Search Results (21)

Background/Objectives: Triple-negative breast cancer (TNBC) is one of the most aggressive breast cancer subtypes and remains associated with limited therapeutic options and high systemic toxicity from conventional chemotherapy. Ipomoea pes-caprae is a coastal medicinal plant traditionally consumed in Mexico for inflammatory and renal disorders and contains bioactive metabolites with reported antioxidant and pharmacological properties. However, its antitumoral activity and systemic safety profile remain poorly understood. This study aimed to characterize the phytochemical composition, antioxidant capacity, antitumoral activity, and toxicity of a traditionally prepared aqueous infusion of I. pes-caprae leaves (IPCAE). Methods: IPCAE was characterized using phytochemical screening and complementary instrumental analyses. Antioxidant activity was evaluated using the DPPH assay. A randomized preclinical study was performed in mice bearing MDA-MB-231 xenografts treated with IPCAE, cisplatin, or saline control. Results: The infusion showed measurable antioxidant activity (72.25 ± 1.25% DPPH inhibition at 1 mg/mL) and a total polyphenol content of 7.29 µg/mg gallic acid equivalents. Phytochemical screening revealed abundant flavonoids and reducing sugars, with moderate saponin content. In vivo, IPCAE produced only a transient and non-significant trend toward slower tumor progression compared with control (p = 0.214) and cisplatin (p = 0.377). However, marked systemic toxicity was observed, including severe thoracic dermal lesions in 40% of animals and 70% mortality by day 15. Survival was significantly reduced compared with control and cisplatin groups (p < 0.001). Conclusions: Although IPCAE exhibited antioxidant activity, no statistically significant antitumoral effect was observed under the evaluated conditions. Furthermore, repeated oral administration resulted in marked systemic toxicity, characterized by visible dermal lesions, clinical deterioration, and increased mortality. Therefore, the present findings do not support the use of the evaluated crude preparation as an anticancer intervention. Future studies should focus on detailed toxicological characterization, bioassay-guided fractionation, dose optimization, and identification of the individual metabolites responsible for the observed biological effects. The antioxidant activity demonstrated in this study should be interpreted independently from antitumoral activity, as no causal relationship between these findings was established. Full article

Amaranth proteins have been associated with various health benefits, including anticancer activity. This study aimed to evaluate the cytotoxic effect of proteins and peptides derived from Amaranthus hypochondriacus. A crude extract (CE) and protein fraction (PF) were obtained; peptides were produced by enzymatic hydrolysis, yielding one sample > 30 kDa (P > 30 kDa) and another < 30 kDa (P < 30 kDa). Protein, phenolic, and antinutritional compound content were determined, along with antioxidant capacity and cytotoxic activity against MDA-MB-231 and SiHa cells. CE exhibited the highest protein content of 182.6 mg/g, total phenols 129.40 mg GAE/g, and antioxidant capacity by both methods, 104.50 µM TEAC/g for ABTS•+ and 75.62 µM TEAC/g for DPPH•. PF showed the greatest concentration of saponins and lectins, 80 HU/mg and 60.30 HA/mg, respectively. PF displayed the strongest cytotoxic effect at 72 h in both cell lines, with IC₅₀ of 44.98 µg/mL for MDA-MB-231 cells and 69.24 µg/mL for SiHa cell line. Transmission electron microscopy (TEM) revealed severe structural damage induced by PF in both cell lines. In conclusion, PF from Amaranthus hypochondriacus seeds showed the greatest in vitro cytotoxic effect against both cancer cell lines, principally in MDA-MB-231 cells. Full article

Kalanchoe daigremontiana, a succulent herbaceous plant in the Crassulaceae family from Madagascar, has gained global popularity as an ornamental and medicinal species. This review examines the traditional uses, phytochemical composition, biological properties, toxicological aspects, and regulatory challenges of K. daigremontiana. The traditional medicinal uses of its leaves and roots include treating burns, rheumatic disorders, hypertension, diabetes, kidney pain, diarrhea, cough, fever, gastric issues, anxiety, inflammation, and cancer. Chemical compounds identified include phenolic acids, flavonoids, tannins, alkaloids, glycosides, saponins, sterols, terpenes, and fatty acids, with phenolic compounds and bufadienolides being predominant. In vitro studies of the crude extracts, bufadienolide-rich fractions, and isolated compounds have shown antioxidant, antibacterial, antifungal, antiviral, antiparasitic, anthelmintic, anti-inflammatory, anticoagulant, anti-aging, cytotoxic, antitumoral, and antiproliferative properties. In vivo studies have demonstrated hepatoprotective, skincare, and cardiac-glycoside-like effects. While crude extracts and bufadienolide-rich fractions have shown toxic effects in 2-week-old chicks, guinea pigs, and Artemia salina, no toxicity has been reported in goats, broiler chickens, laying hens, or human erythrocytes. Although K. daigremontiana-based products are commercially available as dietary supplements with various health claims, these lack scientific validation. Despite the potential pharmaceutical applications of K. daigremontiana, further research is needed to determine its effects, dosage, mechanisms, long-term safety, and side effects, with clinical studies essential to validate its therapeutic potential. Full article

Pharmacological relevance: Ethnic people residing in the Chittagong Hill Tracts (CHTs) of Bangladesh use Pouzolzia sanguinea to alleviate flatulence, for menstruation, inflammation, insomnia, and analgesia. However, there is no scientific evidence regarding the bioactivity of these plants. Aim: This study aimed to isolate bioactive fractional compounds from Pouzolzia sanguinea (IFCPS) crude extract to assess the anti-inflammatory, analgesic, and anxiolytic activities. Materials and Methods: Preparative TLC-bioautography and silica gel two-stage column chromatography were used to isolate bioactive fractional compounds from P. sanguinea methanol crude extracts. The anti-inflammatory, analgesic, and anxiolytic activities of extracts and IFCPS were studied by inhibiting protein denaturation, acetic acid-induced writhing, Eddy’s hot plate, field cross, and hole cross methods. Results: The dried crude extract’s chemical analysis revealed alkaloids, flavonoids, terpenoids, saponins, vitamin C, and tannins. Nine single isolated fractional compounds (IFC₁PS to IFC₉PS) were isolated through TLC. Among these, IFC₂PS exhibited (p ˂ 0.01) the most potent anti-inflammatory activity in the inhibition of protein denaturation studies (70.51%), which was slightly lower than acetyl salicylic acid (82.29%), at160 µg/mL. This inhibitory effect occurred in a dose-dependent manner. IFC₂PS exhibited the most potent peripheral analgesic and moderate central analgesic effects compared to the standard. In contrast, IFC₁PS showed moderate effects in both areas. IFC₈PS showed superior anxiolytic activities compared to crude extracts and other IFCPS. Conclusions: Out of the nine fractional compounds isolated, the IFC₂PS reduced pain and inflammation, whilst IFC₈PS exhibited anxiolytic activities. This is the first comprehensive study demonstrating the anti-inflammatory, analgesic, and anxiolytic effects of crude extracts and isolated fractional compounds from the whole plant of P. sanguinea, which may have immediate experimental and clinical applications. Full article

A gradual surge in the population on Earth has increased the demand for food. Various synthetic materials have been used for food packaging for a long time. These materials are contaminating our environment and disrupting human life and that of other species. This study was conducted to minimize the impact of the pollution caused by using plastics for conventional packaging. A green approach to synthesizing packaging material that prevents food contamination with improved mechanical properties was adopted. Firstly, extracts were obtained from grapes and tomatoes and dissolved into four different solvents, i.e., de-ionized water, dichloromethane, ethyl acetate, and n-hexane. Three different extract solutions were made in de-ionized water, varying the fraction of the extract and de-ionized water. The extracts were then tested for the presence of various phytochemicals. The solutions were then combined with cyclodextrin, starch, alginate, and polyvinyl alcohol, all of which are biodegradable, non-cytotoxic, and pocket-friendly. Calcium chloride was also added because it acts as a firming agent and a desiccant. This resulted in the formation of a total of six membranes with four different solvents. These membranes had varying degrees of biodegradability and antibacterial properties. Various phytochemicals, such as saponins, flavonoids, terpenoids, carotenoids, tannins, phenols, and steroids, were found in the fruit extracts. These phytochemicals act as anti-microbial and anti-fungal agents. Out of the six different membranes that were synthesized, the membrane with a 7:3 composition of crude extract to de-ionized water showed the best results for use as a packaging material, as it showed the best antibacterial properties and good reported biodegradability. The FTIR results for this membrane showed bands at around 3500 cm⁻¹, indicating the presence of -OH and -NH functionality since these bands overlap and cannot be distinguished at this position. The shoulder band indicates the presence of carboxylic acid -OH. Integrating biopolymers with fruit extracts enhances the nutritional value of food and provides an eco-friendly and cost-effective approach to packaging material synthesis. The synthesized membranes are cost-effective as they contain fruit extracts from grapes and tomatoes; starch; and cyclodextrin. The extracts obtained from the fruits were inexpensive, as 300 mL of extract cost around 300 Rs. The synthesized membranes had functional advantages such as biodegradability and providing an enhanced shelf life to food products. Hence, they reduce the losses caused by food spoilage. Another driver of their cost effectiveness is that they can reduce waste disposal costs on the one hand and environmental pollution on the other hand. Full article

Panax ginseng sprouts (GSs) have attracted attention as functional resources due to their short cultivation time and enriched ginsenoside content. This study aimed to evaluate the bioactivities of GSs cultivated using kelp fermentates (KF) as a nutrient solution under a smart-farming system. Ginsenoside-enriched extract (FGE), its water-soluble saponin fraction (WFGE), and 70% ethanol-soluble saponin fraction (EFGE) were analyzed for phytochemical contents and biological activities. The EFGE exhibited the highest levels of eight major ginsenosides, including Rg1, Rb1, Rc, Rg2, Rb2, Rd, Rf, and F2. Total phenolic and flavonoid contents were significantly higher in KF-treated ginseng and their crude saponin fractions, with EFGE showing the highest values. WFGE and EFGE indicated strong antioxidant activity through ABTS radical scavenging assays. In LPS-stimulated RAW264.7 macrophages, all extracts significantly inhibited nitric oxide production and downregulated IL-1β, IL-6, iNOS, and COX-2 expression. Moreover, UVB-irradiated human fibroblasts (Hs68) treated with KF-derived fractions showed increased cell viability, enhanced procollagen synthesis, and reduced MMP-1 and MMP-3 expression. These effects were associated with suppression of MAPK/AP-1 signaling. In conclusion, GSs cultivated with KF exhibit notable antioxidant, anti-inflammatory, and anti-photoaging activities, suggesting their potential as natural ingredients for skin health applications. Full article

Plants serve as reservoirs of bioactive compounds endowed by nature, rendering them promising subjects for investigating chemical diversity. Despite their potential, much remains untapped, whether in standardized extracts or isolated pure compounds. This unexplored terrain has paved the way for significant discoveries in pharmaceuticals. Notably, research has delved into the medicinal properties of Mallotus philippensis, a prominent plant in South Asia. Employing meticulous extraction techniques such as maceration, the fruit of this plant underwent initial antimicrobial screening, revealing encouraging results. Subsequent fractionation of the plant’s extracts via liquid–liquid extractions, utilizing dichloromethane and absolute ethanol, facilitated further analysis. Evaluating these fractions for antibacterial activity demonstrated efficacy against various pathogenic microorganisms, particularly Pseudomonas aeruginosa and Escherichia coli, notably by the ethanolic and dichloromethane extracts. Furthermore, a comprehensive phytochemical analysis unveiled the presence of alkaloids, flavonoids, saponins, glycosides, phenols, and tannins. An assessment of the extracts’ antioxidant potential via the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay showcased significant activity, with a radical scavenging rate of 97%. This underscores the significance of utilizing fruit remnants, which are often rich in valuable chemical constituents yet commonly discarded, thereby adding value to both the species and the environment. Further investigation focused on the composition of Mallotus philippensis fruit, encompassing volatile and non-volatile metabolites through HPLC-MS analysis. Additionally, this study introduced the application of ionic liquid-loaded polysulfone microcapsules to enrich target constituents from crude extracts. An exploration of the key separation conditions, results, and recycling performance of these microcapsules provided insights for future research endeavors. Overall, this comprehensive study of Mallotus philippensis fruit extracts establishes a foundation for the ongoing exploration and development of this medicinal plant. Full article

Malaria remains a life-threatening health problem and is responsible for the high rates of mortality and morbidity in the tropical and subtropical regions of the world. The increasing threat of drug resistance to available artemisinin-based therapy warrants an urgent need to develop new antimalarial drugs that are safer, more effective, and have a novel mode of action. Natural plants are an excellent source of inspiration in searching for a new antimalarial agent. This research reports a systematic investigation for determining the antimalarial potential of the seeds of A. squamosa. The study shows that the crude seed extract (CSE), protein, saponin, and the oily fractions of the seeds were nontoxic at a 2000 mg/kg body weight dose when tested in Wistar rats, thus revealing high safety is classified as class 5. The oily fraction, Annomaal, demonstrated pronounced antimalarial activity with low IC₅₀ (1.25 ± 0.183 μg/mL) against P. falciparum in vitro. The CSE and Annomaal significantly inhibited the growth of P. berghei parasites in vivo with 58.47% and 61.11% chemo suppression, respectively, while the standard drug artemether showed chemo suppression of 66.75%. Furthermore, the study demonstrated that oral administration of Annomaal at a daily dose of 250 mg/kg/day for 3 days was adequate to provide a complete cure to the P. berghei-infected mice. Annomaal thus holds promise as being patient-compliant due to the shorter treatment schedule, eliminating the need for frequent dosing for extended time periods as required by several synthetic antimalarial drugs. Further studies are needed to determine the active compounds in the oily fraction responsible for antimalarial activity. Full article

Antifungal assay-guided fractionation of the methanolic crude extract of Cestrum nocturnum (Solanaceae), popular known as ‘lady of the night’, led the isolation and identification of the steroidal saponin named pennogenin tetraglycoside, which was identified for the first time in this plant species by spectroscopic means. The crude extract, fractions and pennogenin tetraglycoside exhibited mycelial growth inhibition of Fusarium solani and F. kuroshium. F. solani is a cosmopolitan fungal phytopathogen that affects several economically important crops. However, we highlight the antifungal activity displayed by pennogenin tetraglycoside against F. kuroshium, since it is the first plant natural product identified as active for this phytopathogen. This fungus along with its insect symbiont known as Kuroshio shot hole borer (Euwallacea kuroshio) are the causal agents of the plant disease Fusarium dieback that affects more than 300 plant species including avocado (Persea americana) among others of ecological relevance. Scanning electron microscopy showed morphological alterations of the fungal hyphae after exposure with the active fractions and 12 phenolic compounds were also identified by mass spectrometry dereplication as part of potential active molecules present in C. nocturnum leaves. Full article

The flowers of M. velutina were extracted with ethanol to obtain a crude extract that was consecutively extracted using n-hexane, dichloromethane, ethyl acetate and water. The crude extract and fractions were studied for the chemical composition and antioxidant and antidiabetic activities. The extracts had various phytoconstituents, namely steroids, flavonoids, tannins, saponins, alkaloids and glycosides. The aqueous extract had the highest total polyphenol (12.6 mg GAE/g extract) and total flavonoid (205.6 mg QE/g extract) content. The aqueous extract exhibited the strongest antioxidant activities in the ferric reducing antioxidant power assay (EC₅₀ = 4.0 µg/mL), reducing power assay (EC₅₀ = 78.1 µg/mL), 2,2-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid radical cation assay (EC₅₀ = 48.2 µg/mL), total antioxidant capacity assay (EC₅₀ = 8.7 µg/mL) and 1,1-diphenyl-2-picrylhydrazyl assay (EC₅₀ = 9.3 µg/mL). The aqueous extract showed the strongest inhibitory effect on the activity of α-amylase (IC₅₀ = 376.6 μg/mL) and α-glucosidase (IC₅₀ = 69.7 μg/mL). The results showed that the aqueous extract of M. velutina flowers can be a promising candidate for the control of diabetes and oxidative stress. This is the first report about the chemical components and antioxidant and antidiabetic activities of M. velutina flower extracts. Full article

The aqueous extract of Joazeiro stem bark (EJSB) and its high molecular weight fraction (HMWF) were examined as potential corrosion inhibitors of mild steel in 1 mol L⁻¹ hydrochloric acid media, using weight-loss measurements, potentiodynamic polarization curves and an electrochemical impedance spectroscopy (EIS).Varying the concentration of the inhibitors from 100 to 800 mg L⁻¹, the results show an increase in anticorrosive efficiency from 85.4 to 89.8 and 89.8 to 93.0% for EJSB and its HMWF, respectively, using the data of the gravimetric essay, and from 84.5 to 94.5 and 89.9 to 94.7% for EJSB and its HMWF, respectively, from the impedance data. The composition of the crude extract was chemically characterized by liquid chromatography-high resolution mass spectrometry. Additionally, scanning electron microscopy (SEM) and X-ray photoelectron spectroscopy (XPS) were used, respectively, to morphologically and chemically characterize the surface. Considering that the saponin molecules, the main constituent from juá, are responsible for its inhibitory action, quantum chemical calculations showed that the C67, C69 and O144 atoms likely have an important role in the process of electron-donation of saponin to metal, due to the higher values of ƒ_k⁺ and %HOMO observed on these atoms. Full article

Sea cucumbers are slow-moving organisms that use morphological, but also a diverse combination of chemical defenses to improve their overall fitness and chances of survival. Since chemical defense compounds are also of great pharmaceutical interest, we pinpoint the importance of biological screenings that are a relatively fast, informative and inexpensive way to identify the most bioactive organisms prior to further costly and elaborate pharmacological screenings. In this study, we investigated the presence and absence of chemical defenses of 14 different sea cucumber species from three families (Holothuriidae, Stichopodidae and Synaptidae) against ecological factors such as predation and pathogenic attacks. We used the different sea cucumber crude extracts as well as purified fractions and pure saponin compounds in a portfolio of ecological activity tests including fish feeding assays, cytotoxicity tests and antimicrobial assays against environmental pathogenic and non-pathogenic bacteria. Furthermore, we quantified and correlated the concentrations of sea cucumber characteristic saponin compounds as effective chemical defensive compounds in all 14 crude extracts by using the vanillin–sulfuric acid test. The initial results revealed that among all tested sea cucumber species that were defended against at least one ecological threat (predation and/or bacterial attack), Bohadschiaargus, Stichopuscholoronotus and Holothuria fuscopunctata were the three most promising bioactive sea cucumber species. Therefore, following further fractionation and purification attempts, we also tested saponin-containing butanol fractions of the latter, as well as two purified saponin species from B. argus. We could demonstrate that both, the amount of saponin compounds and their structure likely play a significant role in the chemical defense strategy of the sea cucumbers. Our study concludes that the chemical and morphological defense mechanisms (and combinations thereof) differ among the ecological strategies of the investigated holothurian species in order to increase their general fitness and level of survival. Finally, our observations and experiments on the chemical ecology of marine organisms can not only lead to a better understanding of their ecology and environmental roles but also can help in the better selection of bioactive organisms/compounds for the discovery of novel, pharmacologically active secondary metabolites in the near future. Full article

The roots of Polygala tenuifolia Wild (Polygalaceae), which is among the most important components of traditional Chinese herbal medicine, have been widely used for over 1000 years to treat a variety of diseases. In the current investigation of secondary metabolites with anti-inflammatory properties from Korean medicinal plants, a phytochemical constituent study led to the isolation of 15 compounds (1–15) from the roots of P. tenuifolia via a combination of chromatographic methods. Their structures were determined by means of spectroscopic data such as nuclear magnetic resonance (NMR), 1D- and 2D-NMR, and liquid chromatography-mass spectrometry (LC-MS). As the obtained results, the isolated compounds were divided into two groups—phenolic glycosides (1–9) and triterpenoid saponins (10–15). The anti-inflammatory effects of crude extracts, fractions, and isolated compounds were investigated on the production of the pro-inflammatory cytokines interleukin (IL)-12 p40, IL-6, and tumour necrosis factor-α in lipopolysaccharide-stimulated bone marrow-derived dendritic cells. The IC₅₀ values, ranging from 0.08 ± 0.01 to 21.05 ± 0.40 μM, indicated potent inhibitory effects of the isolated compounds on the production of all three pro-inflammatory cytokines. In particular, compounds 3–12, 14, and 15 showed promising anti-inflammatory activity. These results suggest that phenolic and triterpenoid saponins from P. tenuifolia may be excellent anti-inflammatory agents. Full article

Sea cucumbers are bottom dwelling invertebrates, which are mostly found on subtropical and tropical sea grass beds, sandy reef flats, or reef slopes. Although constantly exposed to fouling communities in these habitats, many species are surprisingly free of invertebrate epibionts and microfouling algae such as diatoms. In our study, we investigated the anti-fouling (AF) activities of different crude extracts of tropical Indo-Pacific sea cucumber species against the fouling diatom Cylindrotheca closterium. Nine sea cucumber species from three genera (i.e., Holothuria, Bohadschia, Actinopyga) were selected and extracted to assess their AF activities. To verify whether the sea cucumber characteristic triterpene glycosides were responsible for the observed potent AF activities, we tested purified fractions enriched in saponins isolated from Bohadschia argus, representing one of the most active anti-fouling extracts. Saponins were quantified by vanillin-sulfuric acid colorimetric assays and identified by LC-MS and LC-MS/MS analyses. We were able to demonstrate that AF activities in sea cucumber extracts were species-specific, and growth inhibition as well as attachment of the diatom to surfaces is dependent on the saponin concentration (i.e., Actinopyga contained the highest quantities), as well as on the molecular composition and structure of the present saponins (i.e., Bivittoside D derivative was the most bioactive compound). In conclusion, the here performed AF assay represents a promising and fast method for selecting the most promising bioactive organism as well as for identifying novel compounds with potent AF activities for the discovery of potentially novel pharmacologically active natural products. Full article

Saponins in the Camellia sinensis seeds have a broad spectrum of biological properties and application potentials. However, up to now, no chromatographic methods have been developed to provide full fingerprinting and quality assurance for these saponins. This research aimed to develop a novel method to tentatively identify and quantify saponins in C. sinensis seeds by ultra-high-performance liquid chromatography coupled with photo-diode array detector and quadrupole time-of-flight mass spectrometry (UPLC-PDA-QTOF-MS/MS), and compare it with the classic vanillin-sulfuric acid assay. Fifty-one triterpene saponins, including six potentially new compounds, were simultaneously detected by UPLC-PDA-MS/MS, and their chemical structures were speculated according to the retention behavior and fragmentation pattern. The total saponin content in the crude extract and the purified saponin fraction of C. sinensis seeds were quantified to be 19.57 ± 0.05% (wt %) and 41.68 ± 0.09% (wt %) respectively by UPLC-PDA at 210 nm, while the corresponding values were determined to be 43.11 ± 3.17% (wt %) and 56.60 ± 5.79% (wt %) respectively by the vanillin-sulfuric acid assay. The developed UPLC-PDA -MS/MS method could determine specified saponins, and is more reliable for quantifying the C. sinensis seed saponins than the classic spectrophotometric method. It is of great significance for the future investigations and applications of these saponins. Full article