The resistance of cancer and Helicobacter pylori to several drugs reflects a worldwide problem, and it has been the intention of numerous researchers to overcome this problem. Thus, in this study, Acacia nilotica fruits were subjected to HPLC analysis to detect their phenolic compounds and flavonoids. Moreover, A. nilotica‘s anti-H. pylori activity and its inhibitory activity against human hepatocellular carcinoma (HepG-2 cells) were reported. Various compounds with different concentrations, such as ferulic acid (5451.04 µg/mL), chlorogenic acid (4572.26 µg/mL), quercetin (3733.37 µg/mL), rutin (2393.13 µg/mL), gallic acid (2116.77 µg/mL), cinnamic acid (69.72 µg/mL), hesperetin (121.39 µg/mL) and methyl gallate (140.45 µg/mL), were detected. Strong anti-H. pylori activity at 31 mm was reported, compared to the positive control of the 21.67 mm inhibition zone. Moreover, the MIC and MBC were 7.8 µg/mL and 15.62 µg/mL, respectively, while the MIC and MBC of the positive control were 31.25 µg/mL. The concentration of MBC at 25%, 50% and 75% reflected H. pylori’s anti-biofilm activity of 70.38%, 82.29% and 94.22%, respectively. Good antioxidant properties of the A. nilotica flower extract were documented at 15.63, 62.50, 250 and 1000 µg/mL, causing the DPPH scavenging percentages of 42.3%, 52.6%, 65.5% and 80.6%, respectively, with a IC50 of 36.74 µg/mL. HepG-2 cell proliferation was inhibited (91.26%) using 500 µg/mL of flower extract with an IC50 of 176.15 µg/mL, compared to an IC50 of 395.30 µg/mL used against human normal melanocytes. Molecular docking was applied to investigate ferulic acid with the H. pylori (4HI0) crystal structure to determine the best binding mode that interacted most energetically with the binding sites. Molecular docking indicated that ferulic acid was a proper inhibitor for the 4HI0 protein enzyme of H. pylori. A low energy score (−5.58 Kcal/mol) was recorded as a result of the interaction of ferulic acid with the residue’s SER 139 active site caused by the O 29 atom, which was important for its antibacterial activity.

https://www.mdpi.com/2079-4983/14/4/237/pdf?version=1682067070

Pharmacological Evaluation of Acacia nilotica Flower Extract against Helicobacter pylori and Human Hepatocellular Carcinoma In Vitro and In Silico

The synthesis of two new copolymer conjugates of methoxyoligo(ethylene glycol)methacrylate MPEGMA and betulin methacrylate BM was developed via RAFT polymerization. The molar content of BM units was equal to 9–10 and 13–16 mol%, respectively (HPLC, 1H and 13C NMR); molar weights were equal to 75000–115000. CeO2 NPs as a component of the hybrid material were synthesized for the preparation of the composition with copolymer conjugates of MPEGMA and BM. We showed a significant increase in G6PDH and GR activities by 21–51% and 9–132%, respectively, which was due to the increase in NADPH concentration under the action of copolymers in vitro. The actions of copolymers and CeO2 NPs combination were stronger than those of the individual components: the SOD activity increased by more than 30%, the catalase activity increased dose-dependently from 13 to 45%, and the GR activity increased to 49%. The maximum increase in enzyme activity was observed for the G6PDH from 54% to 151%. The MDA level dose-dependently increased by 3–15% under the action of copolymers compared with the control, and dose-dependently decreased by 3–12% in samples containing CeO2 NPs only. CeO2 NP–copolymer compositions can be used for the design of new biomimetic medical products with controlled antioxidant properties.

/pdf/antioxidant-activity-of-new-copolymer-conjugates-of-3br2h4uq.pdf

Antioxidant Activity of New Copolymer Conjugates of Methoxyoligo(Ethylene Glycol)Methacrylate and Betulin Methacrylate with Cerium Oxide Nanoparticles In Vitro

Acacia nilotica stem bark extract ameliorates obesity, hyperlipidemia, and insulin resistance in a rat model of high fat diet-induced obesity

Development of betulin as phytochemical reference standard for the analysis of Hygrophila schulli plant by a validated high-performance thin-layer chromatography method

Betulin has a broad spectrum of biological and pharmacological properties, such as anticancer, antibacterial, antifungal, and antiviral. Unfortunately, the low bioavailability makes it difficult to use in medicine. The introduction of a triazole ring to the betulin structure leads to the obtainment of new compounds with higher activity and better bioavailability. The title compound was obtained from the triazole derivative of betulin by conversion of the hydroxyl group to an ester moiety in the Steglich reaction. The chemical structure of the hybrid was characterized by nuclear magnetic resonance (1H NMR, 13C NMR, HSQC, HMBC) and HRMS spectroscopy.

/pdf/28-1-3-propionyloxy-propyl-1h-123-triazol-4-yl-19p5s3y8.pdf

28-[1-(3-(Propionyloxy)propyl)-1H-1,2,3-triazol-4-yl]carbonylbetulin

Abstract Medicinal plants are in use of humankind since ancient and still they are playing an important role in effective and safer natural drug delivery systems. Acacia nilotica (native of Egypt) commonly known as babul belongs to family Fabaceae, widely spread in India, Sri Lanka and Sudan. Being a common and important plant, using in many ways from fodder (shoots and leaves to animals) to dyeing (leather coloration) to medicine (root, bark, leaves, flower, gum, pods). The present study is focused on investigating the natural chemistry and important biological activities of the plant. Employing bioassay guided fractionation coupled with TLC and column chromatography, a pure fraction named AN-10 was isolated from ethyl acetate fraction of crude methanol extract which identified as “Betulin (Lupan-3ß,28-diol)” by Liebermann-Burchard test and structure elucidation by UV–Vis, NMR and MS techniques. A battery of in vitro biological assays for antioxidant, anti-inflammatory and anticancer were performed and betulin showed excellent potential in all assays. It was found that the inhibitory potential in all assays were dose dependent manner and after a range of concentration, the activities get leveled off with no further increase in activity. 

/pdf/isolation-characterization-and-biological-activities-of-2jyoybd7.pdf

Rajbir Singh

Papers

Isolation, characterization and biological activities of betulin from Acacia nilotica bark