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Due to side effects and drug resistance, cancer treatment choices are limited despite continued attempts. Topoisomerases are essential for several cellular processes and human topoisomerase I and topoisomerase II alpha inhibitors have proven to be an effective chemotherapeutic alternative for a wide range of cancers, due to its fast proliferating cells and the higher level of these enzymes in solid tumors relative to normal tissue. In this study, around 30 carbazole derivatives were designed using Chem Draw ultra and their ability to inhibit topoisomerase II was investigated using in silico docking studies and molecular dynamics. The results revealed ligand 10 and ligand 25 held good binding energy scores of -9.21 and -9.50, Kcal mol-1 respectively, with good interaction. ADMET analysis assured the drug likeness and better GI absorption than the parent drug and dexrazoxane. Desmond module of Schrödinger Suite was used and it demonstrated the stability in ligand receptor complexes.
Carbazole is a heterocyclic nitrogen-containing chemical. It has a tricyclic structure with two six-membered benzene
rings joined on each side with a nitrogen-containing five-membered ring. When exposed to ultraviolet light, it
produces a powerful fluorescence and a lengthy phosphorescence [1]. Carbazole alkaloids, identified from the
Rutaceae family, are a significant class of naturally occurring heterocycles. Carbazole alkaloids were first isolated as
natural compounds from Murraya koenigii and shown to have potent antibacterial properties. Murraya koenigii stem
bark includes dimeric carbazole alkaloids as well as six carbazole alkaloids. This herb has traditionally been used as a
stimulant, stomachic, febrifuge, analgesic, and to cure diarrhoea, dysentery, and bug stings. It also has antibacterial
properties in addition to these actions [2]. The isolation of ellipticine the first pyrido[4,3-b]. carbazole alkaloid, from
the leaves of Ochrosia elliptica Labill by Goodwin et al. in 1959, was a significant milestone in the development of this
class of natural compounds. The great potency of ellipticines against numerous forms of cancer (osteolytic breast
cancer metastases, kidney cancer, brain tumours, and acute myeloblastic leukemia), low toxic side effects, and total
lack of haematological toxicity are the key reasons for their clinical usage. Nonetheless, these chemicals' mutagenicity
should be assessed as a possible risk factor for these anticancer medicines. In E. coli, they are known to produce
prophage lambda. Furthermore, ellipticine has shown to be a common synthetic target, with a diverse range of
synthetic techniques documented. Furthermore, the structurally similar heteroaryl annulated carbazoles have gotten
a lot of attention in the lab,and these congeners have a better pharmacological profile[3].
Carbazole ring have been exploited by the research field over the past decades since the discovery of parent
compound 9-H carbazole in 1972. Anti-bacterial activity of murrayanine, was the 1st discovered pharmacological
activity which paved the way to further discoveries. Antiplatelet and antimicrobial activities of compounds derived
from Clausena excavata are important among them. Other synthetic derivatives such as 5H-benzo[b]. carbazoles and
furo[3,4-b]. carbazoles have proved the anti-tumour potential of carbazole derived compounds. It’s possible to
explore the carbazole scaffold as a solution to the challenges faced in anticancer drug research. In this review we
focus on the biological potential and applications of carbazole derived compounds ranging from antimicrobial,
antiviral, anti-HIV, anti-oxidant, anti-inflammatory, anti-diabetic, anticancer activities as well topoisomerase 2
inhibition in detail.
The developments in DNA sequencing technology and computational biology have revolutionized the world of
microbiome, which in turn resulted in identifying the contributions of the microbiome to human health.
Dysbiosis of the intestinal microbiota making up the human microbiome can have a marked influence on energy
and immune homeostasis, which results in significant metabolic and immunologic effects on the host, ultimately
leading to many local and systemic diseases including inflammatory bowel disease, asthma, obesity, metabolic
syndrome, cardiovascular disease, immune‐mediated conditions, and neurodevelopmental conditions such as
autism spectrum disorder. In this systematic review, we provide an overview of the evidence on the association
between human gut microbiota and various disorders. Besides, we analyse the effects of microbiome-based
therapies on the above disorders using probiotics
Aloe vera is used for medicinal purposes since ancient times. The botanical name is Aloe barbadensis miller. It belongs to the Liliaceae family. It is also called the healing plant or the silent healer, because of its wound and burn healing properties. Latex and gel are the two basic products of Aloe leaves. The latex and gel contain biologically active components.Polysaccharides contained in the gel of the leaf attribute most of the health benefits associated with Aloe Vera. Aloe was available as pills, ointments, jellies, sprays, drinks, etc. The important application aloe vera was wound healing, treating burns, anti-inflammatory, antidiabetic, anti-cancer, anti-ulcer, protection against skin damage from x-rays, lung cancer, intestinal problems, increasing HDL, reducing LDL, reducing blood glucose in diabetics, fighting against acquired immune deficiency (AIDS), allergies, etc. The aloe vera plant, its biological properties are briefly reviewed in this article.
... 21 Traditionally, Murraya koenigii has been utilized for its stimulant, febrifuge and analgesic effects. 22 In this study, we assessed the effectiveness of koenigicine, a carbazole alkaloid obtained from Murraya koenigii, in mitigating allergic asthma. ...
... Besides the composition, the co-occurrence network of the microbiome may also be useful to explore microbial interactions in the microbiota and identify the keystone taxa that might have the largest influence on diseaserelated symptoms [15]. Studies have revealed some associations between the co-occurrence patterns in the human gut microbiome and predicted metabolic interactions [16], giving new idea in therapies [17]. However, there are very few studies that have explored the ecological relationships between microbiome co-occurrence and respiratory diseases. ...
... While tannins have been shown to affect gut microbiota and metabolism (Tong et al., 2023), flavonoids are said to function as antioxidants and be in charge of the prevention and management of numerous diseases (Ahmad et al., 2015). The biological activities of aloe vera reported in earlier research are likely due to the amount of phytochemicals in the extract (Jose et al., 2021). Also, the discrepancy in the phytochemical profile may be attributed to variations in species, the plant part utilized for analysis, the solvent used and the extraction methodology employed. ...