Chemical characterization, antioxidant activity, and cytotoxicity of fatty acids methyl esters from Handroanthus impetiginosus (Mart. ex DC.) Mattos (Bignoniaceae) seeds.

Handroanthus impetiginosus, popularly known as "ipê-roxo", is used in folk medicine to treat skin inflammations, infections, stomach diseases, and cancer. Fatty acid methyl esters (FAMEs) obtained from the esterification reaction of fatty acids (FA) found in the hexane extract (HE) of seeds of H. impetiginosus were identified by gas chromatography-mass spectrometry (GC-MS). The antioxidant and cytotoxic activities of the HE and FAMEs were evaluated. Methyl palmitate, methyl linoleate, methyl oleate, and methyl stearate were the major FAMEs obtained from the HE. The samples, especially the HE, exhibited a significant antioxidant potential analyzed by ferric reducing ability power (FRAP) assay. In the A. salina larvae bioassay, the HE showed no cytotoxic effects, but the FAMEs exhibited a high toxicity. This study reported, for the first time, the antioxidant and cytotoxic activities of the HE and FAMEs obtained from H. impetiginosus seeds.

Toxicity Evaluation of Anti-cholinesterasic Amphibian Extracts by MTT and an Optimized Artemia salina Test.

The amphibian skin is an important source of bioactive compounds. Recently, our workgroup reported the bioactivity of new extracts from the Hylidae, Microhylidae and Leptodactylidae families against several pathways involved in Alzheimer's disease. However, since cytotoxicity can be a limiting factor for their applicability, we evaluated the toxicity of nine amphibian skin extracts with reported anticholinesterase activity, using the traditional MTT assay and an optimized Artemia salina test. The proposed improvement, guided by experimental design, aims to reduce the amount of biological sample needed. Overall, we proved that the active extracts were non-toxic at effective concentration against cholinesterases (AChE/BChE), positioning the amphibian skin as a promising and preliminary safe source of bioactive compounds in the anti-Alzheimer's treatment. Interestingly, we demonstrated that both toxicity assays can discriminate between toxic and non-toxic samples. We propose the A. salina bioassay as a reliable and cost-effective alternative for early toxicity screening.

Antibacterial activity of herbal formulation against common oral pathogens.

The development of antibiotic resistance in microorganisms is a global challenge for the clinicians, pharmacist and research scientists leading to the development of new medicinal formulations that are effective and easily consumable. The plant yielding essential oil with chief constituent as eugenol has been identified as an important compound with strong inhibition of bacteria, and storage fungi. Ocimum gratissimum and Ocimum sanctum is an aromatic shrub occurring in warm tropical regions has been used in traditional medicine in India to cure various ailments in general and as an antimicrobial agent in particular. The aim of this present study is to assess the antimicrobial and cytoxic activity of the formulation against oral pathogens. The formulation of O. gratissimum and O. sanctum plant extract was prepared and filtered. Antimicrobial activity was done by agar well diffusion method, minimum inhibitory concentration assessment was determined by broth dilution method and cytotoxicity was assessed by brine shrimp lethality assay. Agar well diffusion method against S. mutans, Enterococcus faecalis, C. albicans, Lactobacillus sp, and S. aureus revealed no zone of inhibition but at 100µL concentration at every time interval, the study formulation showed more bacteriostatic activity than positive control and the standard used. The formulation showed very minimal cytotoxicity. The formulation of O. gratissimum and O. sanctum synergistically showed more antibacterial, antifungal and cytotoxic activity and more research has to be done in invivo environment.

Cytotoxicity Analysis and In Silico Studies of Three Plant Extracts with Potential Application in Treatment of Endothelial Dysfunction.

Endothelial dysfunction is the basis of the physiopathological mechanisms of vascular diseases. In addition to the therapeutic activity of plant extracts, cytotoxicity is significant. This research evaluates the cytotoxicity of three vegetal extracts (Calendulae flos extract-CE, Ginkgo bilobae folium extract-GE, and Sophorae flos extract-SE). In vitro evaluation was performed using an endothelial cell line model (Human Pulmonary Artery Endothelial Cells-HPAEC) when a dose-dependent cytotoxic activity was observed after 72 h. The IC50 values were calculated for all extracts: Calendulae flos extract (IC50 = 91.36 µg/mL), Sophorae flos extract (IC50 = 68.61 µg/mL), and Ginkgo bilobae folium extract (IC50 = 13.08 µg/mL). Therefore, at the level of HPAEC cells, the cytotoxicity of the extracts follows the order GE > SE > CE. The apoptotic mechanism implied in cell death was predicted for several phytocompounds using the PASS algorithm and molecular docking simulations, highlighting potential interactions with caspases-3 and -8. In vivo analysis was performed through brine shrimp lethality assay (BSLA) when lethal, behavioral, and cytological effects were evaluated on Artemia salina larvae. The viability examined after 24 h (assessment of lethal effects) follows the same sequence: CE > SE > GE. In addition, the predicted cell permeability was observed mainly for GE constituents through in silico studies. However, the extracts can be considered nontoxic according to Clarckson's criteria because no BSL% was registered at 1200 µg/mL. The obtained data reveal that all three extracts are safe for human use and suitable for incorporation in further pharmaceutical formulations.

Analysis of antibacterial and cytotoxic potential of medicinal plants from Cholistan desert, Pakistan.

This study aimed to investigate the antibacterial and cytotoxic activity of 03 medicinal plants, Calligonum polygonides, Farsetia hamiltonii, and Pulcaria crispa, from Cholistan desert, Pakistan. The active constituents of plants species were extracted in 05 different solvents and the extracts were tested against various bacterial strains and brine shrimps. Although all Calligonum polygonides's extracts except chloroform were active against Staphylococcus aureus the most active was the acetone extract (21 ± 0.00 mm at 200 µg/disc) and activity was better than Caricef (p-value 0.03). While its water extract was more potent (18 ± 1.45 mm at 200 µg/disc) than Augmentin and Caricef (p-value < 0.005). The methanol extract's activity (15 ± 0.39 mm in 200 µg/disc) was comparable to Fucidin against Proteus vulgaris (p-value > 0.99) and activity of diethyl ether extract against Escherichia coli (10 ± 1.16 mm in 200 µg/disc) was same as of Urixin (p-value 0.91). Farsetia hamiltonii's acetone extract against Pseudomonas aeruginosa (10 ± 0.15 mm in 1 µg/disc) was more active than Augmentin Caricef and Cefotax (p-value < 0.02) and against Staphylococcus aureus (15 ± 1.15 mm in 200 µg/disc) activity was higher than Caricef (p-value 0.03). All Pulicaria crispa's extracts except water extract were found active against Staphylococcus aureus. However, the diethyl ether extract was most effective (25 + 0.00 mm at 150 µg /disc) and activity was more than Augmentin, Oxy-tetracycline, Fucidin, Urixin, Ceftriaxone (p-value < 0.05). Although all extracts were exhibited cytotoxic activity, the Calligonum polygonides's acetone extract (100%), Farsetia hamiltonii's diethyl ether extract (90%) and Pulicaria crispa's methanol extract (100%) were most active at 1000 µg/ml concentration. This study validated the medicinal significance of the studied plants and thus opens the way for their therapeutic applications.

Highly Diluted Glyphosate Mitigates Its Effects on Artemia salina: Physicochemical Implications.

Glyphosate is an herbicide widely used in agriculture but can present chronic toxicity in low concentrations. Artemia salina is a common bio-indicator of ecotoxicity; it was used herein as a model to evaluate the effect of highly diluted-succussed glyphosate (potentized glyphosate) in glyphosate-based herbicide (GBH) exposed living systems. Artemia salina cysts were kept in artificial seawater with 0.02% glyphosate (corresponding to 10% lethal concentration or LC10) under constant oxygenation, luminosity, and controlled temperature, to promote hatching in 48 h. Cysts were treated with 1% (v/v) potentized glyphosate in different dilution levels (Gly 6 cH, 30 cH, 200 cH) prepared the day before according to homeopathic techniques, using GBH from the same batch. Controls were unchallenged cysts, and cysts treated with succussed water or potentized vehicle. After 48 h, the number of born nauplii per 100 µL, nauplii vitality, and morphology were evaluated. The remaining seawater was used for physicochemical analyses using solvatochromic dyes. In a second set of experiments, Gly 6 cH treated cysts were observed under different degrees of salinity (50 to 100% seawater) and GBH concentrations (zero to LC 50); hatching and nauplii activity were recorded and analyzed using the ImageJ 1.52, plug-in Trackmate. The treatments were performed blind, and the codes were revealed after statistical analysis. Gly 6 cH increased nauplii vitality (p = 0.01) and improved the healthy/defective nauplii ratio (p = 0.005) but delayed hatching (p = 0.02). Overall, these results suggest Gly 6cH treatment promotes the emergence of the more GBH-resistant phenotype in the nauplii population. Also, Gly 6cH delays hatching, another useful survival mechanism in the presence of stress. Hatching arrest was most marked in 80% seawater when exposed to glyphosate at LC10. Water samples treated with Gly 6 cH showed specific interactions with solvatochromic dyes, mainly Coumarin 7, such that it appears to be a potential physicochemical marker for Gly 6 cH. In short, Gly 6 cH treatment appears to protect the Artemia salina population exposed to GBH at low concentrations.

Antiproliferative assay of suma or Brazilian ginseng (Hebanthe eriantha) methanolic extract on HCT116 and 4T1 cancer cell lines, in vitro toxicity on Artemia salina larvae, and antibacterial activity.

Hebanthe eriantha is a medicinal plant used in folk medicine and a subject of commercial interest. The cytotoxicity effects from H. eriantha root extracts on cancerous and normal cells were assessed by the MTT method, and in vitro toxicity was evaluated on Artemia salina. The inhibition of the proliferation of bacteria and MIC values were examined by the disc diffusion and the broth microdilution method, respectively. Human colon cancer HCT116 and mouse breast tumour model 4T1 cells treated with methanolic extract showed a significant decrease in viability of cells with IC50: 272.6 and 88.5 µg/mL at 72h, respectively. The methanolic extract of H. eriantha showed moderate toxicity against A. salina (LC50: 589.4 µg/mL). In antimicrobial activity, the methanolic extract showed the highest inhibitory function against S. aureus and P. vulgaris (17.5 and 16 mm) with MICs of 500 µg/mL. The results confirmed the potential of plant roots as cytotoxic agents.

Avocado seed by-product uses in emulsion-type ingredients with nutraceutical value: Stability, cytotoxicity, nutraceutical properties, and assessment of in vitro oral-gastric digestion.

The avocado industry obtains 20-30% of the total by-products (peels and seeds). However, byproducts can be uses as sources of economic nutraceutical ingredients with functional potential. This work developed emulsion-type ingredients from avocado seed to evaluate its quality, stability, cytotoxicity, and nutraceutical properties before/after in vitro oral-gastric digestion. Ultrasound lipid extraction achieved an extraction yield of up to 95.75% compared with Soxhlet conventional extraction (p > 0.05). Six ingredients' formulations (E1-E6) were stable for up to day 20 during storage, preserving their antioxidant capacity and displaying low in vitro oxidation compared to control. None of the emulsion-type ingredients were considered cytotoxic according to the shrimp lethality assay (LC50 > 1000 µg/mL). Ingredients E2, E3, and E4 generated low lipoperoxides' concentrations and high antioxidant capacity during the oral-gastric stage. The 25 min-gastric phase showed the highest antioxidant capacity and low lipoperoxidation. Results suggested avocado seed-derived could be used to develop functional ingredients with nutraceutical properties.

Chemical composition, antioxidant and cytotoxic activities of extracts from the pericarp of Tecoma stans (L.) Juss. Ex Kunth (Bignoniaceae).

Tecoma stans (L.), popularly known as ipê-mirim, is used in traditional medicine for the treatment of diabetes and digestive problems. The components of the hexane (HE) and methanol (ME) extracts obtained from the pericarp of T. stans were identified by gas chromatography-mass spectrometry (GC-MS) in their methyl ester forms (FAME). The antioxidant and cytotoxic activities of extracts, fatty acids, and methyl esters were evaluated. Methyl linolenate, methyl linoleate, and methyl palmitate were the major compounds in the HE, while methyl hexacosanoate was the main component in the ME. The samples exhibited significant antioxidant potential by DPPH assay. In the Artemia salina larvae bioassay, FAME (HE) and FAME (ME) were considered toxic. This study showed, for the first time to our knowledge, the chemical composition of the hexane and methanol extracts from T. stans pericarp, as well as the antioxidant and cytotoxic activities of the extracts, fatty acids, and methyl esters.

Understanding the Antilymphoma Activity of Annona macroprophyllata Donn and Its Acyclic Terpenoids: In Vivo, In Vitro, and In Silico Studies.

Annona macroprophyllata Donn (A. macroprophyllata) is used in traditional Mexican medicine for the treatment of cancer, diabetes, inflammation, and pain. In this work, we evaluated the antitumor activity of three acyclic terpenoids obtained from A. macroprophyllata to assess their potential as antilymphoma agents. We identified the terpenoids farnesyl acetate (FA), phytol (PT) and geranylgeraniol (Gg) using gas chromatography-mass spectroscopy (GC-MS) and spectroscopic (1H, and 13C NMR) methods applied to petroleum ether extract of leaves from A. macroprophyllata (PEAm). We investigated antitumor potential in Balb/c mice inoculated with U-937 cells by assessing brine shrimp lethality (BSL), and cytotoxic activity in these cells. In addition, to assess the potential toxicity of PEAm, FA, PT and Gg in humans, we tested their acute oral toxicity in mice. Our results showed that the three terpenoids exhibited considerable antilymphoma and cytotoxic activity. In terms of lethality, we determined a median lethal dose (LD50) for thirteen isolated products of PEAm. Gg, PT and AF all exhibited a higher lethality with values of 1.41 ± 0.42, 3.03 ± 0.33 and 5.82 ± 0.58 µg mL-1, respectively. To assess cytotoxic activity against U-937 cells, we calculated the mean cytotoxic concentration (CC50) and found that FA and PT were closer in respect to the control drug methotrexate (MTX, 0.243 ± 0.007 µM). In terms of antilymphoma activity, we found that FA, PT and Gg considerably inhibited lymph node growth, with median effective doses (ED50) of 5.89 ± 0.39, 6.71 ± 0.31 and 7.22 ± 0.51 mg kg-1 in females and 5.09 ± 0.66, 5.83 ± 0.50 and 6.98 ± 0.57mg kg -1 in males, respectively. Regarding acute oral toxicity, we classified all three terpenoids as category IV, indicating a high safety margin for human administration. Finally, in a molecular docking study of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, we found binding of terpenoids to some amino acids of the catalytic site, suggesting an effect upon activity with a resulting decrease in the synthesis of intermediates involved in the prenylation of proteins involved in cancer progression. Our findings suggest that the acyclic terpenoids FA, PT, and Gg may serve as scaffolds for the development of new treatments for non-Hodgkin's lymphoma.

The Effects of Drying Techniques on Phytochemical Contents and Biological Activities on Selected Bamboo Leaves.

The therapeutic potential of bamboos has acquired global attention. Nonetheless, the biological activities of the plants are rarely considered due to limited available references in Sabah, Malaysia. Furthermore, the drying technique could significantly affect the retention and degradation of nutrients in bamboos. Consequently, the current study investigated five drying methods, namely, sun, shade, microwave, oven, and freeze-drying, of the leaves of six bamboo species, Bambusa multiplex, Bambusa tuldoides, Bambusa vulgaris, Dinochloa sublaevigata, Gigantochloa levis, and Schizostachyum brachycladum. The infused bamboo leaves extracts were analysed for their total phenolic content (TPC) and total flavonoid content (TFC). The antioxidant activities of the samples were determined via the 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and ferric reducing antioxidant power (FRAP) assays, whereas their toxicities were evaluated through the brine shrimp lethality assay (BSLA). The chemical constituents of the samples were determined using liquid chromatography−tandem mass spectrometry (LC-MS/MS). The freeze-drying method exhibited the highest phytochemical contents and antioxidant activity yield, excluding the B. vulgaris sample, in which the microwave-dried sample recorded the most antioxidant and phytochemical levels. The TPC and TFC results were within the 2.69 ± 0.01−12.59 ± 0.09 mg gallic acid equivalent (GAE)/g and 0.77 ± 0.01−2.12 ± 0.01 mg quercetin equivalent (QE)/g ranges, respectively. The DPPH and ABTS IC50 (half-maximal inhibitory concentration) were 2.92 ± 0.01−4.73 ± 0.02 and 1.89−0.01 to 3.47 ± 0.00 µg/mL, respectively, indicating high radical scavenging activities. The FRAP values differed significantly between the drying methods, within the 6.40 ± 0.12−36.65 ± 0.09 mg Trolox equivalent (TE)/g range. The phytochemical contents and antioxidant capacities exhibited a moderate correlation, revealing that the TPC and TFC were slightly responsible for the antioxidant activities. The toxicity assessment of the bamboo extracts in the current study demonstrated no toxicity against the BSLA based on the LC50 (lethal concentration 50) analysis at >1000 µg/mL. LC-MS analysis showed that alkaloid and pharmaceutical compounds influence antioxidant activities, as found in previous studies. The acquired information might aid in the development of bamboo leaves as functional food items, such as bamboo tea. They could also be investigated for their medicinal ingredients that can be used in the discovery of potential drugs.

Antioxidant and antiproliferative activities of n-hexane extract and its fractions from Blumea balsamifera L. leaves.

Blumea balsamifera is a plant species that has been popularly used to treat a broad spectrum of diseases. In efforts of tackling the increasing threat of cancers, B. balsamifera has been studied for its anticancer potentials. Hence, through this research, we aimed to evaluate the antioxidant and antiproliferative activities of n-hexane extract from B. balsamifera L. leaves along with its fractionation products. After the n-hexane extract has been obtained, the sample was column chromatographed using gradient elution with n-hexane:ethyl acetate solvent. All the isolation protocols produced 1 n-hexane extract and 10 different fractions (fractions 1-10). Antioxidant and antiproliferative effects of the samples were assessed based on 2,2-diphenyl-1-picrylhydrazyl and brine shrimp lethality test assay, respectively. None of the samples have a strong antioxidant level because all samples yielded IC50 of more than 100 ppm - the best of them was fraction 8 with IC50 = 113.716 ppm. On contrary, most of the samples were observed to have a potent antiproliferative effect, especially fraction 8 with LC50 = 2.00 ppm. Taken altogether, fraction 8 from the n-hexane extract of B. balsamifera L. leaves is the most potential candidate for proliferative disease therapy, where further studies confirming the results are required.

Mercury chloride toxicity attenuation of the Brine Shrimp Artemia Salinaafter treatment with Mercurius corrosivusas isotherapic

Isotherapics preparedfromtoxic substances have been described as attenuation factors for heavy metal intoxicationin aquatic animals. Herein, Artemia salinaand mercury chloride were usedas a model to identify treatment-related bioresilience. The aim was to describe the effects of Mercurius corrosivus(MC) in different potencies on Artemia salinacyst hatching and on mercury bioavailability. Artemia salinacysts were exposed to 5.0 µg/mL of mercury chloride during the hatching phase. MC6cH, 30cH, and 200cHwere prepared and poured into artificial seawater. Different controls were used (nonchallenged cysts and challenged cysts treated with water, succussed water, and Ethilicum 1cH). Four series of nine experiments were performed for4 weeks to evaluate the percentage of cyst hatchingconsidering all moon phases. Soluble total mercury (THg) levels and precipitated mercury content were also evaluated. Solvatochromic dyes were used to check for eventual physicochemical markers of MCbiological activity. Two-way analysis of variance (ANOVA) with mixed modelswas used for evaluating the effect of different treatments andthe simultaneous influence of the moon phases on the cystshatching rate, at both observation times (24 and 48 hours).When necessary, outliers were removed, using the Tukeycriterion.Thelevel of significance αwas set at 5%. Significant delay (p<0.0001) in cyst hatching was observed after treatment with MC30cH, compared with the controls. An increase inTHg concentration in seawater (p<0.0018) and of chlorine/oxygen ratio (p<0.0001) in suspended micro-aggregateswas also seen, with possiblerelation with mercury bioavailability. Specific interaction of MC30cH with the solvatochromic dye ET33 (p<0.0017) was found. The other observed potencies of Mercurius corrosivus6 and 200 cH were not significant in relation to the observed groups.The results werepostulated as being protective effects of MC30cH on Artemia salina, by improving its bioresilience.

Isolation and Identification of Bioactive Compounds from Bidens spp. Using HPLC-DAD and GC-MS Analysis and Their Biological Activity as Anticancer Molecules.

The genus Bidens a member of family Compositae, is widely documented as an ethno-medicinally important genus of plants. In the present study, anticancer potential of three ethno-medicinally important species i.e., B. bipinnata, B. biternata and B. pilosa were tested. For in-vitro evaluation, an MTT (Thiazolyl blue tetrazolium bromide) assay was performed against cervical cancer cells (HeLa), hepatocellular carcinoma (HepG), and adenocarcinoma human alveolar basal epithelial cells (A549). For in vivo evaluation, Artemia salina, Danio rerio, and Caenorhabditis elegans were used. Among all the tested extracts, the ethanol extract of B. biternata appeared to have highest anticancer activity, and the compounds responsible for this activity were identified to be Tris (2,4-di-tert-butylphenyl), 4-hydroxy-2,4'-dimethoxychalcone, and 2,4-di-tert-butylphenol. This is the first report of the isolation of Tris (2,4-di-tert-butylphenyl) phosphate from the genus Bidens and the first report of 4-hydroxy-2,4'-dimethoxychalcone and 2,4-di-tert-butylphenol from B. biternata. Among the isolated compounds, 4-hydroxy-2,4'-dimethoxychalcone showed the highest anticancer activity with an LD50 value of 236.7 µg/mL. Therefore, this compound carries promising potential for being established as a pharmaceutical for chemoprevention and chemotherapy.

Pharmacological properties and preliminary phytochemical analysis of Pseudocaryopteris foetida (D.Don) P.D. Cantino leaves.

Medicinal plants have significant contribution in pharmaceutical industries being producers of compounds utilized as precursors for drug development. A plant of Lamiaceae family; Pseudocaryopteris foetida had not been investigated for its biomedical potential. Current research was aimed to investigate phytochemical analysis, cytotoxic potential and antioxidant activity of crude methanolic extract and fractions of Pseudocaryopteris foetida (leaves). The preliminary phytochemical analysis of crude methanolic extracts and fractions of Pseudocaryopteris foetida revealed that plant is rich in phenolic and flavonoid classes of secondary metabolites while presence of tannin was observed only in crude methanolic extract. The cytotoxicity was determined using brine shrimp lethality test. Different concentrations (25, 50, 100, 150, 200 and 250 µg/mL) of crude methanolic extract and fractions exhibited dose dependent cytotoxicity. However, The LD50 for all the extracts was more than 200 µg/mL indicating weak cytotoxic potential of Pseudocaryopteris foetida. The antioxidant capabilities of crude methanolic extract and fraction of Pseudocaryopteris foetida were analyzed by in vitro bio assays including DPPH, ABTS, Reducing power and phosphomolybdate antioxidant assays using ascorbic acid as standard. The crude methanolic extract showed IC50 (256.38 ± 0.6 and 314.95 ± 1.1 µg/mL) for DPPH and ABTS respectively, while total antioxidant capacity was calculated as 55.79 ± 0.5 µg/mL for crude methanolic extract of Pseudocaryopteris foetida while ascorbic acid indicated total antioxidant capacity of 71.89 ± 2.3 µg/mL. Study concluded that leaves of Pseudocaryopteris foetida were the rich source of antioxidant phytochemicals. Based on preliminary investigations further research should be focused to isolate bioactive phytochemicals as leading source of clinical medicines in future.

Comparative toxicity, phytochemistry, and use of 53 Philippine medicinal plants.

The study compares the toxicity of 53 selected medicinal plants commonly used in the Philippines to treat various diseases. It uses as a benchmark Vitex negundo L., which was approved by the Philippine Food and Drug Administration as an herbal drug for cough and asthma after passing clinical trials for safety and efficacy. The methods were chosen for their simplicity and accessibility even for resource-limited laboratories. Extracts (95 % ethanol) of the medicinal parts of the plants were (1) chemically profiled using qualitative phytochemical tests that detect the presence of key classes of bioactive compounds; and (2) evaluated for toxicity using the brine shrimp (Artemia sp.) lethality assay (BSLA). General phytochemical screening revealed the presence of tannins in 50 plant extracts, alkaloids in 43, glycosides in 33, flavonoids in 31, steroids in 21, triterpenoids in 20, anthraquinones in 10, and saponins in 8. Extracts from eight plants had LC50 values lower than the potassium dichromate control (approximately 12 µg/mL) and were considered highly toxic; extracts from 21 plants had LC50 values between 12 µg/mL and 100 µg/mL and were considered moderately toxic; extracts from 19 plant extracts, including Vitex negundo and some common vegetables, had LC50 values between 100 µg/mL and 500 µg/mL, and were considered mildly toxic and likely to have reasonable safety margins; five plant extracts, including common vegetables, had LC50 values above 500 µg/mL and were considered essentially nontoxic. No apparent correlation could be found between toxicity and chemical diversity or a specific class of phytochemicals present. Our findings may serve as a guide for herbal drug and nutraceutical development, especially in prioritizing plants for more detailed safety studies.

Two mosquito larvicidal arabinofuranosidetridecanol from Commiphora merkeri exudate.

Two new arabinofuranosidetridecanol, namely 1,2-tridecanediol-1-O-α-L-5'-acetylarabinofuranoside (1) and 1,2-tridecanediol-1-O-α-L-arabinofuranoside (2) together with known compound, 1,2-tridecanediol (3) were isolated from Commiphora merkeri exudate. Compound 1 showed larvicidal activity against Ae. aegypti (LC50 = 40.66 µg/mL), An. gambiae (LC50 = 22.86 µg/mL) and Cx. quinquefasciatus (LC50 = 15.88 µg/mL). Also, Compound 2 had larvicidal activity against Ae. aegypti (LC50 = 33.79 µg/mL), An. gambiae (LC50 = 31.99 µg/mL) and Cx. quinquefasciatus (LC50 = 17.70 µg/mL). There were no significant difference of larvae mortalities (≥ 95%) among the two compounds and among mosquito species except for compound 2 at 72 h for Cx. quinquefasciatus and An. gambiae. Compound 3 was not larvicidal active even after 72 h of exposure time. In addition, none of the compound was cytotoxic to brine shrimps. The two Arabinofuranosidetridecanol are potential against mosquito species and they could be safe in the environment.

Antitumor Potential of Annona muricata Linn. An Edible and Medicinal Plant in Mexico: In Vitro, In Vivo, and Toxicological Studies.

Annona muricata (Am) is a plant used in traditional Mexican medicine to treat cancer. In this study, ethanol extracts of Am collected in Acapulco and Tecpan from Guerrero state were evaluated orally on Balb/c mice inoculated with 4T1 cells, for cytotoxic activity (CA) on 4T1 cells, in brine shrimp lethality assay (BSLA), and for acute oral toxicity in mice. In addition, ethanol extracts were subjected to high-performance liquid chromatography (HPLC) with diode array detection. Results showed that the extracts collected in December in Acapulco (AcDe) and Tecpan (TeDe) exhibited the most significant antitumor and cytotoxic activity. In the BSLA, the most important effect was observed in the extracts from Acapulco and Tecpan collected in June (AcJu) and August (TeAg), respectively. The samples from Acapulco (AcJu, and AcAg) and Tecpan (TeJu and TeAg) showed the highest toxicity. The analysis of the extracts, AcDe and TeDe, by HPLC revealed that flavonoids, rutin, narcissin, and nicotinflorin were the major components. These findings suggest that extracts from Am collected in Acapulco and Tecpan in the month of December may be an important source to obtain flavonoid glycosides with anticancer potential specifically against breast cancer. This also supports the use of Am to treat cancer in Mexican traditional medicine.

Effect of UV Irradiation (A and C) on Casuarina equisetifolia-Mediated Biosynthesis and Characterization of Antimicrobial and Anticancer Activity of Biocompatible Zinc Oxide Nanoparticles.

The green synthesis of nanoparticles has emerged as a simple, safe, sustainable, reliable and eco-friendly protocol. Among different types of NPs, green-synthesized zinc oxide NPs (ZnONPs) show various promising biological uses due to their interesting magnetic, electrical, optical and chemical characteristics. Keeping in view the dependence of the therapeutic efficacy of NPs on their physico-chemical characteristics, the green synthesis of ZnONPs using Casuarina equisetifolia leaf extract under UV-A and UV-C light was carried out in this study. UV-irradiation helped to control the size and morphology of ZnONPs by exciting the electrons in the photoactive compounds of plant extracts to enhance the bio-reduction of ZnO into ZnONPs. C. equisetifolia leaf extract was found enriched with phenolic (2.47 ± 0.12 mg GAE/g DW) and flavonoid content (0.88 ± 0.28 mg QE/g DW) contributing to its 74.33% free-radical scavenging activity. FTIR spectra showed the involvement of polyphenols in the bio-reduction, stabilization and capping of ZnONPs. Moreover, SEM-EDX and XRD analyses showed great potential of UV-C light in yielding smaller (34-39 nm) oval-shaped ZnONPs, whereas UV-A irradiation resulted in the formation of fairly spherical 67-71 nm ZnONPs and control ZnONPs were of mixed shape and even larger size (84-89 nm). Green-synthesized ZnONPs, notably CE-UV-C-ZnONPs, showed promising anti-bacterial activities against Bacillus subtilis, Pseudomonas fluorescens and Pseudomonas aeruginosa. Moreover, ZnONPs also enhanced ROS production which led to a significant loss of mitochondrial membrane potential and activated caspase-3 gene expression and caspase-3/7 activity in human hepatocellular carcinoma (HepG2) cells. CE-UV-C-ZnONP treatment reduced HepG2 cell viability to as low as 36.97% owing to their unique shape and smaller size. Lastly, ZnONPs were found to be highly biocompatible towards brine shrimp and human red blood cells suggesting their bio-safe nature. This research study sheds light on the plausible role of UV radiation in the green synthesis of ZnONPs with reasonable control over their size and morphology, thus improving their biological efficacy.

Antibacterial, Antihemolytic, Cytotoxic, Anticancer, and Antileishmanial Effects of Ajuga bracteosa Transgenic Plants.

Herbal and traditional medicines can play a pivotal role in combating cancer and neglected tropical diseases. Ajuga bracteosa, family Lamiaceae, is an important medicinal plant. The genetic transformation of A. bracteosa with rol genes of Agrobacterium rhizogenes further enhances its metabolic content. This study aimed at undertaking the molecular, phytochemical, and in vitro biological analysis of A. bracteosa extracts. We transformed the A. bracteosa plant with rol genes and raised the regenerants from the hairy roots. Transgenic integration and expression of rolB were confirmed by conventional polymerase chain reaction (PCR) and qPCR analysis. The methanol: chloroform crude extracts of wild-type plants and transgenic regenerants were screened for in vitro antibacterial, antihemolytic, cytotoxic, anticancer, and leishmanial activity. Among all plants, transgenic line 3 (ABRL3) showed the highest expression of the rolB gene. Fourier transform infra-red (FTIR) analysis confirmed the enhanced number of functional groups of active compounds in all transgenic lines. Moreover, ABRL3 exhibited the highest antibacterial activity, minimum hemolytic activity (CC50 = 7293.05 ± 7 µg/mL) and maximum antileishmanial activity (IC50 of 56.16 ± 2 µg/mL). ABRL1 demonstrated the most prominent brine shrimp cytotoxicity (LD5039.6 ± 4 µg/mL). ABRL3 was most effective against various human cancer cell lines with an IC50 of 57.1 ± 2.2 µg/mL, 46.2 ± 1.1 µg/mL, 72.4 ± 1.3 µg/mL, 73.3 ± 2.1 µg/mL, 98.7 ± 1.6 µg/mL, and 97.1 ± 2.5 µg/mL against HepG2, LM3, A549, HT29, MCF-7, and MDA-MB-231, respectively. Overall, these transgenic extracts may offer a cheaper therapeutic source than the more expensive synthetic drugs.