Browsing by Author "Tripathi N."

Now showing 1 - 7 of 7
  • Thumbnail Image
    Item
    In-vitro Anti-inflammatory Potential of Standardized Rottlerin Enriched Fraction of Mallotus philippensis Muell. Arg Anti-inflammatory Potential of Rottlerin Enriched Fraction of Mallotus philippensis
    (Springer, 2024) Tripathi N.; Mandrah K.; Goel B.; Bhardwaj N.; Paswan V.K.; Ravikanth G.; Roy S.K.; Jain S.K.
    A rottlerin enriched fraction was prepared from extract of Mallotus philippensis Muell. Arg leaves in ethyl acetate using HP-20 dianion polymeric resin. The procedure of extraction and fractionation was optimized to get fractions enriched with rottlerin. The different fractions obtained were then evaluated for in-vitro anti-inflammatory activity for COX inhibition. The most active fraction (fraction 6) was subjected to standardization by HPLC and found to contain 70% rottlerin, that could be responsible for the highest activity of the fraction. Further, the chromatographic purification of the active fraction yielded rottlerin (1), isoallorottlerin (2), 8-cinnamoyl-5,7-dihydroxy-2,2,6-trimethyl- 3-chromene (3), and mallotophilippen F (4) as markers. The rottlerin-enriched fraction possessed good in-vitro anti-inflammatory activity against both COX-1 and COX-2 enzymes and was more active than the reference standards drugs viz. etoricoxib and ibuprofen. The optimized protocol for extraction and resin-based fractionation was found to be efficient, reproducible, time-saving, and eco-friendly as operated in semi-aqueous conditions. � The Author(s), under exclusive licence to The National Academy of Sciences, India 2024.
  • Thumbnail Image
    Item
    Isolation of cytotoxic cycloartane triterpenoids from Dysoxylum malabaricum
    (Royal Society of Chemistry, 2024) Bhardwaj N.; Sharma V.K.; Tripathi N.; Pimpre K.; Sonti R.; Ravikanth G.; Koch B.; Jain S.K.
    New cycloartane triterpenoids (2-4) have been recently discovered in the bark of Dysoxylum malabaricum. The extraction process involved the utilization of a cytotoxic dichloromethane-methanol extract, which underwent meticulous bioassay-guided fractionation employing high-performance liquid chromatography. A strategic LCMS-DNP-based dereplication approach was used to target the new compounds. Subsequently, the isolated compounds were thoroughly characterized utilizing nuclear magnetic resonance (NMR) and high-resolution electrospray ionization mass spectrometry (HRESIMS) data, and their absolute configurations were ascertained through electronic circular dichroism (ECD) calculations. In the context of biological activity, the compounds were evaluated for their cytotoxic potential against a panel of breast cancer cell lines and human normal embryonic kidney cancer cells. 2 demonstrated remarkable cytotoxicity, exhibiting an IC50 value of 18 ?M against the T-47D breast cancer cell line, concurrently eliciting apoptotic cell death. The findings of this study emphasize the substantial potential of 2 as a promising candidate for further development as an anti-cancer agent. � 2024 The Royal Society of Chemistry.
  • Thumbnail Image
    Item
    Isolation, Cytotoxicity, and In-silico Screening of Coumarins from Psoralea corylifolia Linn.
    (John Wiley and Sons Inc, 2024) Tripathi N.; Parmar A.; Pandey N.; Bhardwaj N.; Chakrabarty S.; Sarkar R.; Kumar H.; Jain S.K.
    Psoralea corylifolia (syn. Cullen corylifolium), commonly called bawachi, is a medicinal plant extensively used for skin conditions like leukoderma, vitiligo, and psoriasis. It is notably rich in valuable bioactive compounds, particularly coumarins and furanocoumarins. This study isolated fourteen coumarins from P. corylifolia which were tested for cytotoxicity using the MTT assay, with compound 10 showing good cytotoxicity against A549 cells (IC50 0.9 ?M), while compound 1, compound 2, and compound 3 displaying potential cytotoxicity against MDA-MB-231 cells (IC50 0.49 ?M, 0.56 ?M, and 0.84 ?M respectively). Additionally, the compounds? interaction with Epidermal Growth Factor Receptor (EGFR) protein, highly expressed in both cell lines, was investigated through molecular modeling studies, that aligned well with cytotoxicity results. The findings revealed the remarkable cytotoxic potential of four coumarins 1, 2, 3, and 10 against A549 and MDA-MB-231 cell lines. � 2024 Wiley-VHCA AG, Zurich, Switzerland.
  • Thumbnail Image
    Item
    Mangiferin from Enicostemma littorale Blume�with in silico and in�vitro anti-inflammatory potential
    (Taylor and Francis Ltd., 2024) Kumar N.; Tripathi N.; Kumar S.; Kushwaha M.; Banerjee C.; Dey S.
    The bioassay-guided fractionation of the extract of aerial parts of Enicostemma littorale resulted in two fractions 3 and 4 with moderate and potent antioxidant activity, respectively. The purification of fraction 3 gave swertiamarin (1), while the LCMS profile of fraction 4 unveiled the presence of another constituent along with swertiamarin. The extensive purification of fraction 4 led to the unusual isolation of mangiferin (2) from E. littorale. The uncommon isolation of mangiferin from E. littorale motivated us to conduct its in silico and in�vitro screening as an anti-inflammatory agent. Both studies have proved mangiferin to be a promising anti-inflammatory molecule with a binding energy of ?9.17 kcal/mol against Cyclooxygenase-2 protein and IC50 of 146.07 nanomolar. This study is the first report of the isolation of mangiferin, a xanthone glycoside from E. littorale. Communicated by Ramaswamy H. Sarma. � 2023 Informa UK Limited, trading as Taylor & Francis Group.
  • Thumbnail Image
    Item
    New ring-A modified cycloartane triterpenoids from Dysoxylum malabaricum bark: Isolation, structure elucidation and their cytotoxicity
    (Elsevier Inc., 2024) Bhardwaj N.; Gupta P.; Tripathi N.; Chakrabarty S.; Verma A.; Kumari S.; Gautam V.; Ravikanth G.; Jain S.K.
    The Genus Dysoxylum (Meliaceae) consists of approximately 80 species that are abundant in structurally diverse triterpenoids. The present study focused on isolating new triterpenoids from the bark of Dysoxylum malabaricum, one of the predominant species of Dysoxylum present in India. The methanol-dichloromethane bark extract was subjected to LCMS profiling followed by silica gel column chromatography and HPLC analysis to target new compounds. Two new ring A-modified cycloartane-type triterpenoids (1 and 2) were isolated from the bark extract. Spectroscopic methods like NMR, HRESIMS data, and electronic circular dichroism calculations elucidated the structures and absolute configurations of the isolated compounds. These compounds were evaluated for their cytotoxic potential against breast cancer cells and displayed notable cytotoxicity. Compound 1 exhibited the highest cytotoxicity against the MDA-MB-231 cells and induced apoptotic cell death. Also, it was able to inhibit glucose uptake and increase nitric oxide production in breast cancer cells. � 2024 Elsevier Inc.
  • Thumbnail Image
    Item
    Synthesis and Antitubercular Evaluation of Diverse Glycosylated Ureas from D-Glucose
    (Hindawi Limited, 2024) Tripathi N.; Tiwari V.K.
    N, N-disubstituted glycosylated ureas have been synthesized in good-To-excellent yields by 1,4-conjugate addition of amines to glycosylated olefinic esters followed by reaction of resulting glycosyl ?-Amino esters with diisocyanates. The developed sugar-based molecules were well characterized by extensive standard spectroscopic analysis including NMR (1H, 13C, and DEPT), IR, MS, and elemental analysis and were screened for their biological activity against Mycobacterium tuberculosis (M. Tb.), where some of them displayed potent antitubercular activity. The molecules have been designed keeping in view the well-known inhibitors of the enzymes involved in the biosynthesis of mycobacterial cell wall polymers and may be further explored as lead molecules for the successful development of a potential antitubercular drug candidate.Dedicated to Dr. Rama P. Tripathi, Former Chief Scientist at CSIR-Central Drug Research Institute, Lucknow, India, for his extraordinary contribution to "Drug development against Tuberculosis". � 2024 Neetu Tripathi and Vinod K. Tiwari.
  • Thumbnail Image
    Item
    Unveiling the healing properties of 2,3-dehydrosilychristin: a potential silymarin-derived flavonolignan from Vitex negundo
    (Taylor and Francis Ltd., 2024) Tripathi N.; Naik A.; Kumar D.N.; Bhardwaj N.; Goel B.; Kumar S.; Chakrabarty S.; Ranjan A.; Guru S.K.; Kumar S.; Agrawal A.; Jain S.K.
    The compound 2,3-dehydrosilychristin, a flavonolignan linked to silychristin and silymarin, remains intriguing due to its challenging isolation from silymarin. While silymarin has been the exclusive source of flavonolignans�silybin, silychristin and silydianin ? 2,3-dehydrosilychristin is reported in this study from Vitex negundo Linn. leaves. 2,3-Dehydrosilychristin (7) and 14 other compounds were isolated through focused extraction. Its subsequent pharmacological evaluation demonstrated potent antioxidant and in-vitro anti-inflammatory effects, notably inhibiting cytokines TNF-?, IL-6, IL-8 and VEGF. In in-vivo assessments, 2,3-dehydrosilychristin (7) revealed remarkable hepatoprotective potential by reducing liver enzyme levels AST and ALT. These findings expand the potential of 2,3-dehydrosilychristin and suggest bioprospecting Vitex species as alternate sources of bioactive flavonolignans. � 2024 Informa UK Limited, trading as Taylor & Francis Group.