Current Bioactive Compounds - Volume 19, Issue 2, 2023

Background: Glodok fish (Boleophthalmus boddarti) was identified to contain bioactive compounds such as steroids, terpenoids, bufadienolid, carotatoksin, and corticosteroids. These compounds benefit human life, and Lampung coastal communities consume the fish to cure asthma. Various processing methods, such as frying, are used to prepare the fish. The frying process can damage vitamins, proteins, and bioactive compounds. However, there is no data regarding the effect of using different temperatures and times on changes in the bioactive content of the fish. Methods: Sampling was conducted around the mouth of Musi River, South Sumatra. The stages consisted of the preparation process and treatment using 9 variations of temperature and frying time, sample extraction, and bioactive compounds' content analysis by GC-MS. Results: The results showed that the bioactive compounds consisted of corticosteroids, steroids, carotenoids, monoterpenoids, sesquiterpenoids, and triterpenoids. Conclusion: Variations in the treatment resulted in cholesterol of the steroid group in the highest treatment at 14.36% and the loss of betamethasone acetate compounds in the corticosteroid by 0.07%.

Background & Aims: The incidence of cardiovascular disease in climacteric women has increased, becoming the main cause of death in mature women. The use of phytoestrogens, isoflavones, and lignans derived from soy and flaxseed can be natural alternative treatments for this phase of life. This study investigates the utility of isoflavones and lignans derived from soy and flaxseed as natural alternatives to pharmaceuticals to alleviate the symptoms of menopause. Methods: A clinical, prospective, randomized, blind, placebo-controlled trial was performed. Forty- eight women aged 40 to 65 years were divided into two groups, Phytoestrogen (PHY), which received a cereal bar containing isoflavones and lignans for 90 days, and Placebo (PLA), which received expanded rice flake bar. The sociodemographic, clinical, anthropometric data, blood pressure (BP) measurements, and biochemical and hormonal tests were performed. Results: Forty-three women were included in this study (PHY=21 and PLA=22). There was a significant reduction in diastolic BP in the PHY group after the intervention (p<0.001). The frequency of BP fluctuations in the PHY group significantly decreased to 23.8% after the intervention period (p=0.027), with no significant differences for the other indicators studied. Conclusion: The combination of phytoestrogens showed a trend in reducing the blood pressure of climacteric women. However, no significant changes in cardiovascular risk factors were observed.

Background: An alkylating agent named cyclophosphamide (CP) is an immunosuppressant used in the therapy of rheumatoid arthritis and various cancers. The combination of curcumin and quercetin was evaluated for antioxidant activity against CP-induced renal oxidative stress in Wistar rats. Methods: A prophylactic treatment using a combination of curcumin and quercetin is given to the rats at 80 mg/kg and 200 mg/kg (b.w.) of the oral dose administered before a single injection of CP at 200 mg/kg intra-peritoneally (i.p.). The effects of curcumin and quercetin combination on CPinduced nephrotoxicity were investigated using the assay of oxidative stress biomarkers, serum kidney toxicity markers, and histopathology of kidney tissue. Result: A single dose of CP enhanced the malondialdehyde (MDA), creatinine, blood urea nitrogen (BUN) level and reduced body weight indices (OBWI), hematological parameter, glutathione (GSH) content. The oral administration of curcumin and quercetin was caused by a substantial reduction of the MDA, creatinine, and BUN level and increased the OBWI, hematological parameter, and GSH content. Conclusion: The present findings suggest that curcumin and quercetin combination has a prominent role against CP-induced renal injury.

Background: Putoria calabrica is a common Mediterranean plant used topically in folk medicine for medical purposes. The aim of this study is to evaluate the in vitro antioxidant, antibacterial, and antihemolytic properties of Putoria calabrica leaf extracts. Methods: Total phenol content (TPC), total flavonoid content (TFC), and condensed tannins content (CTC) were determined spectrophotometrically. The antioxidant activity was tested using TAC, DPPH, ABTS, and FRAP assays. Agar diffusion method was used to determine the antimicrobial activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans. Anti-hemolytic activity was evaluated by the measurement of erythrocytes turbidity and extracellular hemoglobin concentration using the AAPH method. Results: Methanol was the optimal solvent to extract the bioactive components with the highest extraction yield (30.11 ± 0.42%), TPC (142.11 ± 4.04 mg GAE/g dry extract) and TFC (29.16 ± 0.99 mg QrE/g dry extract). In terms of antioxidant activity, methanol extract was the most effective against ABTS free radical (IC50 = 5.02 ± 0.13 mg/ml) and FRAP (A0.5 = 2.91 ± 0.09 mg/ml). While, acetone extract showed the highest TAC (214.05 ± 8.74 mg GAE/g dry extract) and DPPH scavenging activity (IC50 = 1.94 ± 0.02 mg/ml). The strongest antimicrobial effect at a concentration of 10.24 mg/well was observed with acetone extract against P. aeruginosa (22.52 ± 0.60 mm) and C. albicans (17.33 ± 0.41 mm). While, methanol extract was the most active against S. aureus (17.31 ± 0.98 mm). Aqueous extract showed a good capacity to protect erythrocytes from oxidative damage by preventing their hemolysis and the oxidation of hemoglobin induced by AAPH. Conclusion: P. calabrica leaves hold great importance as a source of therapeutic bioactive compounds.

Background: The number of life-threatening diseases like “Candidiasis” is rapidly increasing worldwide. The effective management of the disease is indeed a great challenge for the clinician. Objectives: In an approach to developing effective antifungal compounds for growing fungal diseases, the present study was conducted to investigate the antifungal activity of selected medicinal plants collected from district Mardan. Methods: Vitis vinifera (Grapes), Lawsonia inermis (Henna), Millettia ovalifolia (Moulmein rosewood), Azadirachta indica (Neem), and Mentha arvensis (Mint). Methanolic extracts of these plant leaves were used against C. albican by using the Disc diffusion susceptibility method. Phytochemical analysis of methanolic plant extracts was then carried out using (High-Performance Liquid Chromatography) HPLC. Results: The result obtained showed that methanolic extract of V. vinifera shows 4, 5, 7 and 9mm zone of inhibition at 2,4,6 and 8μg/ml respectively, followed by L. inermis with a significant antifungal property. While A. indica showed less activity against C. albican at 4mm and 7mm concentrations. No effective antifungal properties were shown by M. ovalifolia and M. arvensis. Conclusions: These selected medicinal plants and their derived compounds could be a significant source of antifungal agents.

Background: Linum usitatissimum is widely used in traditional medicine for the treatment of inflammation, and cardiovascular and respiratory diseases. Methods: Acute oral toxicity and anti-inflammatory and analgesic effects of total alkaloid extract from Linum usitatissimum seeds (ALU) were investigated in vivo. Xylene-induced ear edema was used to determine the anti-inflammatory effect, and acetic acid-induced writhing, formalin-induced paw licking, and tail-immersion tests were used to investigate the analgesic activity. Results: Oral administration of ALU (50, 100, and 200 mg/kg) produced anti-inflammatory and analgesic effects. ALU significantly diminished the edema induced by xylene. ALU also significantly reduced the abdominal construction induced by acetic acid. Furthermore, ALU also inhibited responses in both phases of formalin-induced paw licking and increased the reaction time of mice in the tail-immersion test. Conclusion: These findings suggest the total alkaloid extract from Linum usitatissimum seeds presents significant anti-inflammatory and analgesic effects on chemical, behavioral models of inflammation and nociception in mice.

Background: Inflammation is a natural biological response of the body tissues to harmful stimuli, such as damaged cells, irritants or pathogens, and it is a protective response involving blood vessels, immune cells and molecular mediators. Activator Protein-1 (AP-1) is a dimer composed of both homo and hetero dimers with jun and fos subfamilies. The heterodimer cfos-cjun complex is upregulated in several inflammatory diseases such as asthma, rheumatoid arthritis, psoriasis etc. Since ancient times, several plants have been used as anti-inflammatory sources. Withania somnifera is a vital plant having well-documented anti-inflammatory properties. In this study, the phytochemicals of Withania somnifera are used to study the inhibitory effect on the inflammatory mediator AP-1 factor. Objective: Determining the inhibitory effect of Withania somnifera phytochemicals against AP-1 factor (cfos-cjun complex). Methods: In the present study, the phytochemicals of Withania somnifera were retrieved from the IMPPAT database. All the retrieved molecules were employed to screen in-silico pharmacological properties using in-silico tools such as SwissADME and ProTox II. Further, molecular interactions of receptors and ligands were carried out by the Autodock 4.1 tool. Results: A total of 90 phytochemicals of Withania somnifera were subjected to the IMPPAT database. Among those, 21 Phytochemicals showed the appropriate drug similarity characteristics. The Autodock 4.1 tool was used to analyse the binding effect of these 21 phytochemicals. Withanolide E and Withanolide J molecules showed excellent inhibitory action compared to others. The interaction pattern showed that SER and ARG amino acids participate in the formation of drug hydrogen bonds. Conclusion: Among the 90 phytochemicals of Withania somnifera, only two molecules showed potential ligand binding ability. Further, in-vitro studies may validate the findings.

Background: Chrysopogon zizanioides Roberty root extracts have documented amylase and α-glucosidase inhibition, hepatoprotection, antioxidant, antimicrobial, antihyperglycemic, antidepressant, and antitubercular properties but lack ample reports on health care applications of purified phytoconstituents. Objective: To study the inhibitory properties of phytosterol eluate against cholesterol esterase (CEase) and diabetic foot ulcer (DFU) causing pathogens (clinical isolates). Methods: The shake flask method was adopted to extract the phytoconstituents and standard spectrophotometric assays were carried out to quantify phytosterol constituent and CEase inhibitory activity. Central composite design (CCD) based response surface methodology (RSM) was adopted to observe the improvement of phytosterol constituent and CEase inhibitory activity. Two dimensional preparative thin layer chromatography (2D PTLC) technique was executed to purify the phytosterol content and HRLC-based APCI – Q-TOF/ MS² analysis was done to predict the phytosterol structures. Standard disc assay was used to explore the inhibitory effect of extract and purified phytosterol content against DFU-causing pathogens. Results: The crude extracts exhibited a moderate CEase inhibitory activity (Ethylacetate: 67 ± 3.2%) and appreciable phytosterol content (Acetone: 11.24 ± 0.52 mg/g tissue). CCD based RSM has improved the CEase inhibitory activity (Ethylacetate: 96.56 ± 1.1%) as well as the phytosterol content (6.45 ± 0.5 mg/g tissue). The purified phytosterol fractionate (PTLC eluate) was found to contain stigmasterol related novel phytosterol and revealed a significant CEase inhibitory activity (81 ± 2.5 %; Ki: 54.89 μg) with mixed type inhibition. Conclusion: Both the extract and the PTLC eluate have recorded a substantial control over DFU causing bacterial pathogens.

Malaria is one of the deadliest vectors of spreading diseases, which causes enormous health concerns in the tropical world, especially in sub-Saharan countries. Despite tremendous efforts around the globe, malaria is one of the leading causes of death in those areas. In addition, the appearance of resistance to the currently available drugs is making the situation more alarming, which highlights the urgency for continued research to stay prepared, and evaluation of natural products could be the best approach in this direction. In drug discovery, nature plays an important role. Most currently marketed drugs are either modified or non-modified or synthetic compounds with a natural product as a pharmacophore. Even in the case of antimalarial drugs, starting from the discovery of quinine to the currently utilized artemisinin, most of the effective antimalarial drugs are derived from terrestrial natural sources. However, although the ocean constitutes almost 75% of the Earth, the exploration and discovery of antimalarial drugs from marine sources are minimal. This comprehensive review assimilates antimalarial natural products from marine sources in recent times. Natural products from oceanic microbes and their plants, in particular, are regarded sources for the review.