Exploring the pharmacological and chemical aspects of pyrrolo-quinazoline derivatives in Adhatoda vasica.

Adhatoda or Justicia is one of the biggest and complex genera of the Acanthaceae family. Adhatoda vasica is commonly known as 'Adosa'. It is an ayurvedic medicine with a medicinal history of more than a thousand years in India. Traditionally, it is used to treat cough, asthma, phlegm, bleeding hemorrhoids, for both adults and youth. This plant possesses antiarthritis, antiseptic, antimicrobial, anti-tuberculosis, anti-inflammatory and abortifacient properties. Alkaloids are the major phytoconstituents present in the plant in the form of pyrrolo-quinazoline derivatives viz vasicine, vasicinone, vasicinol, adhatodine, adhatodinine, adhavasinone and anisotine etc. The asserted objectives are to conduct a systematic review on the phytochemistry, pharmacology and traditional uses of A. vasica, as well as highlighting the challenges found in the research. This will promote the utilization of A. vasica at extract level and further development of new drug leads based on the compounds isolated and used for treatment of various ailments. The present review covers the literature survey from 1888 to 2023. The relevant data has been collected from various peer-reviwed journals, and books via Sci-Finder, PubMed, Science Direct, Google Scholar, EBSCO, online electronic journals, SpringerLink and Wiley. This paper aims to present a systematic review of known traditional applications, pharmacological and chemical aspects in Adhatoda vasica.

Study of potent CDK7 inhibitor secondary metabolites from Tecomella undulata.

Chemical investigation of the petroleum ether extract of heartwood of Tecomella undulata led to the isolation of tectonaquinone B (1), 2-methylquinizarin (2) along with tecomaquinone I (3), lapachol (4), 2-isopropenylnaphtho[2,3-b]-furan-4,9-quinone (5), dehydro-α-lapachone (6), α-lapachone (7), and ß-lapachone (8). This is the first report of isolation of tectonaquinone B and 2-methylquinizarin from this plant. The structures of compounds were elucidated by advanced spectroscopic methods. Molecular docking study for potential inhibitory action toward CDK7 (cyclin-dependent kinase 7) were performed, which proved that these compounds have high binding affinities with the receptor protein (CDK7). 2-Methylquinizarin exhibited best docking score (-7.70 kcal/mol) among all the tested compounds. The present study showed that 2-methylquinizarin may exhibit potent anticancer activity through inhibiting CDK7 via interaction with Met94.

Tectonaquinones A, B and C: three new naphthoquinone derivatives from the heartwood of Tectona grandis.

Chemical investigation of the chloroform extract of heartwood of Tectona grandis L. f. led to the isolation of three new naphthoquinone derivatives, tectonaquinones A (1), B (2) and C (3), along with six known compounds: barleriaquinone-I (4), tectoquinone (5), tecomaquinone I (6), lapachol (7), obtusifolin (8) and 2-hydroxy-3-methyl anthraquinone (9). The structures of the new compounds were elucidated by spectroscopic methods including 2 D NMR experiments. Tectonaquinone B is the first natural compound that has a hexa-cyclic dinaphthofuran-dione scaffold. Tectonaquinone C has a bicyclic acetal motif that is unusual in nature.

A review on phytochemical constituents and pharmacological potential of Calotropis procera.

Calotropis procera is locally known as Aak or Madar in Hindi, milk weed in English and belongs to the family Apocynaceae and subfamily Asclepiadoideae. Although a wasteland plant, it is of sacred use as its flowers are offered for worshipping Lord Shiva, a Hindu God. Tribes all over the world use the plant in treatment of various diseases like snake bite, body pain, asthma, epilepsy, cancer, sexual disorders, skin diseases and many more. This plant contains various phytoconstituents such as flavonoids, terpenoids, cardenolides, steroids oxypregnanes etc. Though literature searches reveal many reviews about ethnomedicinal uses, chemical composition and pharmacological activities, no recent papers are available that provide an overview of the therapeutic potential and toxicity of Calotropis procera. Hence, the insight of this review is to provide a systemic summary of phytochemistry, pharmacology, toxicology and therapeutic potential of Calotropis procera and to highlight the gaps in the knowledge so as to offer inspiration for future research.

Facile Synthesis of Naphtha-quinoxaline Derivatives from ß-lapachone Using Graphene Oxide as Catalyst.

OBJECTIVE: To develop efficient method for the synthesis of naphtha-quinoxaline derivatives via the reaction of ß-lapachone with various 1,2-diamines. METHODS: A mixture of ß-lapachone (1mmol), 1,2-diamine (1mmol) and graphene oxide (20mg) in methanol (3mL) was heated at 60°C, under constant stirring for appropriate time. After completion of the reaction, the catalyst was filtered off, washed with ethyl acetate (3x3mL) and the combined filtrate was washed with H2O, dried (anhy. Na2SO4) and concentrated under vacuum. The residue was chromatographed over a column of silica gel eluting with a mixture of hexane and ethyl acetate in different ratios, to afford the desired product. All synthesized compounds were assigned with the help of analytical and 1H, 13C NMR, IR, and mass spectral studies. RESULTS: To establish the catalytic role of GO in the synthesis of naphtha-quinoxaline derivatives, the reaction of ß-lapachone with 3,4-diaminotoluene was selected as a model reaction. The catalytic activity of graphene oxide in comparison with other catalysts like acidic resin amberlyst-15 and solid acid catalyst like montmorillonite K-10 were studied. The reaction was also observed in various solvents such as water, acetonitrile, toluene, dichloromethane, ethanol and 1,4-dioxane using GO as a catalyst. Excellent yields were obtained at 60°C in methanol. The efficacy of the present protocol was investigated by the reaction of ß- lapachone with other 1,2-diamines. CONCLUSION: An attractive green metal free carbocatalyst Graphene Oxide (GO) has been successfully utilized for the expedient synthesis of naphtha-quinoxaline derivatives. GO showed high catalytic activity which is attested by the desired products being produced in shorter time. The main advantage of this method is the reusability of the catalyst which makes the procedure sustainable.

Tectona grandis (teak) - A review on its phytochemical and therapeutic potential.

Tectona grandis Linn (Teak), is locally known as Sagwan, belongs to Lamiaceae family. It is one of the most valuable timber in the world, due to its beautiful surface and its resistance to termite and fungal damage. The main active ingredient compounds that are responsible for these action are tectoquinone, lapachol and deoxylapachol. Naphthoquinones, anthraquinones and isoprenoid quinones are abundant metabolites in teak. In addition to these, teak contains several other phytochemicals such as triterpenoids, steroids, lignans, fatty esters and phenolic compounds. Pharmacologically, the plant has been investigated for antioxidant, anti-inflammatory, anti-pyretic, cytotoxic, analgesic, hypoglycemic, wound healing and antiplasmodial activities. The present review highlights the phytochemical and pharmacological aspects of teak.