Current Bioactive Compounds - Online First

Age-related Alzheimer's disease is a common neurodegenerative disease. The number of Alzheimer's patients worldwide is expected to reach approximately 150 million by 2050. Breast cancer is one of the most common cancers in females, and its prevalence rises each year. Annually, worldwide, almost 500,000 women pass away due to breast cancer. Current treatments for Alzheimer’s disease and cancer aim to stop or slow the progression of the disease. Developing more effective methods of treatment has become a global effort. Many scientists from around the world are busy in finding effective treatment solutions for Alzheimer’s disease and cancer. The metal-ligand chemistry shows a variety of applications, including physiological and pharmacological activities.

The green and efficient synthesis of coordination complexes of novel azo-Schiff
base ligand 4-[(E)-(5-chloro-2-hydroxy-3-{(E)-(3-nitrophenyl)diazenyl}benzylidene)amino]-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one was performed by grinding technique. Further, metal salts were introduced to this azo-Schiff base ligand, and metal complexes were synthesized. These synthesized products were characterized by ¹H-NMR spectra, mass spectra, FTIR spectra, electronic spectra, elemental analysis, thermal analysis, X-ray powder diffraction, molar conductivity, etc., and their anti-Alzheimer’s, anticancer, and antimicrobial activities were assessed by MTT assay and disc diffusion method, respectively.

The structures of the azo-Schiff base ligand and its metal complexes were confirmed by using various spectroscopic techniques. In the biological activity study, many complexes showed higher inhibition than the standard reference drug.

The synthesized metal complexes exhibited higher biological activities than the azo-Schiff base ligand. All metal complexes, except for some, served as anti-Alzheimer’s and anticancer agents.

Nowadays, medicinal herbs and their phytochemicals have emerged as a great therapeutic option for many disorders. However, poor bioavailability and selectivity might limit their clinical application. Among all approaches, phyto-phospholipid complexes (named phytosomes) have appeared to be a great method to overcome the problems. With the new developments in drug delivery technologies, anticancer drugs ranging from hydrophilic macromolecules to lipophilic drugs can be administered via phytosomes to treat cancer.

In the present review, various drugs targeted by phytosomes to treat varied forms of cancer, like breast cancer, pancreatic cancer, lung cancer, colon cancer, prostate cancer, etc, are discussed.

In this review, recent literature covering phytosomes to treat various forms of cancer, patent applications, and clinical trials involving phytosomes employed to cure mainly cancer are covered.

Phytosomes have proved their potential to cure cancer. They increase the bioavailability of the drug by site-specific drug delivery and can reduce the side effects/- toxicity associated with anticancer drugs and also sustain the release of drugs.

The potential of phytosomes to carry the drug may unclutter novel ways for therapeutic intercessions in various tumors.

Alkaloids are naturally occurring nitrogen-containing chemicals in plants, fungi, and mammals. These chemicals protect plants from herbivores and pathogens and have a wide range of biological actions, making them useful in pharmacology and medicine. Alkaloids offer potent therapeutic effects, including antifungal, local anaesthetic, anti-inflammatory, antineoplastic, pain-killing, neuropharmacological, and antibacterial properties. Morphine is commonly used to relieve pain, quinine for malaria, and vincristine for cancer. Because of their considerable therapeutic potential, alkaloids have become a focus of study in the development of medications to treat infections, inflammation, neurological diseases, and cancer.

The primary goal of this research is to isolate, purify, and validate amide alkaloids from the seeds of PIPER guineense, a West African species while contrasting traditional alkaloid extraction methods with novel techniques such as molecular distillation, membrane separation, molecular imprinting, and high-speed counter-current chromatography. The study aims to address the challenges posed by conventional methods' high cost and low yield, by providing insights into more efficient, scalable, and advanced technologies for alkaloid extraction and purification, which are critical for the advancement of complementary and Chinese medicine.

The seeds of Piper guineense were extracted using a Soxhlet device with methanol as the solvent. The extracted extract was purified and separated into amide alkaloids using column chromatography. Thin-layer chromatography (TLC) was used to confirm the presence of alkaloids. The isolated compounds were examined and characterized using an array ofspectrum methods, including Mass spectra, FTIR, and NMR spectroscopy. Natural substances with nitrogen in the exocyclic outlook, such as mescaline, serotonin, & dopamine, were recognized as amines rather than alkaloids in the investigation.

The synthesized chemicals, including Piperine, Wisanine, Piperlonguminine, Propiverine, and Piperidine, were satisfactorily characterized using FTIR, NMR, mass spectrometry, and HPLC. The FTIR spectra showed distinct peaks whichwere consistent with conventional standards, demonstrating the effective synthesis. NMR research, performed with a BRUKER AVANCE NEO-500MHz spectrometer, revealed information on the chemical surroundings of the protons, confirming the molecular structure. Mass spectroscopy was done using a MICROMASS Q-TOF micro-mass spectrometer to precisely measure molecular weights and identify fragmentation patterns, verifying the existence of important functional groups and assuring the structural integrity of the compounds.

This work effectively extracted, purified, and characterized numerous amide alkaloids from Piper guineense seeds using modern chromatographic and spectroscopic methods. The compounds, which included Piperine, Wisanine, Piperlonguminine, Propiverine, and Piperidine, were validated using FTIR, NMR, mass spectroscopy, and HPLC to ensure structural integrity and composition. The study reveals the efficacy of contemporary extraction and analytical procedures, offering useful insights into how to improve alkaloid purification processes. These discoveries advance our understanding of alkaloid chemistry and have the potential for future uses in alternative medicine and pharmaceutical research.

In recent years, chemical and biological studies have explored medicinal plants to develop new treatments for oxidative stress, inflammation, and diabetes.

This study aims to characterize for the first time the chemical composition of the hexane extract from the roots of Salvia argentea using GC and GC/MS techniques. We also isolated its major compound and evaluated its biological activities, including its antioxidant, anti-inflammatory, antidiabetic, and hemolytic effects, as well as the combination of this major compound with reference drugs.

Antioxidant activity was assessed using DPPH, β-carotene, and phosphomolybdenic tests. The anti-inflammatory effect was measured by the egg albumin denaturation method and protein denaturation inhibition. The antidiabetic activity was determined by evaluating the inhibition of α-amylase, with acarbose as a positive reference. The combined effect of aethiopinone with standards was also studied to reduce the minimum effective dose and minimize side effects.

The hexane extract of Salvia argentea is mainly composed of aethiopinone (53.3%) and ferruginol (20.5%). aethiopinone was isolated and identified using spectroscopic methods, including ¹H NMR, ¹³C NMR, and IR. The biological activity assessment showed that hexane extract and aethiopinone had promising antioxidant, anti-inflammatory, and antidiabetic properties. In addition, synergistic effects were observed when aethiopinone was combined with positive references, resulting in a significant reduction of the required minimum inhibitory concentrations. The human erythrocyte toxicity assessment showed that hexane extract and aethiopinone induced very low hemolysis levels, reaching 24.18% and 31.13%, respectively, at high concentrations of 2000 μg/mL.

Further research is needed to confirm their therapeutic effects and assess their potential for use in the pharmaceutical industry.

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.