Chemical characterization, in vivo safety profile and effects of the extract from unconventional food plant Acca sellowiana (O. BERG) Burret on endothelial cells under glucose overload.

"Guava" (Acca sellowiana) is an unconventional edible plant from Brazil. It is used in traditional medicine as an anti-diabetic; however, pharmacological studies on this plant are scarce. This study aimed to evaluate the chemical and safety profile of an aqueous A. sellowiana peel extract (ASPE) and its effects on endothelial EA.hy926 cells under glucose overload and in vivo (Artemia salina). An ethanolic extract from A. sellowiana peels (ASPEetOH) was also produced and characterized. Results showed that ASPE did not present in vivo toxicity, and it was found to contain high phenolic content and redox capacity. ASPE (50 µg/mL; 24 h) prevented oxidative stress and mitochondrial dysfunction, besides positively modulating Sirtuins 1 and 3, and prevented the increase of COX-2 and NF-kß expression levels in EA.hy926 cells under glucose overload. Chromatographic fractionation, metabolite profiling, spectroscopic and bioinformatics analyses revealed the presence of phenolic acids, flavan-3-ols, flavonols, flavones, flavanones, and anthocyanidins, displaying a diversity of compounds in the crude and fractionated ASPEetOH. This study provided evidence on the safety profile, chemical composition, and pharmacological activities of A. sellowiana.

The Role of Traditional Chinese Medicines in the Treatment of Osteoporosis.

Osteoporosis (OP) represents a substantial public health issue and is associated with increasing rates of morbidity and mortality. It is characterized by reduced bone mineral density, deterioration of bone tissue quality, disruption of the microarchitecture of bones, and compromised bone strength. These changes may be attributed to the following factors: intercellular communication between osteoblasts and osteoclasts; imbalanced bone remodeling; imbalances between osteogenesis and adipogenesis; imbalances in hormonal regulation; angiogenesis; chronic inflammation; oxidative stress; and intestinal microbiota imbalances. Treating a single aspect of the disease is insufficient to address its multifaceted nature. In recent decades, traditional Chinese medicine (TCM) has shown great potential in the treatment of OP, and the therapeutic effects of Chinese patent drugs and Chinese medicinal herbs have been scientifically proven. TCMs, which contain multiple components, can target the diverse pathogeneses of OP through a multitargeted approach. Herbs such as XLGB, JTG, GSB, Yinyanghuo, Gusuibu, Buguzhi, and Nvzhenzi are among the TCMs that can be used to treat OP and have demonstrated promising effects in this context. They exert their therapeutic effects by targeting various pathways involved in bone metabolism. These TCMs balance the activity of osteoblasts (bone-forming cells) and osteoclasts (bone-resorbing cells), and they exhibit anti-inflammatory, immunomodulatory, anti-oxidative, and estrogen-like functions. These multifaceted mechanisms underlie the efficacy of these herbs in the management and treatment of OP. Herein, we examine the efficacy of various Chinese herbs and Chinese patent drugs in treating OP by reviewing previous clinical trials and basic experiments, and we examine the potential mechanism of these therapies to provide evidence regarding the use of TCM for treating OP.

Systematic investigation of the material basis, effectiveness and safety of Thesium chinense Turcz. and its preparation Bairui Granules against lung inflammation.

BACKGROUND: Thesium chinense Turcz. (Named as Bai Rui Cao in Chinese) and its preparations (e.g., Bairui Granules) have been used to treat inflammatory diseases, such as acute mastitis, lobar pneumonia, tonsillitis, coronavirus disease 2019 (COVID-19), and upper respiratory tract infection. However, the material basis, pharmacological efficiency, and safety have not been illustrated. METHODS: Anti-inflammatory activity-guided isolation of constituents has been performed using multiple column chromatography, and their structures were elucidated by NMR spectroscopy and ECD calculations. The inhibitory effects on lung inflammation and safety of the crude ethanol extract (CE), Bairui Granules (BG), and the purified active constituents were evaluated using lipopolysaccharide (LPS)-stimulated acute lung inflammation (ALI) mice model or normal mice. RESULTS: Seven new compounds (1-7) and fifty-six known compounds (8-63) were isolated from T. chinense, and fifty-four were reported from this plant for the first time. The new flavonoid glycosides 1-2, new fatty acids 4-5, new alkaloid 7 as well as the known constituents including flavonoid aglycones 8-11, lignans 46-54, alkaloids 34 and 45, coumarins 57, phenylpropionic acids 27, and simple aromatic compounds 39, 44 and 58 exhibited anti-inflammatory activity. Network pharmacology analysis indicated that anti-inflammation of T. chinense was attributed to flavonoids and alkaloids by regulating inflammation-related proteins (e.g., TNF, NF-κB, TGF-ß). Furthermore, constituents of T. chinense including kaempferol-3-O-glucorhamnoside (KN, also named as Bairuisu I, 19), astragalin (AG, Bairuisu II, 12), and kaempferol (KF, Bairuisu III, 8), as well as CE and BG could alleviate lung inflammation caused by LPS in mice by preventing neutrophils infiltration and the expression of the genes for pro-inflammatory cytokines NLRP3, caspase-1, IL-1ß, and COX-2. After a 28-day subacute toxicity test, BG at doses of 4.875 g/kg and 9.750 g/kg (equivalent to onefold and twofold the clinically recommended dose) and CE at a dose of 11.138 g/kg (equivalent to fourfold the clinical dose of BG) were found to be safe and non-toxic. CONCLUSIONS: The discovery of sixty-three constituents comprehensively illustrated the material basis of T. chinense. T. chinense and Bairui Granules could alleviate lung inflammation by regulating inflammation-related proteins and no toxicity was observed under the twofold of clinically used doses.

Landolphia (P. Beauv.) genus: Ethnobotanical, phytochemical and pharmacological studies.

The genus Landolphia (P. Beauv.) belongs to the Apocynaceae family with over 65 species distributed all over the tropical regions. This genus has a considerable number of documented medicinal, industrial, and ecologically beneficial effects. Therefore, this review is tailored towards the appraisal of the traditional significance, phytochemistry, and pharmacological activities of the genus Landolphia. This will help researchers understand future research trends by bridging the gaps between documented literature and contemporary uses. Relevant information was obtained from selection of scientific databases such as Web of Science, PubMed, Scopus, Google Scholar, ScienceDirect and Wiley. From documented literature, different parts of Landolphia have been used to improve fertility, lessen menstrual pain, boost sex libido, cure malaria and typhoid. Several classes of bioactive constituents such as terpenoids, phenolics, flavonoids, steroids, fatty acids, saponins, phytosterol and phenylpropanoid, volatile compounds, lignans and coumarins have been isolated from this genus. These secondary metabolites could be responsible for the reported antimicrobial, antimalarial, aphrodisiac, antioxidant, anti-inflammatory, antidiabetic and anticancer activities exhibited by this genus. The leaves, flower, bark and root of this genus have a wide range of essential nutrients and antinutrients which are essential for normal growth and development in living organisms. Despite all findings indicating the economical, industrial and pharmacological activities of Landolphia species, secondary metabolites and pharmacological potency of Landolphia of this genus are not adequately documented. Therefore, bioassay-guided isolation on the Landolphia extracts with proven biological activities should be prioritised in order to isolate pharmacophores with unique structural frameworks.

A Review on Ethnobotany, Phytochemistry and Pharmacological Activities of Euphorbia antiquorum L.

Euphorbia antiquorum L. is a small plant in the Euphorbiaceae family that is found primarily in tropical and subtropical Asia. It has a long tradition of being utilized in Chinese, Ayurvedic, and other traditional systems for a variety of ailments. To date, More than 116 bioactive constituents were isolated from Euphorbia antiquorum, with diterpenoids being the most abundant. Extracts and isolated chemicals from various portions of the plant have demonstrated significant pharmacological activities such as anti-inflammatory, analgesic, antidiabetic, anticancer etc. It is necessary to conduct an in-depth investigation of the phytochemicals along with the pharmacological properties of E. antiquorum. This review summarised the knowledge of ethnobotany, phytochemistry and pharmacological activities of the plant which will provide a better understanding to clarify the traditional uses of the species and its relation to modern pharmacology which will ultimately pave the way for its clinical application.

Mirror, mirror on the wall, which phytochemicals in Clinacanthus nutans inhibits advanced glycation end products of them all?

In our quest to discover advanced glycation end products (AGEs) inhibitors from Clinacanthus nutans (Burm.f.) Lindau leaves, we conducted a bioactivity-based molecular networking. This approach integrates LC-MS2 profiling and in vitro antiglycation data to predict bioactive compounds. We began by screening three extracts: 100% ethanol, 70% ethanol and 100% water alongside the in vitro antioxidant activity, total phenolics content (TPC) and schaftoside content. Among these extracts, 100% ethanol extract exhibited the highest total AGEs inhibition effects (IC50 = 80.18 ± 11.6 µg/mL), DPPH scavenging activity (IC50 = 747.40 ± 10.30 µg/mL) and TPC (26.54 ± 2.09 µg GAE /mg extract). Intriguingly, 100% ethanol extract contained the lowest amount of schaftoside, suggesting the involvement of other phytochemicals in the antiglycation effects. The molecular networking and in silico structural annotations of 401 LC-MS features detected in the fractions from 100% ethanol extract predicted 21 bioactive compounds (p < 0.05, r > 0.90), including several C40 carotenoids, alkaloids containing tetrapyrrole structures and fatty acids. On the contrary, all phenolics showed weak correlations with antiglycation effects. These predictions were further validated in vitro, where carotenoid lutein showed half maximal inhibitory concentration, IC50 = 96 ± 8 µM and selected flavonoid-C-glycosides exhibited weaker inhibitions (IC50 between 568 and 1922 µM). Notably, lutein content was higher in freeze-dried leaves (12.42 ± 0.82 mg/100 g) than oven-dried, although the former was associated with elevated mercury levels. In summary, C. nutans exhibited potential antiglycation and antioxidant activity, and lutein was identified as the main bioactive principle.

The exogenous application of naringenin and rosmarinic acid modulates functional traits in Lepidium sativum.

BACKGROUND: Phenolic modulators have attracted attention for their potential in shaping functional traits in plants. This work investigated the impact of naringenin (Nar) and rosmarinic acid (RA) on the functional properties of Lepidium sativum leaves and roots. RESULTS: Untargeted metabolomics identified a diverse phenolic profile, including flavonoids, phenolic acids, low molecular weight phenolics, lignans, and stilbenes. Cluster, analysis of variance multiblock orthogonal partial least squares (AMOPLS), and orthogonal projection to latent structures discriminant analysis (OPLS-DA) multivariate analyses confirmed tissue-specific modulation of bioactive compounds. The tissue was the hierarchically most influential factor, explaining 27% of observed variability, while the treatment and their interaction were statistically insignificant. Thereafter, various in vitro assays were employed to assess antioxidant capacity, including 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS) radical scavenging activity, cupric ion reducing antioxidant capacity (CUPRAC), and ferric ion reducing antioxidant power (FRAP), metal chelating ability, and phosphomolybdenum (PMD) assays. Extracts were also tested for inhibitory effects on cholinesterase, amylase, glucosidase, and tyrosinase enzymes. RA application positively impacted antioxidant and enzyme inhibitory activities, holding valuable implications in shaping the health-promoting properties of L. sativum. CONCLUSION: The untargeted metabolomics analysis showed a significant tissue-dependent modulation of bioactive compounds, determining no synergistic effect between applying phenolic compounds in combination. Specifically, the sole application of RA increased anthocyanins and hydroxyphenyl propanoic acid content on leaves, which was strictly related to enhancing the biological activities. © 2023 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

Traditional Chinese medicines treat ischemic stroke and their main bioactive constituents and mechanisms.

Ischemic stroke (IS) remains one of the leading causes of death and disability in humans. Unfortunately, none of the treatments effectively provide functional benefits to patients with IS, although many do so by targeting different aspects of the ischemic cascade response. The advantages of traditional Chinese medicine (TCM) in preventing and treating IS are obvious in terms of early treatment and global coordination. The efficacy of TCM and its bioactive constituents has been scientifically proven over the past decades. Based on clinical trials, this article provides a review of commonly used TCM patent medicines and herbal decoctions indicated for IS. In addition, this paper also reviews the mechanisms of bioactive constituents in TCM for the treatment of IS in recent years, both domestically and internationally. A comprehensive review of preclinical and clinical studies will hopefully provide new ideas to address the threat of IS.

Transcriptomics and metabolomics reveal the primary and secondary metabolism changes in Glycyrrhiza uralensis with different forms of nitrogen utilization.

The roots and rhizomes of Glycyrrhiza uralensis Fisch. represent the oldest and most frequently used herbal medicines in Eastern and Western countries. However, the quality of cultivated G. uralensis has not been adequate to meet the market demand, thereby exerting increased pressure on wild G. uralensis populations. Nitrogen, vital for plant growth, potentially influences the bioactive constituents of plants. Yet, more information is needed regarding the effect of different forms of nitrogen on G. uralensis. G. uralensis seedlings were exposed to a modified Hoagland nutrient solution (HNS), varying concentrations of nitrate (KNO3), or ammonium (NH4)2SO4. We subsequently obtained the roots of G. uralensis for physiology, transcriptomics, and metabolomics analyses. Our results indicated that medium-level ammonium nitrogen was more effective in promoting G. uralensis growth compared to nitrate nitrogen. However, low-level nitrate nitrogen distinctly accelerated the accumulation of flavonoid ingredients. Illumina sequencing of cDNA libraries prepared from four groups-treated independently with low/medium NH4 + or NO3 - identified 364, 96, 103, and 64 differentially expressed genes (DEGs) in each group. Our investigation revealed a general molecular and physiological metabolism stimulation under exclusive NH4 + or NO3 - conditions. This included nitrogen absorption and assimilation, glycolysis, Tricarboxylic acid (TCA) cycle, flavonoid, and triterpenoid metabolism. By creating and combining putative biosynthesis networks of nitrogen metabolism, flavonoids, and triterpenoids with related structural DEGs, we observed a positive correlation between the expression trend of DEGs and flavonoid accumulation. Notably, treatments with low-level NH4 + or medium-level NO3 - positively improved primary metabolism, including amino acids, TCA cycle, and glycolysis metabolism. Meanwhile, low-level NH4 + and NO3 - treatment positively regulated secondary metabolism, especially the biosynthesis of flavonoids in G. uralensis. Our study lays the foundation for a comprehensive analysis of molecular responses to varied nitrogen forms in G. uralensis, which should help understand the relationships between responsive genes and subsequent metabolic reactions. Furthermore, our results provide new insights into the fundamental mechanisms underlying the treatment of G. uralensis and other Glycyrrhiza plants with different nitrogen forms.

[Quality evaluation of Lysimachiae Herba from different habitats based on simultaneous determination of multiple bioactive constituents combined with multivariate statistical analysis].

A method based on ultra-high performance liquid chromatography coupled with triple quadrupole linear ion trap-tandem mass spectrometry(UHPLC-QTRAP-MS/MS) was developed for the simultaneous determination of 41 bioactive constituents of flavonoids, organic acids, nucleosides, and amino acids in Lysimachiae Herba. The content of multiple bioactive constituents was compared among the samples from different habitats. The chromatographic separation was performed in a Waters XBridge®C_(18) column(4.6 mm×100 mm, 3.5 µm) at 30 ℃. The gradient elution was performed with 0.4% methanol(A)-formic acid water(B) as the mobile phase at a flow rate of 0.8 mL·min~(-1), and the multiple-reaction monitoring(MRM) mode was adopted. According to the content of 41 constituents, hierarchical cluster analysis(HCA), orthogonal partial least squares discriminant analysis(OPLS-DA), and gray relational analysis(GRA) were perfomed to comprehensively evaluate the samples from different habitats. The results showed that the 41 constituents exhibited good linear relationship within the tested concentration ranges, with the correlation coefficients(r) greater than 0.999 4. The method featured good precision, repeatability, and stability with the relative standard deviations(RSDs) less than 5.0%. The average recoveries of the 41 constituents ranged from 98.06% to 101.9%, with the RSDs of 0.62%-4.6%. HCA and OPLS-DA separated 48 batches of Lysimachiae Herba samples from different habitats into three categories: the producing areas in Sichuan and Chongqing, the producing areas in Jiangsu, Zhejiang, and Jiangxi, and the producing areas in Guizhou. The content of 41 constituents varied among the Lysimachiae Herba samples from different habitats. The GRA results revealed that the Lysimachiae Herba sample from Nanchong City, Sichuan Province had the best comprehensive quality. The method developed in this study was accurate and reliable and thus can be used for comprehensive evaluation of Lysimachiae Herba quality and provide basic information for the selection of habitats.

Multi-Omics Elucidates Difference in Accumulation of Bioactive Constituents in Licorice (Glycyrrhiza uralensis) under Drought Stress.

Licorice is a frequently applied herb with potential edible and medicinal value based on various flavonoids and triterpenes. However, studies on detailed flavonoid and triterpene metabolism and the molecular basis of their biosynthesis in licorice are very limited, especially under drought conditions. In the present study, we carried out transcriptome, proteome, and metabolome experiments. To ultimately combine three omics for analysis, we performed a bioinformatics comparison, integrating transcriptome data and proteome data through a Cloud platform, along with a simplified biosynthesis of primary flavonoids and triterpenoids in the KEGG pathway based on metabolomic results. The biosynthesis pathways of triterpenes and flavonoids are enriched at both gene and protein levels. Key flavonoid-related genes (PAL, 4CL, CHS, CHI, CYP93C, HIDH, HI4OMT, and CYP81E1_7) and representative proteins (HIDH, CYP81E1_7, CYP93C, and VR) were obtained, which all showed high levels after drought treatment. Notably, one R2R3-MYB transcription factor (Glyur000237s00014382.1), a critical regulator of flavonoid biosynthesis, achieved a significant upregulated expression as well. In the biosynthesis of glycyrrhizin, both gene and protein levels of bAS and CYP88D6 have been found with upregulated expression under drought conditions. Most of the differentially expressed genes (DEGs) and proteins (DEPs) showed similar expression patterns and positively related to metabolic profiles of flavonoid and saponin. We believe that suitable drought stress may contribute to the accumulation of bioactive constituents in licorice, and our research provides an insight into the genetic study and quality breeding in this plant.

Effect of Predry-treatment on the bioactive constituents and quality of avocado (Persea americana Mill.) oil from three cultivars growing in China.

Avocado oil has gained a lot of favor in foods and cosmetics because of its high-quality fatty acid composition and bioactive components. This study aimed to compare the effect of various predry-treatments on the yield and quality of avocado oil from three Chinese avocado (Persea americana Mill.) varieties (Hass, Reed, and Pinkerton). The results showed that drying methods had significant effect on the avocado oil yield and its composition. Among the three drying methods the highest yield was obtained by freeze drying, and Hass showed the highest yield in the three avocado varieties with its oil owning the lowest peroxide and anisidine value. Reed oil owned the highest levels of functional micronutrients (e.g., tocopherols, phenolics, squalene). Vacuum drying resulted in higher concentrations of tocopherols, phytosterols, phenolics, squalene, and thus rendered greater DPPH and ABTS scavenging activity. These results are important to improve the quality of Chinese avocado oil.

[Analysis and evaluation of bioactive constituents from different parts of Epimedium brevicornum].

A comprehensive analytical method based on ultra-fast liquid chromatography coupled with triple quadrupole/linear ion trap tandem mass spectrometry(UFLC-QTRAP-MS/MS) was established for simultaneous determination of the content of 45 bioactive constituents including flavonoids, alkaloids, amino acids, phenolic acids, and nucleosides in Epimedium brevicornum. The multiple bioactive constituents in leaves, petioles, stems and rhizomes of E. brevicornum were analyzed. The gradient elution was performed at 30 ℃ in an XBridge~® C_(18) column(4.6 mm×100 mm, 3.5 µm) with 0.4% formic acid aqueous solution-acetonitrile as the mobile phase at a flow rate of 0.8 mL·min~(-1). Single factor experiment and response surface methodology were employed to optimize the extraction conditions. Multivariate statistical analyses including systematic cluster analysis(SCA), principal component analysis(PCA), partial least squares discriminant analysis(PLS-DA), and one-way analysis of variance(One-way ANOVA) were carried out to classify the samples from different parts and identify different constituents. Grey relation analysis(GRA) and entropy weight-TOPSIS analysis were performed to build a multi-index comprehensive evaluation model for different parts of E. brevicornum. The results showed that there was a good relationship between the mass concentrations of 45 constituents and the corresponding peak areas, with the correlation coefficients(r) not less than 0.999 0. The precision, repeatability, and stability of the established method were good for all the target constituents in this study, with the relative standard deviations(RSDs) less than 5.0%(0.62%-4.9%) and the average recovery of 94.51%-105.7%. The above results indicated that the bioactive constituents varied in different parts of E. brevicornum, and the overall quality followed the trend of leaves > petioles > rhizomes > stems. This study verified the rationality of the Chinese Pharmacopoeia(2020 edition) stipulating that the medicinal part of E. brevicornum is the leaf. Moreover, our study indicated that the rhizome had the potential for medicinal development. The established method was accurate and reliable, which can be used to comprehensive evaluate and control the quality of E. brevicornum. This study provides data reference for clarifying the medicinal parts and rationally utilizing the resources of E. brevicornum.

Antibacterial and Antibiofilm Effects of Different Samples of Five Commercially Available Essential Oils.

Essential oils (EOs) have gained economic importance due to their biological activities, and increasing amounts are demanded everywhere. However, substantial differences between the same essential oil samples from different suppliers are reported-concerning their chemical composition and bioactivities-due to numerous companies involved in EOs production and the continuous development of online sales. The present study investigates the antibacterial and antibiofilm activities of two to four samples of five commercially available essential oils (Oregano, Eucalyptus, Rosemary, Clove, and Peppermint oils) produced by autochthonous companies. The manufacturers provided all EOs' chemical compositions determined through GC-MS. The EOs' bioactivities were investigated in vitro against Gram-positive (Staphylococcus aureus) and Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa). The antibacterial and antibiofilm effects (ABE% and, respectively, ABfE%) were evaluated spectrophotometrically at 562 and 570 nm using microplate cultivation techniques. The essential oils' calculated parameters were compared with those of three standard broad-spectrum antibiotics: Amoxicillin/Clavulanic acid, Gentamycin, and Streptomycin. The results showed that at the first dilution (D1 = 25 mg/mL), all EOs exhibited antibacterial and antibiofilm activity against all Gram-positive and Gram-negative bacteria tested, and MIC value > 25 mg/mL. Generally, both effects progressively decreased from D1 to D3. Only EOs with a considerable content of highly active metabolites revealed insignificant differences. E. coli showed the lowest susceptibility to all commercially available essential oils-15 EO samples had undetected antibacterial and antibiofilm effects at D2 and D3. Peppermint and Clove oils recorded the most significant differences regarding chemical composition and antibacterial/antibiofilm activities. All registered differences could be due to different places for harvesting the raw plant material, various technological processes through which these essential oils were obtained, the preservation conditions, and complex interactions between constituents.

Development of Phytochemical Delivery Systems by Nano-Suspension and Nano-Emulsion Techniques.

The awareness of the existence of plant bioactive compounds, namely, phytochemicals (PHYs), with health properties is progressively expanding. Therefore, their massive introduction in the normal diet and in food supplements and their use as natural therapeutics to treat several diseases are increasingly emphasized by several sectors. In particular, most PHYs possessing antifungal, antiviral, anti-inflammatory, antibacterial, antiulcer, anti-cholesterol, hypoglycemic, immunomodulatory, and antioxidant properties have been isolated from plants. Additionally, their secondary modification with new functionalities to further improve their intrinsic beneficial effects has been extensively investigated. Unfortunately, although the idea of exploiting PHYs as therapeutics is amazing, its realization is far from simple, and the possibility of employing them as efficient clinically administrable drugs is almost utopic. Most PHYs are insoluble in water, and, especially when introduced orally, they hardly manage to pass through physiological barriers and scarcely reach the site of action in therapeutic concentrations. Their degradation by enzymatic and microbial digestion, as well as their rapid metabolism and excretion, strongly limits their in vivo activity. To overcome these drawbacks, several nanotechnological approaches have been used, and many nanosized PHY-loaded delivery systems have been developed. This paper, by reporting various case studies, reviews the foremost nanosuspension- and nanoemulsion-based techniques developed for formulating the most relevant PHYs into more bioavailable nanoparticles (NPs) that are suitable or promising for clinical application, mainly by oral administration. In addition, the acute and chronic toxic effects due to exposure to NPs reported so far, the possible nanotoxicity that could result from their massive employment, and ongoing actions to improve knowledge in this field are discussed. The state of the art concerning the actual clinical application of both PHYs and the nanotechnologically engineered PHYs is also reviewed.

Plant-derived smoke water and karrikinolide (KAR1) enhance physiological activities, essential oil yield and bioactive constituents of Mentha arvensis L.

Introduction: The current study was carried out with the hypothesis that foliar application of plant-derived smoke water (PDSW) and karrikinolide (KAR1) might enhanced the plant growth, physiology, and essential oil production of the Mentha arvensis L. Karrikinolide (KAR1) is one of the most important bioactive constituents of PDSW. Methods: Mint (Mentha arvensis L.) was grown in natural conditions in the net-house. Different concentrations of PDSW (1:125, 1:250, 1:500 and 1:1000 v/v) and KAR1 (10-9 M, 10-8 M, 10-7 M and 10-6 M) were used as foliar-spray treatments, using double-distilled water as control. The PDSW was prepared by burning the dried wheat-straw that acted as a growth-promoting substance. Results: Foliar-spray treatment 1:500 v/v of PDSW and 10-8 M of KAR1 proved optimal for enhancing all morphological, physiological, and essential-oil yield related parameters. In comparison with the control, 1:500 v/v of PDSW and 10-8 M of KAR1 increased significantly (p ≤ 0.05) the height of mint plant (19.23% and 16.47%), fresh weight (19.30% and 17.44%), dry weight (35.36% and 24.75%), leaf area (18.22% and 17.46%), and leaf yield per plant (28.41% and 23.74%). In addition, these treatments also significantly increased the photosynthetic parameters, including chlorophyll fluorescence (12.10% and 11.41%), total chlorophyll content (25.70% and 20.77%), and total carotenoid content (29.77% and 27.18%). Likewise, 1:500 v/v of PDSW and 10-8 M of KAR1 significantly increased the essential-oil content (37.09% and 32.25%), essential oil productivity per plant (72.22% and 66.66%), menthol content (29.94% and 25.42%), menthyl acetate content (36.90% and 31.73%), and menthone content (44.38% and 37.75%). Furthermore, the TIC chromatogram of the GCMS analysis revealed the presence of 34 compounds, 12 of which showed major peak areas. Discussion: Treatment 1: 500 v/v of PDSW proved better than the treatment 10-8 M of KAR1 with regard to most of the parameters studied. The outcome of the study can be used as a recommendation tool for agricultural and horticultural crops, since it costs much lesser than that of KAR1. In fact, the foliar application of PDSW proved economical and played bioactive role at very low concentrations.

Edible mushrooms as potential functional foods in amelioration of hypertension.

Edible mushrooms are popular functional foods attributed to their rich nutritional bioactive constituent profile influencing cardiovascular function. Edible mushrooms are omnipresent in various prescribed Dietary Approaches to Stop Hypertension, Mediterranean diet, and fortified meal plans as they are rich in amino acids, dietary fiber, proteins, sterols, vitamins, and minerals. However, without an understanding of the influence of mushroom bioactive constituents, mechanism of action on heart and allergenicity, it is difficult to fully comprehend the role of mushrooms as dietary interventions in alleviating hypertension and other cardiovascular malfunctions. To accomplish this endeavor, we chose to review edible mushrooms and their bioactive constituents in ameliorating hypertension. Hypertension and cardiovascular diseases are interrelated and if the former is managed by dietary changes, it is postulated that overall heart health could also be improved. With a concise note on different edible varieties of mushrooms, a particular focus is presented on the antihypertensive potential of mushroom bioactive constituents, mode of action, absorption kinetics and bioavailability. Ergosterol, lovastatin, cordycepin, tocopherols, chitosan, ergothioneine, γ-aminobutyric acid, quercetin, and eritadenine are described as essential bioactives with hypotensive effects. Finally, safety concerns on allergens and limitations of consuming edible mushrooms with special reference to chemical toxins and their postulated metabolites are highlighted. It is opined that the present review will redirect toxicologists to further investigate mushroom bioactives and allergens, thereby influencing dietary interventions for heart health.

Antiviral and ROS scavenging potential of Carica papaya Linn and Psidium guajava leaves extract against HIV-1 infection.

Antiretroviral therapy is the only treatment option for HIV-infected patients; however, it has certain drawbacks in terms of developing multiple toxic side effects. Thus, there is a continuous need to explore safe and efficacious anti-retroviral agents. Carica papaya Linn and Psidium guajava are known for their various biological activities. In this study, we characterized the bioactive fractions of methanolic leaves extract from both plants using the High-resolution electrospray ionization mass spectrometry (HR-ESI-MS) technique, followed by the investigation of their potential as anti-HIV-1 and antioxidant agents through in vitro mechanistic assays. The anti-HIV-1 activity was examined in TZM-bl cells through luciferase gene assay against two different clades of HIV-1 strains, whereas the intracellular ROS generation was analyzed by Fluorescence-Activated Cell Sorting. Additionally, the mechanisms of action of these phyto-extracts were determined through the Time-of-addition assay. The characterization of Carica papaya Linn and Psidium guajava leaves extract through HR-ESI-MS fragmentation showed high enrichment of various alkaloids, glycosides, lipids, phenolic compounds, terpenes, and fatty acids like bioactive constituents. Both the phyto-extracts were found to be less toxic and exhibited potent antiviral activity against HIV-1 strains. Furthermore, the phyto-extracts also showed a decreased intracellular ROS in HIV-1 infected cells due to their high antioxidant potential. Overall, our study suggests the anti-HIV-1 potential of Carica papaya Linn and Psidium guajava leaves extract due to the synergistic action of multiple bioactive constituents.

Zootherapy as traditional therapeutic strategy in the Cholistan desert of Bahawalpur-Pakistan.

The use of traditional medicines has tremendously increased over the past few decades. Approximately 80% of the world's population relies on traditional medicines for their primary healthcare needs because of their cost effectiveness and efficiency with no or minimal side effects. Zootherapy refers to the use of medicines that are prepared or derived from animals or from their products. The current study documented the folk knowledge related to the practice of various animal-derived products and ethnozoological based drugs used as medicines by the residents of the Cholistan desert of Bahawalpur (Pakistan). In this regard 46 knowledgeable and reliable elderly people, hakims and spiritual healers ranging from 35-60 years of age having knowledge related to zootherapy were included in the current study. A field survey from February 2006 to November 2007 was conducted by interviewing the selected respondents through a structured questionnaire. They provided knowledge regarding the use of animals and their derived products in traditional medicine. The zootherapeutic knowledge was based on both domestic animals as well as wild animals. A total of 20 animal species were included in the study, among which nine animals were domestic while 11 were wild animals. Among selected animals, nine were mammals, four birds, four reptiles and three insects. It was reported that camel was the most commonly used (n = 32 respondents) among mammals while Pigeon (n = 39 respondents), Spiny-tailed lizard (n = 41 respondents) and Indian honey bee (n = 27 respondents) among birds, reptiles and insects, respectively, have significant use for the treatment of different diseases. Based on this communication we could recommend that this type of abandoned knowledge should be considered for the management and conservation of faunistic resources. However, the advantageous role of animals and their products was reported but more extensive research is required to explore the bioactive constituents in the raw material of these animals responsible for their beneficial effects.

Amalgamation of Nanotechnology for Delivery of Bioactive Constituents in Solid Tumors.

Solid tumor is one of the highly prevalent cancers among humans and the treatment is often restricted by drug resistance to chemotherapeutics. One of the main reasons might be attributed to the limited penetration ability of drugs through tumor tissues due to heterogeneity within the tumor microenvironment. Over the recent years, so much research has been carried out for developing phytochemicals as cancer therapeutic agents. These are well-established as potential candidates for preventing and treating cancer, especially solid tumors, but have limited clinical applications due to their large molecular size, low bioavailability, stability, and target specificity, along with other side effects when used at high concentrations. There has been a widely proposed nano delivery system of bioactive constituents to overcome these obstacles. This nanostructured system might be able to potentiate the action of plant constituents, by reducing the side effects at a lesser dose with improved efficacy. Indeed, nanosystems can deliver the bioactive constituents at a specific site in the desired concentration and avoid undesired drug exposure to normal tissues. Furthermore, these nanoparticles demonstrate high differential absorption efficiency in the target cells over normal cells by preventing them from interacting prematurely with the biological environment, enhancing the cellular uptake and retention effect in disease tissues, while decreasing the toxicity. This review discusses various treatment stratagems used for the management of solid tumors with special emphasis on nanocarrier systems as a potential treatment strategy for herbal drugs. This also covers a wide list of plants that are used for the treatment of solid tumors and cancers along with their mechanisms of action and enlists various nanocarrier systems used for different phytoconstituents. This review gives a brief idea about different plants and their constituents exploited for their anticancer/antitumor potential along with several nanocarrier systems employed for the same and gives future directions to stress the nanotechnology platform as a valuable approach for the prevention and treatment of solid tumors.