Background:
Lamiaceae is one of the large families that occur worldwide and has species
that are adaptable to almost all habitats and altitudes. Plectranthus is an important genus of Lamiaceae,
recognized globally as an ornamental as well as a medicinal herb with good economic interest.
The Plectranthus species possess antiseptic, vermicidal and purgative activities.
Objective:
The isolated compounds (1-3) from Plectranthus bishopianus were tested for their preliminary
pharmacological evaluation for antibacterial, antioxidant and cytotoxic activities.
Materials and Methods:
The Plectranthus bishopianus leaves were collected from the Western
Ghats of India. Extractions followed by isolation of the three compounds and structures were identified
by NMR, HRMS.
Results:
The isolated compounds, 6,7-dehydroroyleanone (1), 6β-hydroxy-7α-methoxyroyleanone
(2) and 6β, 7α-dihyroxyroyleanone (3) showed good antioxidant activity by DPPH method. The
results of the cytotoxicity evaluation of the compounds (1-3) displayed excellent activity against
MCF-7 cell line with IC50 values at 3.8 µg/mL, 3.85 µg/mL and 3.7 µg/mL respectively, which is
more potent than the reference standard cisplatin.
Conclusion:
The structures of isolated compounds were confirmed by NMR, LC-HRMS and further
pharmacological evaluation was accomplished. In addition, the isolates (1-3) were subjected to
insilico molecular properties prediction by employing Molinspiration software for calculating their
oral bioavailability and predicted to possess excellent oral bioavailability.
Chemical examination of the MeOH extract of Plectranthus bishopianus Benth., a rare and endangered plant, resulted in isolation of a new abietane diterpene, 6β‐hydroxy‐7α‐methoxyroyleanone (1), along with two more diterpenoids, 6,7‐dehydroroyleanone, and 6β,7α‐dihydroxyroyleanone, a triterpene oleanolic acid, and two sterols, β‐sistosterol and stigmasterol. The structures of the isolated compounds were elucidated on the basis of spectroscopic data and also by comparison with authentic samples.
Forced degradation study of argatroban under conditions of hydrolysis (neutral, acidic and alkaline), oxidation, photolysis and thermal stress, as suggested in the ICH Q1A (R2), was accomplished. The drug showed significant degradation under hydrolysis (acidic, alkaline) and oxidation (peroxide stress) conditions. The drug remained stable under thermal and photolytic stress conditions. In total, seven novel degradation products (DP-1 to DP-7) were found under diverse conditions, which were not reported earlier. The chemical structures of these degradation products were characterized by 1H NMR, 13C NMR, 2D NMR, Q-TOF-MSn and IR spectral analysis and the proposed degradation products structures were further confirmed by the individual synthesis.
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