Cancer Letters ◽

10.1016/s0304-3835(98)00061-5 ◽

1998 ◽

Vol 128 (2) ◽

pp. 183-188 ◽

Cited By ~ 30

Author(s):

K Narasimha Rao ◽

R.K Bhattacharya ◽

S.R Venkatachalam

Keyword(s):

Thymidylate Synthase ◽

Acute Lymphocytic Leukemia ◽

Lymphocytic Leukemia ◽

Chronic Myelocytic Leukemia ◽

Myelocytic Leukemia ◽

Phenanthroindolizidine Alkaloids

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Cytotoxic and Anti-HIV Phenanthroindolizidine Alkaloids from Cryptocarya chinensis†

Natural Product Communications ◽

10.1177/1934578x1200700608 ◽

2012 ◽

Vol 7 (6) ◽

pp. 1934578X1200700 ◽

Cited By ~ 4

Author(s):

Tian-Shung Wu ◽

Chung-Ren Su ◽

Kuo-Hsiung Lee

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Optical Rotation ◽

Ethanol Extract ◽

Cancer Cell Lines ◽

Spectroscopic Methods ◽

Bioassay Guided Fractionation ◽

Phenanthroindolizidine Alkaloids ◽

Anti Hiv

Bioassay-guided fractionation of the cytotoxic ethanol extract of Cryptocarya chinensis has led to the isolation of 11 compounds, including two phenanthroindolizidine alkaloids [(-)-antofine (1) and dehydroantofine (2)], five pavine alkaloids (3-7), and four proaporphine alkaloids (8-11). The structures of the isolated compounds were determined by means of NMR spectroscopic methods, and supported by HRMS and optical rotation data. Compounds 1 and 2 showed cytotoxic activity against four cancer cell lines, L1210, P388, A549, and HCT-8, with 1 being the most potent against A549 and HCT-8 with EC50 values of 0.002 and 0.001 μg/mL, respectively. In addition, 2 is first reported to exhibit significant anti-HIV activity.

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