Current Bioactive Compounds - Online First

The pharmacological significance of 5-hydroxy-3,7,4'-trimethoxy flavone (5HTMF), a flavonoid isolated from Cleome gynandra L. (Capparidaceae), in mononuclear lymphocytes of patients with Rheumatoid Arthritis (RA) has been well-documented. In previous studies, the anti-inflammatory and anti-arthritis activity of CWF was reported.

However, there is a lack of information on the toxicity of 5HTMF. This study aimed to assess the embryonic toxicity of 5HTMF on zebrafish embryos, using dexamethasone as a standard for liver toxicity. At 12 hours post fertilization (hpf), no significant toxicity from 5HTMF was observed on allantoic membrane development.

By 24 hpf, 20% of embryos showed minor changes in tail development at a 100 μM concentration of 5HTMF, while dexamethasone (10 μM) disrupted the allantoic membrane in 61.11% of embryos. In the liver toxicity assay, 5HTMF did not show any significant toxicity.

At 48 hpf, dexamethasone exhibited substantial toxicity at a concentration of 10 μM. In conclusion, the findings suggest that 5HTMF may be a safe and non-toxic dietary supplement for treating chronic inflammatory conditions such as RA.

The overuse of food additives and preservatives has become a source of concern globally due to the inherent risks associated with them. This study evaluated neurobehavioral performance, atherogenic risk, and oxido-inflammatory response in mice fed with normal and high-fat diets supplemented with combined sodium benzoate (SB) and monosodium glutamate (MSG).

Mice were divided into four groups (n=6) and fed with normal diet (ND), high-fat diet (HFD), ND+MSG+SB, and HFD + MSG +SB, respectively, for 28 days. Neurobehavioral performance in mice was carried out in an open field, and Y-maze tests were performed. Serum was obtained to determine lipid profile and atherogenic risk, while brain homogenate was used to determine oxidative stress, inflammatory markers, and neurotransmitter-related enzyme activities.

This study reported that in mice fed with HFD, ND+MSG+SB, and HFD + MSG +SB, there was a significant (p < 0.05) decrease in explorative activity, an increase in anxiety-like behavior, as well as decreased memory performance. Malondialdehyde and nitrites levels increased, while levels of reduced glutathione and antioxidant enzyme activities, catalase and superoxide dismutase, were significantly reduced. Pro-inflammatory cytokines (TNF-α and IL-6) were significantly increased in the brains of mice fed with HFD, ND+MSG+SB, and HFD + MSG +SB when compared with control. Moreover, the activities of acetylcholinesterase increased while glutamic acid decarboxylase decreased significantly.

In conclusion, SB and MSG supplementation in diets caused neurobehavioral deficits in mice, increased atherogenic risk, and upregulated oxidative stress and inflammatory response in mice brains.

This review aims to discuss the traditional applications, ethnobotanical significance, phytochemistry, and pharmacological profile of Acacia catechu (A. catechu). By examining the crude extracts, isolated components, and various fractions of the plant, the review seeks to identify potential new therapeutic agents.

The available published literature on the plant was searched in databases like Scopus, Google Scholar, Science Direct, ACS, Wiley, Web of Science, Springer Link, and PubMed for all appropriate information to bring this review in place. In addition, other official electronic sources like the Encyclopedia Britannica and Northern Regional Center of the Botanical Survey of India, along with the links theplantlist.org, were also searched. In addition to these sources, some book chapters and books were also searched for the same.

A. catechu is a well-documented tree with numerous medicinal uses, widely utilized in Asia and beyond. The plant exhibits various pharmacological properties, including antibacterial effects, antidiarrheal activity, analgesic properties, cholesterol-lowering capabilities, ulcer protection, antidiabetic effects, inhibition of cell growth and anti-inflammatory actions.

This article goes into great detail about plants, ethnopharmacology, phytochemistry, pharmacology and toxicity studies.

Oxazole and the compounds containing sulphonamides are utilized for various treatments of microbial disease as well as for diabetic patients. In the current study, the above moiety synthesizes the new molecule for the treatment of diabetes and microbial infection. The present work involved oxazole-based sulphonamide derivatives by the N-acylation and N-sulphonation. The synthesis was carried out by treating substituted anilines with chloroacetic chloride. The cycloaddition reaction was carried out using triethyl amine as a base catalyst. In the final steps, toluene sulphonyl chloride was used for sulphonation. The synthesized substance was confirmed viaIR, 1H NMR, ESI, Mass spectroscopy, and elemental investigation technique.

Every reagent and starting material used in the synthesis was pure enough to be used as a reagent. To provide an inert environment, the solvents were purified in accordance with conventional laboratory protocols under a nitrogen atmosphere. Melting points are expressed in degrees Celsius and are uncorrected. They were determined by the open capillary technique. KBr pellets and a Shimadzu 8201 PC FTIR spectrophotometer were used to obtain FTIR spectra. Using JEOL and Bruker 500 MHz NMR spectrometers, ~1H and ~13C NMR spectra were obtained in CDCl3 and DMSO-d6, with TMS serving as the internal reference. A Thermo-Finnigan mass spectrophotometer was used to determine the masses of the chemical using the ESI technique.

The present work involved oxazole-based sulphonamides derivatives by the N-acylation and N-sulphonation. The synthesis was carried out by treating substituted anilines with chloroacetic chloride. The cycloaddition reaction was carried out using triethyl amine as a base catalyst. In the final steps, toluene sulphonyl chloride was used for sulphonation. IR, 1HNMR, ESI, Mass spectroscopy and elemental analysis technique confirmed the synthesized compound.

Oxazoles are also related to compounds called 1,3-azoles[nitrogen and oxygen heteroatoms in a 5-membered ring]. Oxazole demonstrates aromaticity since Huckel's rule requires 6π electrons, which are provided by the delocalization of a single pair of electrons from the oxygen atom. It has a wide range of pharmacological aspects like anti-allergic, hypertension, inflammation, schizophrenia, and inflammation. Similarly, sulphonamides are also used as preventive and chemotherapeutic agents against various diseases such as antibacterial, antiprotozoal, antifungal, and translation initiation inhibitors.

The preliminary biological activity was performed on a preliminary level for the antimicrobial and antidiabetic profile. The disc diffusion approach was utilized to achieve the antibacterial activity; similarly diabetic activity was carried out by the induced method. Out of all the synthesized compounds N-[5-[2-[4-bromophenyl amino]acetyloxazole2 yl]-4methylo benzene sulphonamide [4a], N-[5-2[2-FLoro-5nitrophenyl amino]acetyloxazole2yl]-4methylo benzene sulfonamide [4b] show significant effect compared to standard drugs.

Cucurbitacin-induced apoptosis and inhibition of cell growth can render several cancers ineffective. The microbial transformation of cucurbitacin-E-glucoside to cucurbitacin-E was carried out by Curvularia lunata (NRRL 2178). Moreover, in vitro anticancer activity against the MCF-7 cell line as well as in vivo anticancer activity against dimethylbenz (a) anthracene (DMBA)-induced breast cancer in mice using cucurbitacin-E was evaluated.

The cucurbitacin-E-glucoside was biotransformed by Curvularia lunata to cucurbitacin-E, and the isolated compound was tested in vitro against the MCF-7 cell line, and its IC50 was calculated. LD50 of cucurbitacin-E was estimated in mice, and its protective activity against DMBA-induced cancer in mice was studied. Breast cancer induction was done by a single-dose subcutaneous administration of DMBA (50 mg). Plasma ALT, AST, ALP, and LDH, as well as GSH, SOD, GPx, MDA, TNF-α, IL-6, and tumor suppressor P53 assays, were used to assess cucurbitacin-E's capacity to protect the liver and breast against DMBA-induced toxicity. Moreover, by assessing the gene expression of tumor suppressor genes (BRCA 1 and 2) and conducting histopathological analysis, the suppressive effect of cucurbitacin-E was examined.

The IC50 value of cucurbitacin-E against MCF-7 cell lines equals 72.15 ± 0.64 µg/ml. LD50 of cucurbitacin-E given orally in adult mice is equal to 1200 mg/kg b.w. The levels of plasma ALT, AST, ALP, and LDH were decreased significantly in DMBA-treated mice when administered with cucurbitacin-E at 1/50 LD50 (24 mg/kg/b.w.) and 1/20 LD50 (60 mg/kg/b.w.). In breast tissue, the levels of GSH, SOD, GPx, and P53 were significantly increased, as were decreased levels of TNF-α, IL-6, P53, and MDA. Conversely, there was a downregulation in the mRNA expression levels of BRCA1 and BRCA2. The histopathological analysis revealed that cucurbitacin-E management improved the tissue architecture of breast tumors.

These findings demonstrate the ability of cucurbitacin-E to inhibit cancer cells in the rat breast by controlling oxidative stress and inflammatory biomarkers, as well as downregulating the mRNA expression levels of BRCA1 and BRCA2.