RESUMO
PREMISE: Light is essential for plants, and local populations exhibit adaptive photosynthetic traits depending on their habitats. Although plastic responses in morphological and/or physiological characteristics to different light intensities are well known, adaptive divergence with genetic variation remains to be explored. This study focused on Saxifraga fortunei (Saxifragaceae) growing in sun-exposed and shaded habitats. METHODS: We measured the leaf anatomical structure and photosynthetic rate of plants grown in their natural habitats and in a common greenhouse (high- and low-intensity light experimental sites). To assess differences in ecophysiological tolerance to high-intensity light between the sun and shade types, we evaluated the level of photoinhibition of photosystem II and the leaf mortality rate under high-intensity light conditions. In addition, population genetic analysis was conducted to investigate phylogenetic origins. RESULTS: Clear phenotypic differences were found between the sun and shade types despite their recent phylogenetic origin. The leaf anatomical structure and photosynthetic rate showed plastic changes in response to growing conditions. Moreover, the sun type had a well-developed palisade parenchyma and a higher photosynthetic rate, which were genetically fixed, and a lower level of photoinhibition under high-intensity light. CONCLUSIONS: Our findings demonstrate that light intensity is a selective pressure that can rapidly promote phenotypic divergence between the sun and shade types. While phenotypic changes in multiple photosynthetic traits were plastic, genetic divergence in specific traits related to adaptation to high-intensity light would be fundamental for ecotypic divergence to different light regimes.
Assuntos
Adaptação Fisiológica , Fotossíntese , Saxifragaceae , Saxifragaceae/genética , Saxifragaceae/fisiologia , Sistema Solar , Ecossistema , Variação Genética , Microclima , Genética Populacional , Folhas de Planta/anatomia & histologia , Folhas de Planta/fisiologiaRESUMO
Herein, we report the properties of nanostructured lipid carriers (NLCs) prepared with a gradient concentration of Bergenin (BGN) isolated from Pentaclethra macrophylla stem bark powder. A gradient concentration of BGN (BGN 0, 50, 100, 150, and 200 mg) was prepared in a 5 % lipid matrix consisting of Transcutol HP (75 %), Phospholipon 90H (15 %), and Gelucire 43/01 (10 %) to which a surfactant aqueous phase consisting of Tween 80, sorbitol, and sorbic acid was dissolved. The NLCs were evaluated by size, polydispersity index (PDI), zeta potential, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), encapsulation efficiency, and in vitro drug release. The result shows polydispersed nanoparticles with high drug encapsulation (94.26-99.50 %). The nanoparticles were mostly spherical, but those from the 50 mg BGN batch were more cuboidal than spherical. The drug release was highest from the latter to the tune of 40 % compared to the pure BGN solution, which released about 15 % BGN. The anti-inflammatory activity of the BGN-NLC and total plant extract was studied on lipopolysaccharide (LPS)-inflamed macrophages. The cell study showed that BGN and plant extract had low cytotoxicity on macrophages and exhibited a dose-dependent anti-inflammatory effect on the LPS-induced inflammatory process in macrophages.
Assuntos
Anti-Inflamatórios , Benzopiranos , Portadores de Fármacos , Lipídeos , Lipopolissacarídeos , Macrófagos , Nanopartículas , Lipopolissacarídeos/farmacologia , Animais , Camundongos , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Portadores de Fármacos/química , Benzopiranos/farmacologia , Benzopiranos/administração & dosagem , Benzopiranos/química , Nanopartículas/química , Lipídeos/química , Células RAW 264.7 , Liberação Controlada de Fármacos , Nanoestruturas/química , Saxifragaceae/química , Tamanho da Partícula , Inflamação/tratamento farmacológico , Inflamação/induzido quimicamente , Extratos Vegetais/farmacologia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/químicaRESUMO
Mountain biota survived the Quaternary cold stages most probably in peripheral refugia and/or ice-free peaks within ice-sheets (nunataks). While survival in peripheral refugia has been broadly demonstrated, evidence for nunatak refugia is still scarce. We generated RADseq data from three mountain plant species occurring at different elevations in the southeastern European Alps to investigate the role of different glacial refugia during the Last Glacial Maximum (LGM). We tested the following hypotheses. (i) The deep Piave Valley forms the deepest genetic split in the species distributed across it, delimiting two peripheral refugia. (ii) The montane to alpine species Campanula morettiana and Primula tyrolensis survived the LGM in peripheral refugia, while high-alpine to subnival Saxifraga facchinii likely survived in several nunatak refugia. (iii) The lower elevation species suffered a strong population decline during the LGM. By contrast, the higher elevation species shows long-term stability of population sizes due to survival on permanently ice-free peaks and small population sizes at present. We found peripheral refugia on both sides of the Piave Valley, which acted as a major genetic barrier. Demographic modelling confirmed nunatak survival not only for S. facchinii but also for montane to alpine C. morettiana. Altitudinal segregation influenced the species' demographic fluctuations, with the lower elevation species showing a significant population increase at the end of the LGM, and the higher elevation species either showing decrease towards the present or stable population sizes with a short bottleneck. Our results highlight the role of nunatak survival and species ecology in the demographic history of mountain species.
Assuntos
Altitude , Camada de Gelo , Refúgio de Vida Selvagem , Primula/genética , Genética Populacional , Densidade Demográfica , Saxifragaceae/genética , Europa (Continente)RESUMO
Mountains are among the most biodiverse places on Earth, and plant lineages that inhabit them have some of the highest speciation rates ever recorded. Plant diversity within the alpine zone - the elevation above which trees cannot grow-contributes significantly to overall diversity within mountain systems, but the origins of alpine plant diversity are poorly understood. Here, we quantify the processes that generate alpine plant diversity and their changing dynamics through time in Saxifraga (Saxifragaceae), an angiosperm genus that occurs predominantly in mountain systems. We present a time-calibrated molecular phylogenetic tree for the genus that is inferred from 329 low-copy nuclear loci and incorporates 73% (407) of known species. We show that upslope biome shifts into the alpine zone are considerably more prevalent than dispersal of alpine specialists between regions, and that the rate of upslope biome shifts increased markedly in the last 5 Myr, a timeframe concordant with a cooling and fluctuating climate that is likely to have increased the extent of the alpine zone. Furthermore, alpine zone specialists have lower speciation rates than generalists that occur inside and outside the alpine zone, and major speciation rate increases within Saxifraga significantly pre-date increased rates of upslope biome shifts. Specialisation to the alpine zone is not therefore associated with speciation rate increases. Taken together, this study presents a quantified and broad scale perspective of processes underpinning alpine plant diversity.
Assuntos
Saxifragaceae , Filogenia , Ecossistema , Clima , BiodiversidadeRESUMO
OBJECTIVE: The goal of this study was to explore the hypolipidemic effects of bergenin extracted from Saxifraga melanocentra Franch (S. melanocentra), which is a frequently utilized Tibetan medicinal plant known for its diverse bioactivities. Establishing a quality control system for black stem saxifrage is crucial to ensure the rational utilization of its medicinal resources. METHODS: A one-step polyamide medium-pressure liquid chromatography technique was applied to isolate and prepare bergenin from a methanol extract of S. melanocentra. A zebrafish model of hyperlipidemia was used to investigate the potential hypolipidemic effects of bergenin. RESULTS: The results revealed that bergenin exhibited substantial hypo efficacy in vivo. Specifically, bergenin significantly reduced the levels of triglycerides (TG), total cholesterol (TC), and low-density lipoprotein cholesterol (LDL-c) while simultaneously increasing high-density lipoprotein cholesterol (HDL-c) levels. At the molecular level, bergenin exerted its effects by inhibiting the expression of FASN, SREBF1, HMGCRα, RORα, LDLRα, IL-1ß, and TNF while promoting the expression of IL-4 at the transcriptional level. Molecular docking analysis further demonstrated the strong binding affinity of bergenin to proteins such as FASN, SREBF1, HMGCRα, RORα, LDLRα, IL-4, IL-1ß, and TNF. CONCLUSIONS: Findings indicate that bergenin modulates lipid metabolism by regulating lipid and cholesterol synthesis as well as inflammatory responses through signaling pathways associated with FASN, SREBF1, and RORα. These results position bergenin as a potential candidate for the treatment of hyperlipidemia.
Assuntos
Hiperlipidemias , Saxifragaceae , Animais , Hiperlipidemias/tratamento farmacológico , Hiperlipidemias/genética , Interleucina-4 , Simulação de Acoplamento Molecular , Peixe-Zebra , Triglicerídeos , LDL-Colesterol , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêuticoRESUMO
The Heuchera genus, a member of the Saxifragaceae family, encompasses a wide array of varieties and hybrids, serving both traditional medicinal and ornamental purposes. However, a significant knowledge gap persists in achieving efficient mass propagation of diverse Heuchera cultivars creating a substantial market void. To address this, our study focuses on expedited seedling regeneration by investigating leaf cutting and tissue culture techniques to offer novel insights to cultivators. Herein, we successfully rooted thirteen distinct cultivars from the Heuchera and Heucherella (Heuchera × Tiarella) genera through cutting. Moreover, in vitro culture experiments led to the successful induction of calli and shoots from petiole samples. Notably, variations in measured parameters were observed across cultivars in both cutting and tissue culture methodologies. When petiole explants were exposed to cytokinin 6-benzylaminopurine (BA) at concentrations of 0.5, 1.0, and 2.0 mg/L along with auxin α-naphthaleneacetic acid (NAA) at 0.5 mg/L, shoots were produced either directly or indirectly during the primary culture. Exposure to darkness and the application of 2,4-dichlorophenoxyacetic acid (2,4-D) did not promote shoot formation but were beneficial for callus stimulation. Interestingly, a negative correlation was observed between the ease of initiating cutting recovery and inducting tissue culture regeneration, suggesting that cultivars that easily regenerate through cutting might encounter difficulties during induction by tissue culture. In light of these findings, we devised a streamlined and effective protocol for rapid Heuchera propagation. This protocol involves micropropagation, directly acquiring adventitious shoots from primary cultures supplemented by cutting-based propagation methods.
Assuntos
Calosidades , Heuchera , Saxifragaceae , CogniçãoRESUMO
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), influenza A virus (IAV), and norovirus are global threats to human health. The application of effective virucidal agents, which contribute to the inactivation of viruses on hands and environmental surfaces, is important to facilitate robust virus infection control measures. Naturally derived virucidal disinfectants have attracted attention owing to their safety and eco-friendly properties. In this study, we showed that multiple Japanese Saxifraga species-derived fractions demonstrated rapid, potent virucidal activity against the SARS-CoV-2 ancestral strain and multiple variant strains, IAV, and two human norovirus surrogates: feline calicivirus (FCV) and murine norovirus (MNV). Condensed tannins were identified as active chemical constituents that play a central role in the virucidal activities of these fractions. At a concentration of 25 µg/mL, the purified condensed tannin fraction Sst-2R induced significant reductions in the viral titers of the SARS-CoV-2 ancestral strain, IAV, and FCV (reductions of ≥3.13, ≥3.00, and 2.50 log10 50% tissue culture infective doses [TCID50]/mL, respectively) within 10 s of reaction time. Furthermore, at a concentration of 100 µg/mL, Sst-2R induced a reduction of 1.75 log10 TCID50/mL in the viral titers of MNV within 1 min. Western blotting and transmission electron microscopy analyses revealed that Sst-2R produced structural abnormalities in viral structural proteins and envelopes, resulting in the destruction of viral particles. Furthermore, Saxifraga species-derived fraction-containing cream showed virucidal activity against multiple viruses within 10 min. Our findings indicate that Saxifraga species-derived fractions containing condensed tannins can be used as disinfectants against multiple viruses on hands and environmental surfaces. IMPORTANCE SARS-CoV-2, IAV, and norovirus are highly contagious pathogens. The use of naturally derived components as novel virucidal/antiviral agents is currently attracting attention. We showed that fractions from extracts of Saxifraga species, in the form of a solution as well as a cream, exerted potent, rapid virucidal activities against SARS-CoV-2, IAV, and surrogates of human norovirus. Condensed tannins were found to play a central role in this activity. The in vitro cytotoxicity of the purified condensed tannin fraction at a concentration that exhibited some extent of virucidal activity was lower than that of 70% ethanol or 2,000 ppm sodium hypochlorite solution, which are popular virucidal disinfectants. Our study suggests that Saxifraga species-derived fractions containing condensed tannins can be used on hands and environmental surfaces as safe virucidal agents against multiple viruses.
Assuntos
Desinfetantes , Vírus da Influenza A , Norovirus , Proantocianidinas , SARS-CoV-2 , Saxifragaceae , Desinfetantes/farmacologia , Vírus da Influenza A/efeitos dos fármacos , Norovirus/efeitos dos fármacos , Proantocianidinas/farmacologia , SARS-CoV-2/efeitos dos fármacos , Saxifragaceae/química , TaninosRESUMO
Seven new phenylhexanoids, (S)-(+)-3,4-dihydroxy-11-methoxyphenylhex-9-one (1), (E) 3,4-dihydroxy-phenylhex-10-en-9-one (2), (E)-4-hydroxyphenylhex-10-en-9-one (3), (R)-(-)-3,4,11-trihydroxyphenylhex-9-one 11-O-ß-d-glucopyranoside (4), (R)-(-)-4,11-dihydroxyphenylhex-9-one 11-O-ß-d-glucopyranoside (5), phenylhex-4,9,11-triol 11-O-ß-d-glucopyranoside (6), and 9-O-acetyl-phenylhex-4,9,11-triol 11-O-ß-d-glucopyranoside (7), were isolated and identified from Tibetan medicine Saxifraga umbellulata var. pectinate. The antioxidant activities of these compounds were evaluated using the DPPH and ABTS radical scavenging experiments. In the ABTS experiment, compounds 1 (IC50 13.99 ± 2.53 µM) and 2 (IC50 13.11 ± 0.94 µM) exhibited significantly better antioxidant activity than L-ascorbic acid (IC50 23.51 ± 0.44 µM).
Assuntos
Antioxidantes , Saxifragaceae , Antioxidantes/farmacologia , Antioxidantes/química , Saxifragaceae/químicaRESUMO
Selection leading to adaptation to interactions may generate rapid evolutionary feedbacks and drive diversification of species interactions. The challenge is to understand how the many traits of interacting species combine to shape local adaptation in ways directly or indirectly resulting in diversification. We used the well-studied interactions between Lithophragma plants (Saxifragaceae) and Greya moths (Prodoxidae) to evaluate how plants and moths together contributed to local divergence in pollination efficacy. Specifically, we studied L. bolanderi and its two specialized Greya moth pollinators in two contrasting environments in the Sierra Nevada in California. Both moths pollinate L. bolanderi during nectaring, one of them-G. politella-also while ovipositing through the floral corolla into the ovary. First, field surveys of floral visitors and the presence of G. politella eggs and larvae in developing capsules showed that one population was visited only by G. politella and few other pollinators, whereas the other was visited by both Greya species and other pollinators. Second, L. bolanderi in these two natural populations differed in several floral traits putatively important for pollination efficacy. Third, laboratory experiments with greenhouse-grown plants and field-collected moths showed that L. bolanderi was more efficiently pollinated by local compared to nonlocal nectaring moths of both species. Pollination efficacy of ovipositing G. politella was also higher for local moths for the L. bolanderi population, which relies more heavily on this species in nature. Finally, time-lapse photography in the laboratory showed that G. politella from different populations differed in oviposition behavior, suggesting the potential for local adaptation also among Greya populations. Collectively, our results are a rare example of components of local adaptation contributing to divergence in pollination efficacy in a coevolving interaction and, thus, provide insights into how geographic mosaics of coevolution may lead to coevolutionary diversification in species interactions.
Assuntos
Mariposas , Saxifragaceae , Animais , Feminino , Polinização , Flores , Adaptação Fisiológica , PlantasRESUMO
Hybridization and polyploidy are major forces in plant evolution. Homoploid hybridization can generate new species via hybrid speciation, or modify extant evolutionary lineages through introgression. Polyploidy enables instantaneous reproductive isolation from the parental lineage(s) and is often coupled with evolutionary innovations, especially when linked to hybridization. While allopolyploidy is a well-known and common mechanism of plant speciation, the evolutionary role of autopolyploidy might have been underestimated. Here, we studied the saxifrages of Saxifraga subsection Saxifraga in the Pyrenees, which easily hybridise and include polyploid populations of uncertain origin, as a model to unravel evolutionary consequences and origin of hybridization and polyploidy. Additionally, we investigate the phylogenetic relationship between the two subspecies of the endemic S. pubescens to ascertain whether they should rather be treated as different species. For these purposes, we combined ploidy-informed restriction associated DNA analyses, plastid DNA sequences and morphological data on a comprehensive population sample of seven species. Our results unravel multiple homoploid hybridization events at the diploid level between different species pairs, but with limited evolutionary impact. The ploidy-informed analyses reveal that all tetraploid populations detected in the present study belong to the widespread alpine species S. moschata. Although of autopolyploid origin, they are to some extent morphologically differentiated and underwent a different evolutionary pathway than their diploid parent. However, the high plastid DNA diversity and the internal structure within eastern and western population groups suggest multiple origins of the polyploids. Finally, our phylogenetic analyses show that S. pubescens and S. iratiana are clearly not sister lineages, and should consequently be considered as independent species.
Assuntos
Saxifragaceae , Filogenia , Poliploidia , Hibridização Genética , Ploidias , PlantasRESUMO
Astilbe chinensis (A. chinensis) is a perennial herb that is used to treat chronic bronchitis and pain. The anticancer activity of 3ß,6ßdihydroxyurs12en27oic acid (ACT3), a major component isolated from A. chinensis, has not yet been investigated in detail. The purpose of the present study was to investigate the histone deacetylase (HDAC) inhibitory and anticancer activities of ACT3 compared with suberoylanilide hydroxamic acid (SAHA) in MCF7 human breast cancer cells. The purity of ACT3 was determined using highperformance liquid chromatography. In the present study, the effects of ACT3 on anticancer effects of MCF7 cells were determined by measuring the level of apoptotic cell death and cell cycle regulator using flow cytometry analysis and western blot analysis, respectively. The effects of ACT3 on HDAC enzyme activity were measured using assay kits. ACT3 and SAHA increased the levels of acetylated histone H3 and reduced the levels of HDAC1 and HDAC3 in MCF7 cells. ACT3 significantly decreased the cell viability in a concentrationdependent manner and induced different morphological changes at high concentrations. ACT3 and SAHA significantly inhibited the colony formation in MCF7 cells. ACT3 inhibited total HDAC activity in a dosedependent manner. ACT3 significantly reduced the expression levels of cyclin D1 and cyclindependent kinase 4, and upregulated the expression levels of p21WAF1 and p53. A significant increase in the G1 phase cell population was observed in MCF7 cells and ACT3 induced apoptosis by reducing the ratio of Bcell lymphoma2 (Bcl2)/Bcl2associated X (Bax) and releasing cleaved caspase 9. Additionally, ACT3 significantly increased autophagic cell death by inhibiting the serinethreonine kinase/mammalian target of the rapamycin pathway. Autophagy induction was confirmed via acridine orange staining. ACT3 significantly increased the pERK1/2 and p21 in MCF7 cells. Thus, the activated ERK pathway played an important role in cell cycle arrest and apoptosis via ERKdependent induction of p21 in MCF7 cells. These data indicated that ACT3 can be used as a promising anticancer agent to overcome the limitations and reduce the side effects of conventional anticancer drugs.
Assuntos
Antineoplásicos , Neoplasias da Mama , Inibidores de Histona Desacetilases , Saxifragaceae , Feminino , Humanos , Apoptose , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Proliferação de Células , Inibidores de Histona Desacetilases/isolamento & purificação , Inibidores de Histona Desacetilases/farmacologia , Inibidores de Histona Desacetilases/uso terapêutico , Células MCF-7 , Proteínas Proto-Oncogênicas c-akt , Proteínas Proto-Oncogênicas c-bcl-2 , Serina-Treonina Quinases TOR , Vorinostat/farmacologia , Vorinostat/uso terapêutico , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Saxifragaceae/químicaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: People of all ages experience injuries, whether mild or severe. The most available option to treat wounds as an alternative to allopathic care in both urban and rural populations is traditional medicine, which is mostly target inflammation. Bergenia ciliata (Haw.) Sternb rhizome and leaf powder are used in Ayurveda and local communities for various ailments including healing of wounds and burns. Owing to this property it is traditionally known as "Zakham-e-hayat" (wound healer). AIM OF THE STUDY: In the present study, we compared biological activity and wound healing potential of B. ciliata rhizome (R) extract and bergenin, a glycoside isolated from B. ciliata. MATERIALS AND METHODS: Reverse-phase high performance liquid chromatography (RP-HPLC) was performed to analyze polyphenols and bergenin in B. ciliata R extract. Samples were subjected to in vitro antioxidant assays including free radical scavenging, ferric chloride reducing power and total antioxidant capacity. Micro-broth dilution method, brine shrimp lethality assay and isolated RBC hemolysis assay were conducted to assess in vitro antibacterial and cytotoxic activities. Moreover, in vivo wound healing potential was determined by an excision wound model in mice. RESULTS: RP-HPLC showed significant content of polyphenols and bergenin (6.05 ± 0.12 µg/mg) in B. ciliata R extract. Crude extract possesses higher overall antioxidant and antibacterial capacities than bergenin due to presence of multiple phytoconstituents in extract. Both samples showed low hemolytic activity indicating their safe profile. Furthermore, mice treated with B. ciliata R extract depicted substantial decrease in wound area (99.3%; p < 0.05) as compared to bergenin, which showed 88.8% of wound closure after 12 days of treatment. Additionally, both treatments reduced epithelization duration by 1.6- and 1.4-fold in B. ciliata R extract (12.0 ± 0.6 days) and bergenin (14.2 ± 0.8 days) treated mice, respectively. This was supported by histopathological examination that showed greater epithelization, fibroblast proliferation, collagen synthesis, and revascularization in mice treated with B. ciliata R. CONCLUSION: Concisely, it is evident that B. ciliata R contains phytoconstituents in addition to bergenin, which potentiated wound healing activity of the extract. Hence, B. ciliata R is good source of compounds for treating wounds.
Assuntos
Antioxidantes , Saxifragaceae , Camundongos , Animais , Antioxidantes/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/química , Benzopiranos/farmacologia , Benzopiranos/uso terapêutico , Saxifragaceae/química , Polifenóis , Antibacterianos/farmacologiaRESUMO
Acute liver damage (ALD) can cause biochemical and pathological changes, which can lead to major complications and even death. The goal of the study was to examine the therapeutic efficacy of liposomes of Bergenia ciliata extract against thioacetamide-induced liver damage in rats. Liposomal batches of B. ciliata extract were prepared by altering the kind and amount of phospholipids and characterized through various physiochemical properties such as laser diffraction, TEM, encapsulation efficiency, stability and in-vitro release studies. In-vivo hepatoprotective studies were performed on TAA-induced acute hepatic damage model. Further, in-silico studies of bergenin against the three hepatic damage markers viz. TGF-ß1, TNF-α and interleukin-6 were also performed. Laser diffraction and TEM showed that most stable liposome batch of B. ciliata extract were in the range of 678-1170 nm with encapsulation efficiency of 84.3±3.5. Extract was found to be rapidly dissociated from B. ciliata liposomes in HCl than PBS, according to in-vitro release data. In-vivo data revealed a significant decline in LFT indicators, amelioration of pathological changes and high bergenin bioavailability in the liposomal group. Protective activity of bergenin against ALD targets like TGF-ß1, TNF-α and interleukin-6 was anticipated via molecular docking research. As a result, the current findings of the study indicate that B. ciliata liposomes and bergenin have promising ameliorative potential in the management of ALD.
Assuntos
Lipossomos , Extratos Vegetais , Saxifragaceae , Animais , Ratos , Interleucina-6 , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Saxifragaceae/química , Fator de Crescimento Transformador beta1 , Fator de Necrose Tumoral alfaRESUMO
Yttrium (Y) has gained importance in high tech applications and, together with the other rare earth elements (REEs), is also considered to be an emerging environmental pollutant. The alpine plant Saxifraga paniculata was previously shown to display high metal tolerance and an intriguing REE accumulation potential. In this study, we analysed soil grown commercial and wild specimens of Saxifraga paniculata to assess Y accumulation and shed light on the uptake pathway. Laser ablation inductively coupled plasma mass spectrometry and synchrotron-based micro X-ray fluorescence spectroscopy was used to localise Y within the plant tissues and identify colocalized elements. Y was distributed similarly in commercial and wild specimens. Within the roots, Y was mostly located in the epidermis region. Translocation was low, but wild individuals accumulated significantly more Y than commercial ones. In plants of both origins, we observed consistent colocalization of Al, Fe, Y and Ce in all plant parts except for the hydathodes. This indicates a shared pathway during translocation and could explained by the formation of a stable organic complex with citrate, for example. Our study provides important insights into the uptake pathway of Y in S. paniculata, which can be generalised to other plants.
Assuntos
Metais Terras Raras , Saxifragaceae , Humanos , Ítrio/química , Metais Terras Raras/análise , Solo/química , PlantasRESUMO
Herbal products have been used in traditional systems of medicine and by ethnic healers for ages to treat various diseases. Currently, it is estimated that about 80% of people worldwide use herbal traditional medicines against various ailments, partly due to easy accessibility and low cost, and the lower side effects they pose. Bergenia ligulata, a herb ranging from the Himalayas to the foothills, including the north-eastern states of India, has traditionally been used as a remedy against various diseases, most prominently kidney stones. The medicinal properties of B. ligulata have been attributed to bergenin, its most potent bioactive component. Apart from bergenin, the other compounds available in B. ligulata are arbutin, gallic acid, protocatechuic acid, chlorogenic acid, syringic acid, catechin, ferulic acid, afzelechin, paashaanolactone, caryophyllene, 1,8-cineole, ß-eudesmol, stigmasterol, ß-sitosterol, parasorbic acid, 3-methyl-2-buten-1-ol, phytol, terpinen-4-ol, tannic acid, isovalaric acid, avicularin, quercetin, reynoutrin, and sitoinoside I. This review summarizes various medicinal properties of the herb, along with providing deep insight into its bioactive molecules and their potential roles in the amelioration of human ailments. Additionally, the possible mechanism(s) of action of the herb's anti-urolithiatic, antioxidative, antipyretic, anti-diabetic, anti-inflammatory and hepatoprotective properties are discussed. This comprehensive documentation will help researchers to better understand the medicinal uses of the herb. Further studies on B. ligulata can lead to the discovery of new drug(s) and therapeutics for various ailments.
Assuntos
Antipiréticos , Catequina , Plantas Medicinais , Saxifragaceae , Humanos , Quercetina , Arbutina , Ácido Clorogênico , Estigmasterol , Eucaliptol , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ácido Gálico , Taninos , FitolRESUMO
Saxifraga species are widely distributed in alpine and arctic regions in the Northern hemisphere. Highly morphological diversity within this genus brings great difficulties for species identification, and their typical highland living properties make it interesting how they adapt to the extreme environment. Here, we newly generated the chloroplast (cp) genomes of two Saxifraga species and compared them with another five Saxifraga cp genomes to understand the characteristics of cp genomes and their potential roles in highland adaptation. The genome size, structure, gene content, GC content, and codon usage pattern were found to be highly similar. Cp genomes ranged from 146,549 bp to 151,066 bp in length, most of which comprised 130 predicted genes. Yet, due to the expansion of IR regions, the second copy of rps19 in Saxifraga stolonifera was uniquely kept. Through sequence divergence analysis, we identified seven hypervariable regions and detected some signatures of regularity associated with genetic distance. We also identified 52 to 89 SSRs and some long repeats among seven Saxifraga species. Both ML and BI phylogenetic analyses confirmed that seven Saxifraga species formed a monophyletic clade in the Saxifragaceae family, and their intragenus relationship was also well supported. Additionally, the ndhI and ycf1 genes were considered under positive selection in species inhabiting relatively high altitudes. Given the conditions of intense light and low CO2 concentration in the highland, the products of these two genes might participate in the adaptation to the extreme environment.
Assuntos
Genoma de Cloroplastos , Saxifragaceae , Dióxido de Carbono , Evolução Molecular , Repetições de Microssatélites , Filogenia , Saxifragaceae/genéticaRESUMO
In this study, a 100 g sample of Saxifraga atrata was processed to separate 1.3 g of 11-O-(4'-O-methylgalloyl)-bergenin (Fr1) after 1 cycle of MCI GEL® CHP20P medium pressure liquid chromatography using methanol/water. Subsequently, COX-2 affinity ultrafiltration coupled with reversed-phase liquid chromatography was successfully used to screen for potential COX-2 ligands in this target fraction (Fr1). After 20 reversed-phase liquid chromatography runs, 74.1 mg of >99% pure 11-O-(4'-O-methylgalloyl)-bergenin (Fr11) was obtained. In addition, the anti-inflammatory activity of 11-O-(4'-O-methylgalloyl)-bergenin was further validated through molecular docking analyses which suggested it was capable of binding strongly to ALOX15, iNOS, ERBB2, SELE, and NF-κB. As such, the AA metabolism, MAPK, and NF-κB signaling pathways were hypothesized to be the main pathways through which 11-O-(4'-O-methylgalloyl)-bergenin regulates inflammatory responses, potentially functioning by reducing pro-inflammatory cytokine production, blocking pro-inflammatory factor binding to cognate receptors and inhibiting the expression of key proteins. In summary, affinity ultrafiltration-HPLC coupling technology can rapidly screen for multi-target bioactive components and when combined with molecular docking analyses, this approach can further elucidate the pharmacological mechanisms of action for these compounds, providing valuable information to guide the further development of new multi-target drugs derived from natural products.
Assuntos
Saxifragaceae , Ultrafiltração , Anti-Inflamatórios/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Ciclo-Oxigenase 2/metabolismo , Espectrometria de Massas , Simulação de Acoplamento Molecular , NF-kappa B , Saxifragaceae/metabolismo , Ultrafiltração/métodosRESUMO
Saxifraga atrata is an important traditional Tibetan medicine used to treat cough and pneumonia, and has tremendous medicinal potential. In this study, we devised a technique to separate 1,1-diphenyl-2-picrylhydrazyl inhibitors from a methanol extract of S. atrata. The material was first processed using MCI GEL CHP20P medium-pressure liquid chromatography, yielding 1.1 g of the target fraction Fr2. Subsequently, online hydrophilic interaction liquid chromatography-1,1-diphenyl-2-picrylhydrazyl assay was used to identify prospective 1,1-diphenyl-2-picrylhydrazyl inhibitors, and two 1,1-diphenyl-2-picrylhydrazyl inhibitor fractions (Fr24 and Fr25) were identified from Fr2. Then, medium-pressure preparation was continued using an XIon column to separate two 1,1-diphenyl-2-picrylhydrazyl inhibitor fractions (Fr24 and Fr25). The target compound was concentrated in fractions Fr24 and Fr25 using reverse-phase liquid chromatography during further separation procedures. Finally, the purity, structure, and 1,1-diphenyl-2-picrylhydrazyl inhibitory activity of the isolated 1,1-diphenyl-2-picrylhydrazyl inhibitors were determined. Two 1,1-diphenyl-2-picrylhydrazyl inhibitors (adenosine with the half maximal inhibitory concentration of 66.87 ± 14.33 µM and (-)-4-O-(E)-caffeoyl-l-threonic acid with the half maximal inhibitory concentration of 59.06 ± 5.02 µM) were isolated with purities exceeding 95%. The results showed that this technology is effective in the targeted separation of antioxidants from natural products.
Assuntos
Antioxidantes , Saxifragaceae , Antioxidantes/análise , Compostos de Bifenilo , Cromatografia Líquida de Alta Pressão/métodos , Picratos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Estudos ProspectivosRESUMO
BACKGROUND: Cancer remains a major world health issue due to its high morbidity and mortality rate. Plant based natural products (NPs) have played vital role in discovery of valuable anti-cancer drugs. Darjeeling Himalayan region has a rich diversity of therapeutic plants that can be utilized for development of novel drugs. AIM: We previously reported cytotoxic potential of rhizome extract of A.rivularis, a Darjeeling himalayan herb. Present study reports isolation and characterization of a phytosteroid from the plant rhizome in a bioassay-guided approach and evaluation of its anti-tumorigenic potential. RESULTS: The phytosteroid was characterized as stigmasta-5(6), 22(23)-dien-3-beta-yl acetate (A11) by various spectrometric techniques (IR, NMR, MS etc.). The catalytic inhibition and structural alteration of human dihydrofolate reductase (hDHFR) by A11 was evaluated using methotrexate (MTX), a DHFR inhibitor anticancer drug as a reference. A11 inhibited hDHFR activity with IC50 values of 1.20 µM A11 caused concentration dependent quenching of tryptophan fluorescence of hDHFR suggesting its effect on alteration of enzyme structure. Molecular docking of A11 on crystal structure of hDHFR revealed significant interaction with free energy of binding and Ki values of -10.86 kcal/mol and 11 nM, respectively. Subsequent in vitro studies at cellular level showed a relatively greater cytotoxic effect of A11 against human kidney (ACHN, IC50 60 µM) and liver (HepG2, IC5070 µM) cancer cells than their respective normal cells (HEK-293, IC50 350 µM and WRL-68, IC50 520 µM). Scanning electron microscopy of A11 treated cells revealed the morphological feature of apoptosis, like cell rounding and surface detachment, membrane blebbing, loss of cilia and increased number of pores of decreased sizes. A11 mediated apoptosis of cancer cells was found to be correlated with induction of intracellular of reactive oxygen species (ROS) level and fragmentation of genomic DNA.
Assuntos
Antineoplásicos , Fitosteróis , Saxifragaceae , Acetatos/farmacologia , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Ésteres , Células HEK293 , Humanos , Simulação de Acoplamento Molecular , Saxifragaceae/metabolismo , Esteroides , Tetra-Hidrofolato Desidrogenase/química , Tetra-Hidrofolato Desidrogenase/genética , Tetra-Hidrofolato Desidrogenase/metabolismoRESUMO
Two olean-27-carboxylic acid-type triterpenoids (1 and 2) were isolated from Saxifraga umbellulata (Saxifragaceae), representing the first case in the chemical discoveries of genus Saxifraga. Compound 1 was determined to be a new compound named 'Saxifragic acid' based on the comprehensive spectroscopic and X-ray crystallographic analyses. Compound 2 (deacetylated saxifragic acid) is a known compound reported before, but its absolute configuration through X-ray crystallographic analyses was first described here. In addition, their cytotoxicity against five digestive human cancer cell lines (BGC-823, GBC-SD, CCC-9810, HT-29, and HepG2) and hepatoprotective activity against CCl4 -induced L-o2 cell injury inâ vitro were evaluated. Interestingly, UPLC-QTOFMS analysis showed that these two compounds could be used as chemical markers to discriminate between S.â umbellulata and S.â tangutica, both of which are used for the treatment of hepatobiliary diseases in traditional Tibetan medicine.