Simultaneous estimation of Curcumin and Gefitinib in bulk by using RP-HPLC technique with PDA detector

Plan: RP-HPLC method development and validation for the simultaneous estimation of curcumin and Gefitinib in bulk. Preface: RP-HPLC chromatographic method the been widely employed in the determination of individual components in a mixture or fixed dose combination. For the ternary mixture containing Curcumin and Gefitinib, no chromatographic method for simultaneous evaluation has been reported so far. Thus our aim is to develop a simultaneous estimation method for curcumin and gefitinib by using an RP-HPLC method using a PDA detector. Methodology: The method was validated as per ICH guidelines. The recovery studies confirmed the accuracy and precision of the method. Outcome: The proposed method was found to be accurate, repeatability and consistent. It was successfully applied for the analysis of the drug in the marketed formulation and could be effectively used for the routine analysis of formulation containing the drug without any alteration in the chromatography conditions.

In vitro anti-inflammatory and cytotoxicity studies of two mangrove associated lichens, Dirinaria consimilis and Ramalina leiodea extracts

Plan: To evaluate the anti-inflammatory and cytotoxicity activity of different extracts from two different manglicolous lichens (Dirinaria consimilis and Ramalina leiodea). Preface: Inflammation is the origin of several deadly diseases like cancer, atherosclerosis, Alzheimer’s and rheumatoid arthritis. From decades, lichen extracts and its metabolites are well known in treating inflammation and cancer. Outcome: The outcome of protein denaturation method confirmed that the ethyl acetate and acetone extract of R. leiodea depicted better inhibitory profile against protein denaturation with IC50 values of 268 and 330 µg/mL Furthermore, the results of SRB assay showed that ethyl acetate and acetone extracts of both the lichens acts potently against MCF-7, DLD-1, HeLa and A549. Simultaneously, all the tested extracts depicted the low degree of specificity towards NHME, they are less toxic. Hence, further screening of these extracts may lead to the exploration of safe and potent anti-inflammatory and anticancer agents.

Studies on the antioxidant activity of Costus igneus leaf extract

Plan: The antioxidant activity studies of the extract of Costus igneus leaves Preface: Costus igneus commonly known as fiery costus or Spiral flag is a species of herbaceous plant. It is claimed to help build up insulin in the human body and is sometimes referred to as insulin plant. Insulin plant Costus igneus (Fam: Zingiberaceae) is a tropical evergreen shrub with large, smooth, dark green leaves. The Costus igneus is valued mainly for its tonic, stimulant, and antiseptic properties. It is said to be aphrodisiac and to be able to prevent the hair from turning grey. Its root is anodyne, antibacterial, antispasmodic, aphrodisiac, carminative, stimulant, stomachic, tonic and vermifuge. Methodology: In the present study the antioxidant activity of the leaf extract was studied using four methods viz. DPPH assay, reducing power assay, superoxide radical scavenging assay, and Folin-ciocalteu assay. Outcome: The studies have proved that extract possesses antioxidant activity. In reducing power assay, the plant extract showed 75.43 % increase in reducing power compared to Ascorbic acid which showed 91.94%, at a concentration of 16µg/ml. In DPPH assay, plant extract produced 71.85% DPPH scavenging activity, compared to Ascorbic acid which produced 84.47% at a concentration of 160µg/ml. In superoxide scavenging activity, the plant extract produced 68.19% radical scavenging activity compared to the standard which showed 79.78% at a concentration of 800µg/ml. The IC50 was found to be177 and 367 µg/ ml of the standard and plant extract respectively.

THE BAOBAB TREE

Trees are known to live for many years. Gautama Buddha attained enlightenment while meditating underneath a peepal tree (Ficus religiosa). A branch of the original tree was rooted in Anuradhapura, Sri Lanka in 288 B.C. and is known as Jaya Sri Maha Bodhi. It is the oldest plant in the world. Long-living plants are found in many parts of the world. The Baobab tree is one among them. Baobab is the common name of a genus of trees (Adansonia) distributed in Madagascar, Africa, Australia and India. The Baobab is the national tree of Madagascar. The Baobab is also known as “bottle tree”, “the tree of life”, “upside-down tree”, and “monkey bread tree”.

Screening of Antimicrobial Activity of Siddha drug Kukkiladhi Choornam

Plan: Kukkiladhi choornam is one of the Siddha drugs, which has been indicated for its anti-microbial properties. The aim of the present study was to validate the antibacterial and antifungal activity of Kukkiladhi choornam extract against various microorganisms. Preface: The present study examined the in-vitro screening of antimicrobial activity of Siddha drug Kukkiladhi choornam. Methodology: The extracts were tested for antimicrobial activity using agar well diffusion on solid media. The microorganisms used in the present study include Streptococcus pyogenes, Staphylococcus aureus, Escherichia coli, Salmonella typhi, Shigella flexneri, Proteus vulgaris, and Candida albicans. Outcome: The study revealed that 50µl extract of Kukkiladhichoornam had significant inhibiting activity against Shigellaflexneri (17mm), Streptococcus pyogenes (17mm) and Candida albicans (18mm).

Synthesis and Antioxidant activity of novel Pyrazoline derivatives

Plan: A novel series of pyrazolines were synthesized through chalcones. The synthesized compounds were evaluated for various antioxidant activities. Preface: Pyrazolines belongs to five-membered nitrogen classes of compounds. Pyrazolines were reported with widespread chemotherapeutic activities. Methodology: A new series of Chalcones (2a-j) were prepared by reacting substituted aldehydes and ketones in alcohol medium in presence of NaOH. The chalcones (2a-j) undergoes selective cyclization with benzhydrazide (1) in glacial acetic acid medium to yield the title compounds 1, 3, 5-trisubstituted Pyrazolines (3a-j). The new compounds were assigned on the basis of 1H-NMR, IR and Mass spectral data. The newly synthesized compounds were screened for their In-Vitro antioxidant activity by DPPH, superoxide and nitric oxide methods. Outcome: Some of the tested compounds 3e, 3g, and 3f showed moderate activity when compared to the standard drug ascorbic acid.

Synthesis, characterization and anti-fungal potential evaluation of 1, 4 thiazine derivatives by Mannich bases

Plan: The present research work is aimed to synthesize newer, less toxic and more effective Mannich bases of 1, 4 thiazine derivatives and further compare their antifungal activities. Preface: Microbial infections are becoming the most important issue for global health and economy. Among these fungal infections are the major problem these days. The morbidity and mortality of invasive fungal infections are unacceptably high. It is an urgent need for the development of new antifungal agents to treat these life-threatening invasive infections. Methodology: Mannich base was synthesized by using o-amino thiophenol with maleic anhydride. Further, four derivatives of Mannich bases were synthesized from 3-oxo-3, 4-dihydro-2H-1, 4-benzothiazin-2-yl) acetic acid with sulpha drugs, ethanol, and formaldehyde. Then synthesized Mannich bases were docked against Dihydrofolate reductase complexed with NADPH and 6- methyl-5- [3-methyl-3-(3,4,5-trimethoxyphenyl) but-1-yn-1-yl]pyrimidine-2,4-diamine (UCP115A)using Argus Lab software. On this basis, we selected 3QLS as a biological target for docking study of synthesized compound. Outcome: The structures of the synthesized compounds were confirmed by UV, IR and Mass Spectroscopic studies. All the newly synthesized derivatives were screened for antifungal activity against Candida albicans NCIM 3100 and Aspergillus niger NCIM 596 by agar diffusion method (Kirby- Bauer method) using fluconazole (10µg/disc) as the standard and dimethyl sulphoxide as the vehicle. The docking results indicate the Mannich bases of 1, 4-thiazines (ligand binding energy varies from -8.9046kcal/mol to -12,0457kcal/mol) shows considerable antifungal activity against Candida albicans. Out of the four derivatives, E4 (Sulfamethoxazole substituted 1, 4- thiazine) possess the best ligand pose energy (-12.0414 kcal/mol) and two hydrogen bond. Among these synthesized compounds, compound E4([4({[4-(N-(5-methyl-3-isoxazolyl) amino sulfonyl) phenyl] amino} methyl)-3-oxo-3,4-dihydro-2H1,4-benzothiazin-2yl] acetic acid) showed highest antifungal activity due to the presence of 1,4- thiazine with sulfamethoxazole substitution.