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Aims: Nilavembu kudineer chooranam is one of the best polyherbal formulations in Siddha tradition of medicinal practice. This formulation has nine herbs as ingredients. This research article explores the scientific analysis of the therapeutic and phytochemical potential of this herbal formulation. Methodology: In this study, Nilavembu Kudineer Chooranam is extracted with hot ethyl acetate using a Soxhlet apparatus. This study focuses on the pharmacognosy, phytochemistry, physico-chemistry TLC analysis and antioxidant ability of Nilavembu Kudineer chooranam. High-performance thin-layer chromatography (HPTLC) is used to analyze the extract of Nilavembu Kudineer Chooranam to screen for active principles. Antioxidant activity of Nilavembu Kudineer Chooranam was determined using DPPH assay. Gas Chromatogram Mass Spectrometric method (GCMS) was carried out in the ethyl acetate extract of NKC for phytochemical analysis. Results: The preliminary phytochemical analysis of the ethyl acetate extract of Nilavembu Kudineer Chooranam reveals the presence of phytochemicals. The quantitative phytochemical estimations show the presence of 0.082 mg of alkaloid, 5.81 mg of flavanoid, 4.32 mg of tannin and 0.736 mg of phenolics in ethyl acetate extract. The HPTLC analysis confirmed the presence of such phytochemicals that are well known for their medicinal properties. The percentage of moisture content, total Ash, acid-soluble ash, and a water-soluble ash content of NKC were found to be 3.7%, 9.07%,1.66%, and 0.75% respectively. The fluorescence analysis of NKC powder with different chemical reagents revealed the presence of several active principles in the extract. The antioxidant ability of NKC extract was also assessed by FACS analysis using DCFDA assay in THP-I (human monocyte) cells. Conclusion: In this in-vitro assay NKC extract significantly reduced the intracellular antioxidant levels in THP-I cells. Thus the in-vitro assay further confirmed the antioxidant potential of NKC extract. It is apparent from the above results and discoveries that NKC makes a perfect health drink.

The pore size of hexagonal mesoporous carbon nitride (HMCN) materials were engineered with different pore sizes of 3.5, 4.7, 5.9, 7.1, 7.9 and 9.2 nm using SBA-15 hard template synthesised at 80, 100, 120, 150, 160 and 180 °C, respectively. HMCN (x) and SBA-15 (x) materials were characterized by XRD, N2 sorption, FESEM, CHN, FTIR, Raman and DR UV–Vis spectroscopy. N2 sorption isotherms of HMCN (x) and SBA-15 (x) samples showed a type IV isotherm with H1 hysteresis loop having a region of steep increase due to capillary condensation. The catalytic performance of HMCN (x) catalysts were studied on the synthesis of α, β-unsaturated carboxylic acid and its derivatives via Knoevenagel-Doebner reaction in metal/pyridine-free, azeotropic conditions (Dean-Stark apparatus) by an environmental friendly approach. Among the HMCN (x) catalysts studied, HMCN (5.9) showed an excellent performance of 94.5% p-hydroxybenzaldehyde conversion with 100% selectivity of p-hydroxycinnamic acid (91% isolated yield) within 60 min. The reaction parameters of temperature, time and catalyst amount were studied on p-hydroxycinnamic acid synthesis. The derivatives of α, β-unsaturated carboxylic acid were synthesised under optimized reaction parameters. The experimental results of our study proved that the pore size engineering of HMCN is important for the catalytic reaction to get maximum product yield for the reactants with different molecular dimensions.

Bacterial communication, termed Quorum Sensing (QS), is a promising target for virulence attenuation and the treatment of bacterial infections. Infections cause inflammation, a process regulated by a number of cellular factors, including the transcription Nuclear Factor kappa B (NF-κB), this factor is found to be upregulated in many inflammatory diseases, including those induced by bacterial infection. In this study, we tested 32 synthetic derivatives of coumaperine (CP), a known natural compound found in pepper (Piper nigrum), for Quorum Sensing Inhibition (QSI) and NF-κB inhibitory activities. Of the compounds tested, seven were found to have high QSI activity, three inhibited bacterial growth and five inhibited NF-κB. In addition, some of the CP compounds were active in more than one test. For example, compounds CP-286, CP-215 and CP-158 were not cytotoxic, inhibited NF-κB activation and QS but did not show antibacterial activity. CP-154 inhibited QS, decreased NF-κB activation and inhibited bacterial growth. Our results indicate that these synthetic molecules may provide a basis for further development of novel therapeutic agents against bacterial infections.

5-Lipoxygenase (5-LOX) is a key enzyme involved in the biosynthesis of pro-inflammatory leukotrienes, leading to asthma. Developing potent 5-LOX inhibitors especially, natural product based ones, are highly attractive. Coumaperine, a natural product found in white pepper and its derivatives were herein developed as 5-LOX inhibitors. We have synthesized twenty four derivatives, characterized and evaluated their 5-LOX inhibition potential. Coumaperine derivatives substituted with multiple hydroxy and multiple methoxy groups exhibited best 5-LOX inhibition. CP-209, a catechol type dihydroxyl derivative and CP-262-F2, a vicinal trihydroxyl derivative exhibited, 82.7% and 82.5% inhibition of 5-LOX respectively at 20 µM. Their IC50 values are 2.1 ± 0.2 µM and 2.3 ± 0.2 µM respectively, and are comparable to zileuton, IC50 = 1.4 ± 0.2 µM. CP-155, a methylenedioxy derivative (a natural product) and CP-194, a 2,4,6-trimethoxy derivative showed 76.0% and 77.1% inhibition of 5-LOX respectively at 20 µM. Antioxidant study revealed that CP-209 and 262-F2 (at 20 µM) scavenged DPPH radical by 76.8% and 71.3% respectively. On the other hand, CP-155 and 194 showed very poor DPPH radical scavenging activity. Pseudo peroxidase assay confirmed that the mode of action of CP-209 and 262-F2 were by redox process, similar to zileuton, affecting the oxidation state of the metal ion in the enzyme. On the contrary, CP-155 and 194 probably act through some other mechanism which does not involve the disruption of the oxidation state of the metal in the enzyme. Molecular docking of CP-155 and 194 to the active site of 5-LOX and binding energy calculation suggested that they are non-competitive inhibitors. The In-Silico ADME/TOX analysis shows the active compounds (CP-155, 194, 209 and 262-F2) are with good drug likeliness and reduced toxicity compared to existing drug. These studies indicate that there is a great potential for coumaperine derivatives to be developed as anti-inflammatory drug.