Bashir Ahmad Chaudhary

Recent Developments and Biological Activities of N-Substituted Carbazole Derivatives: A Review

Carbazoles represent an important class of heterocycles. These have been reported to exhibit diverse biological activities such as antimicrobial, antitumor, antiepileptic, antihistaminic, antioxidative, anti-inflammatory, antidiarrhoeal, analgesic, neuroprotective and pancreatic lipase inhibition properties. A series of carbazole derivatives such as N-substituted carbazoles, benzocarbazoles, furocarbazoles, pyrrolocarbazoles, indolocarbazoles, imidazocarbazoles, etc. have been synthesized. The N-substituted derivatives have gained the attention of researchers due to their therapeutic potential against neurological disorders and cell proliferation. Herein an attempt is made to review the medicinal importance of recently synthesized N-substituted carbazoles.

Antifungal and antispasmodic activities of the extracts of Euphorbia granulata

The dichloromethane and methanolic extracts of the plant Euphorbia granulata were investigated for their antifungal, antibacterial, phytotoxic, brine-shrimp cytotoxic, antioxidant, spasmolytic (antispasmodic) and acetylcholinestrase inhibitory activities. The dichloromethane extract showed strong inhibition against Microsporum canis (90%) and against Aspergillus flavus (50%). Both the extracts inhibited the spontaneous contractions in rabbit jejunum preparations with EC50 value of 0.17 and 1.3 mg/mL, respectively and also relaxed the K + -induced contractions with EC50 0.2 and 2.8 mg/mL, respectively, suggesting a calcium channel blocking activity. However, the extracts did not show antibacterial, phytotoxic, brine-shrimp cytotoxic, antioxidant and acetylcholinestrase inhibitory activities.

ISOLATION OF PENTANDRAONE FROM METHANOLIC EXTRACT OF AERIAL PART OF ZALEYA PENTANDRA

Zaleya pentandra is a well known species in the genus Zaleya . It has wide traditional medicinal uses. Zaleya pentandra is being used for treatment of stomach diseases, respi ratory tract infection and cough. For the purpose of isolation from the dried aerial parts of Zaleya pentandra was subjected to extraction with methanol, this combined extract was concentrated and column chromatography was then carried out. The isolation a nd purification yielded amorphous solid which was subjected to physical, chemical, and spectral techniques like UV, IR, 1 H - NMR, 13 C – NMR and HREI - MS for the structure elucidation of compound. The compound was concluded as pentandraone, a novel compound iso lated for the first time from the methanolic extract of aerial part of Zaleya pentandra .

Isolation of squarrosal and squarrosol compounds from methanol root extract of Ruellia squarrosa (Acanthaceae)

Purpose : To identify, characterize and structurally elucidate bioactive compounds from root of Ruellia squarrosa. Methods : One kilogram of crude Ruellia squarrosa root was shade dried for 14 days, ground to a fine powder and subjected to a methanol extraction. The resultant extract underwent column chromatography for further purification. The isolated compounds were subjected to ultraviolet spectroscopy (UV), infra-red (IR), proton nuclear magnetic resonance ( 1 H-NMR), 13 C–NMR and high resolution electron ionization mass spectrometry (HR-EI-MS) for the identification, characterization and structural elucidation of bioactive compounds. The most active compounds were tested for anticancer activities against human prostate cancer cell. Results : Two active compounds, squarrosol and squarrosal, were obtained with half-maximal inhibitory concentration (IC 50 ) of 15.6 and 26.6 μg/mL, respectively, against human prostate cancer cell lines. Squarrasol showed a significantly (p < 0.05) greater inhibition of cell proliferation than the same dose of squarrasal. Conclusion : These findings suggest that extracts of Ruellia squarrosa containing the bioactive compounds, squarrosol and squarrosal, can potentially be developed for the treatment of human prostate cancer. Keywords : Ruellia squarrosa, Prostate cancer, Squarrosol, Squarrosal, Anit-proliferative