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1.
Ther Deliv ; 2024 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-38651887

RESUMO

Despite having current advanced therapy, vulvovaginal candidiasis (VVC) remains a common yet debated healthcare-associated topic worldwide due to multi-drug resistance Candida species. In our review, we outlined and highlighted upcoming values with scope of existing and emerging information regarding the possibility of using various natural molecules combined with modern technology that shows promising anti-candida activity in VVC. Furthermore, in this review, we compiled herbal drug molecules and their nanocarriers approach for enhancing the efficacy and stability of herbal molecules. We have also summarized the patent literature available on herbal drug molecules and their nanoformulation techniques that could alternatively become a new innovative era to combat resistance VVC.


There is a type of fungi called Candida that is responsible for infections like vulvovaginal candidiasis in the human vagina. Due to resistance of currently available antifungal medicines, there are side effects on the body. Therefore, researchers are studying and preparing natural-based medicine from plants which may provide very good effects on human health. Also, herbal-based medicines have shown evidence based good antifungal activity. Combinations of herbal drugs with very small-sized particles called nanomaterials have added advantage as it helps herbs (drug) to reach their target. Its activity is enhanced as it stays for longer time in the body. So, in the future more research is needed to make sure plant medicines are safe and work well on vaginal infections and its uses should be promoted so that could be a good solution for treating vaginal candidiasis.

2.
Nat Prod Res ; : 1-6, 2024 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-38163964

RESUMO

In this recent investigation, the focus centred on exploring the potential phytoconstituents within the bark of Dysoxylum malabaricum. A profiling strategy employing LC-HRMS (Liquid Chromatography-High Resolution Mass Spectrometry) was implemented for the rapid identification of compounds from the bark extract. The crude extract underwent fractionation, resulting in the isolation of four previously known compounds (1-4) and a novel cycloartane triterpenoid named Mahamanalactone A (5). Compound 5 represents a cycloartane triterpenoid with a modified ring-A, featuring £-caprolactone fusion at positions 4 and 5, distinguishing it from other reported compounds where £-caprolactone is typically fused at positions 3 and 4. Cytotoxicity assessment revealed that the newly identified compound 5 exhibited a moderate cytotoxic profile (IC50 29 to 78 µM) against a panel of cancer cell lines.

3.
Anticancer Agents Med Chem ; 24(5): 317-333, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-37936467

RESUMO

AIMS: The aim of this study is to isolate the Millettia pinnata (Karanj) leaf extract for pure compound with anticancer properties and to study the molecular target of the isolates in non-small cell lung cancer cell lines. BACKGROUND: In our earlier research Millettia pinnata leaf extract has demonstrated potential anticancer activities. Thus, in pursuit of the bioactive compounds, the most potential active extract from our previous study was purified. Furthermore, the anticancer properties of the isolated compound karanjin was studied and aimed for apoptosis and restraining growth. METHODS: A novel method was developed through column chromatography for isolation and purification of the compound karanjin from leaf chloroform extract. The purified component was then characterised using FTIR, mass spectrometry, and NMR. An MTT-based cytotoxicity assay was used to analyse cell cytotoxicity, whereas fluorescence staining was used for apoptosis and reactive oxygen species inhibition quantification. Furthermore, the real-time PCR assay was used to determine the molecular mechanism of action in cells causing cytotoxicity induced by karanjin dosing. RESULTS: The anticancer activity of karanjin in A549 cell line exhibited prominent activity revealing IC50 value of 4.85 µM. Conferring the predicted molecular pathway study, karanjin restrains the proliferation of cancer cells through apoptosis, which is controlled by extrinsic pathway proteins FAS/FADD/Caspases 8/3/9. Downregulation of KRAS and dependent gene expression also stopped cell proliferation. CONCLUSION: Karanjin has been identified as a compound with potential effect in non-small cell lung cancer cells. Molecular mechanism for apoptosis and inhibition of reactive oxygen species induced through H2O2 were observed, concluding karanjin have medicinal and antioxidant properties.


Assuntos
Benzopiranos , Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Humanos , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Espécies Reativas de Oxigênio/metabolismo , Peróxido de Hidrogênio/farmacologia , Neoplasias Pulmonares/tratamento farmacológico , Linhagem Celular Tumoral , Apoptose , Extratos Vegetais/farmacologia , Modelos Teóricos
4.
Naunyn Schmiedebergs Arch Pharmacol ; 396(10): 2331-2346, 2023 10.
Artigo em Inglês | MEDLINE | ID: mdl-37178275

RESUMO

Erigeron annuus L. is a flowering herb of North America, Europe, Asia and Russia. This plant is used as folk medicine in China for the cure of indigestion, enteritis, epidemic hepatitis, haematuria and diabetes. Phytochemical studies showed the presence of 170 bioactive compounds like coumarins, flavonoids, terpenoids, polyacetylenic compounds; γ-pyrone derivatives, sterols and various caffeoylquinic acids derived from the essential oil and organic extracts from its various parts such as aerial parts, roots, leaves, stems and flowers. The pharmacological studies demonstrated various extracts and the compounds of E. annuus to exhibit anti-fungal, anti-atherosclerosis, anti-inflammatory, antidiabetic, phytotoxic, cytoprotective, antiobesity and antioxidant activities. This article covers a critical compendious on geographical distribution, botanical description, phytochemistry, ethnomedicinal uses and pharmacological activities of E. annuus. However, further in-depth studies are needed to determine the medical uses of E. annuus and its chemical constituents, pharmacological activities and clinical applications.


Assuntos
Erigeron , Medicina Tradicional , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Compostos Fitoquímicos/farmacologia , Folhas de Planta , Fitoterapia
5.
Indian J Pharmacol ; 55(6): 385-394, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38174535

RESUMO

Thymus serpyllum L. from the Lamiaceae family is an underexplored perennial medicinal shrub with traditional usage in treating respiratory and gastrointestinal issues in the upper foothills of India. This review aims to provide a comprehensive assessment of current knowledge concerning the traditional uses, phytochemistry, and pharmacology of T. serpyllum. The primary objective is to collect updated information on this plant and encourage further in vivo and in vitro research to validate local claims. Notably, the essential oil derived from T. serpyllum has gained significant attention as a plant-derived product due to its diverse pharmacological properties, including antioxidative, antimicrobial, anti-inflammatory, and anticancer activities. Ethnomedicinal research revealed a vast scope of T. serpyllum in developing new drugs to address numerous health sector challenges. While T. serpyllum has been used widely, pharmacological studies are not enough. Most studies are either in vivo or in vitro. More studies are required to assess these medicinal claims through well-planned pharmacological experiments. This review will provide the groundwork for future research. While T. serpyllum has been put to considerable conventional use, pharmacological studies are insufficient; most studies are either in vivo or in vitro. More compound isolation, comprehensive pharmacological analysis, and exploration of food applications are vital areas to investigate.


Assuntos
Lamiaceae , Fitoterapia , Etnofarmacologia , Medicina Tradicional , Índia , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/toxicidade
6.
Ther Deliv ; 13(2): 81-93, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-35075915

RESUMO

Background: Chebulinic acid (CA), a component in Terminalia chebula, exhibits antiulcer activity, but has poor aqueous solubility. Raft-forming systems incorporating solid dispersions (SDs) of CA, were developed to overcome its poor biopharmaceutical properties and to prolong the gastric residence time for maximum activity. Methods: SDs were formulated by a solvent evaporation method using Eudragit EPO. Raft formulations consisted of sodium alginate as a polymer. Results: Release of CA in the dissolution medium was 40%, whereas SDs showed 95.45% release. The CA raft system (20 mg/kg) showed curative efficacy in an alcohol-induced gastric ulcer model and increased protection when compared with omeprazole (10 mg/kg) and CA suspension (20 mg/kg). Conclusion: These studies demonstrated SD raft systems to be a promising approach for antiulcer therapy by CA.


Assuntos
Úlcera Gástrica , Terminalia , Taninos Hidrolisáveis/farmacologia , Taninos Hidrolisáveis/uso terapêutico , Solubilidade , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico
7.
J Ethnopharmacol ; 266: 113434, 2021 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-33017636

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Hippophae rhamnoides L. (family- Elaeagnaceae, common name- Sea buckthorn) is a flowering shrub native to cold temperate regions of Eurasia. Berries, seeds, and leaves of the plant are widely used as a folk medicine for the treatment of hypertension, oedema, inflammation, tissue-regeneration, skin-grafts, burns/injury, wounds, and ulcers. AIM OF THE REVIEW: This article reviews geographical distribution, botanical description, phytochemistry, ethnomedicinal uses, and dermatological activities including, cosmeceuticals of H. rhamnoides available in the market. MATERIALS AND METHODS: The data has been compiled employing the various search engines like Science Direct, Pub Med, Google, Google Scholar, EBSCO, SCOPUS, and SciVal. RESULTS AND DISCUSSION: H. rhamnoides is primarily found in cold-temperate regions of Eurasia and was first located in China. Berries are the most prominent feature of the plant. Phytochemical studies reveal the presence of a wide variety of compounds like flavonoids, carotenoids, polyunsaturated fatty acids, minerals, vitamins, Omega 3, 6, 9 and rarest Omega 7 and about 190 bioactive compounds. The pharmacological studies demonstrated, sea buckthorn to exhibit antibacterial, anti-sebum, antifungal, anti-psoriasis, anti-atopic dermatitis and wound healing activities. Besides, it has also been included in various cosmeceuticals for its use in skin-eventone, smoothening, rejuvenation, removal of wrinkles, scars, and pigmentation, and also in hair related problems. CONCLUSION: Pharmacological evaluation confirmed the ethnomedically claimed biological actions and other beneficial effects on the skin of H. rhamnoides using scientifically accepted protocols and controls, although some of the studies require more elaborative studies. Its full application in the dermatology may be attributed to the presence of a variety of flavonoids, vitamins, and unsaturated fatty acids. Great use of plant in the traditional system for dermatological aspect, demands further comprehensive phytochemical work based on its actual use by the traditional population. Demonstration of the plant in the traditional system, pharmacology, cosmeceuticals not only demands its further therapeutic studies but also warrants focus towards its cultivation and propagation across the globe.


Assuntos
Fármacos Dermatológicos/farmacologia , Hippophae/química , Preparações de Plantas/farmacologia , Animais , Fármacos Dermatológicos/isolamento & purificação , Humanos , Medicina Tradicional , Compostos Fitoquímicos , Preparações de Plantas/química , Dermatopatias/tratamento farmacológico , Dermatopatias/patologia
8.
Planta Med ; 86(4): 267-275, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31968380

RESUMO

Infections caused by HSV-2 are a public health concern worldwide, and there is still a great demand for the discovery of novel anti-herpes virus agents effective against strains resistant to current antiviral agents. In this context, medicinal plants represent an alternative source of active compounds for developing efficient antiviral therapies. The aim of this study was to evaluate the antiviral activity of Arisaema tortuosum, a plant used in the traditional medicine of India. A chloroform soluble fraction of the leaves exhibited anti-HSV-2 activity with a selectivity index of 758. The extract was also active against acyclovir-resistant HSV-2 and HSV-1. The mechanism of action of the extract was investigated evidencing inhibition of both early and late events of the HSV-2 replicative cycle. A HPLC-PDA-MS/MS analysis showed the presence of flavonoids including apigenin and luteolin in the chloroform extract (CE). Apigenin and luteolin showed a high inhibitory activity with EC50 values of 0.05 and 0.41 µg/mL, respectively. Both compounds exhibited antiviral activity when added up to 6 h post infection and were able to reduce the viral progeny production. In addition, apigenin interfered with cell-to-cell virus spread.


Assuntos
Antivirais , Arisaema , Herpes Simples , Herpesvirus Humano 2 , Índia , Extratos Vegetais , Espectrometria de Massas em Tandem , Células Vero
9.
Carbohydr Polym ; 230: 115659, 2020 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-31887940

RESUMO

While the wound healing activity of thymoquinone (TQ) is well known, its clinical effectiveness remains limited due to the inherently low aqueous solubility, resulting in suboptimal TQ exposure in the wound sites. To address these problems, TQ loaded chitosan-lecithin micelles for wound healing were prepared and its efficacy was determined in vivo in the excision wound model. Firstly, the co-block polymer of chitosan and soya lecithin was synthesized which has low critical micelle concentration (CMC). Its employment in the development of TQ loaded polymeric micelles by Self-assembly method resulted in the stable polymeric micelle composition having requisite small particle size (<100 nm), narrow size distribution (close to zero) and high entrapment efficiency (98.77 %) of TQ. The designed nano-carriers not only substantially entrapped the drug but also controlled the release rate of TQ. The TQ-polymeric micelle hydrogel exhibited superior wound healing efficacy to the native TQ and Silver Sulphadiazine.


Assuntos
Benzoquinonas/administração & dosagem , Quitosana/farmacologia , Portadores de Fármacos/uso terapêutico , Descoberta de Drogas , Lecitinas/farmacologia , Nanofibras/uso terapêutico , Animais , Quitosana/química , Liberação Controlada de Fármacos , Lecitinas/química , Camundongos Endogâmicos BALB C , Micelas , Tamanho da Partícula , Cicatrização/efeitos dos fármacos
10.
Nat Prod Res ; 34(5): 638-645, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30169967

RESUMO

A new ether derivative of phenylpropanoid compound, γ-(γ'-isohydroxychavicol)-chavicol octanyl ether (K1) along with one known phenylpropanoid named allyl-pyrocatechol or hydroxychavicol (2) were isolated from Piper betle var. kali collected from Tumluk district, West Bengal India. We first report the presence of compound K1 in the genus Piper. Their structures were established on the basis of various spectroscopic analyses. Compounds K1 and 2 showed excellent antioxidant DPPH free radical scavenging activity with IC50 values of 4.61 and 4.12 µg/mL compared to ascorbic acid as a standard antioxidant drug with IC50 value of 3.42 µg/mL, respectively. Evaluation of in vitro cytotoxic activities of compounds K1 and 2 showed significant effects against human oral cancer cell lines (AW13516 and AW8507), human hepatoma cell lines (HEPG2 and PLC-PRF-5) and a human pancreatic cell line (MIA-PA-CA-2), compared to Doxorubicin® as a standard cytotoxic drug with GI50 values of <10 and 18.18 µg/mL.


Assuntos
Antineoplásicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Eugenol/análogos & derivados , Piper betle/química , Compostos Alílicos , Antineoplásicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Carcinoma Hepatocelular/tratamento farmacológico , Linhagem Celular Tumoral , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Fenóis , Extratos Vegetais/química , Folhas de Planta/química
11.
Int J Nanomedicine ; 14: 2301-2325, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31114188

RESUMO

Antimicrobial agents have been widely investigated for protecting against microbial infections in modern health. Drug-related limitations, poor bioavailability, toxicity to mammalian cells, and frequent bacteria drug resistance are major challenges faced when exploited in nanomedicine forms. Specific attention has been paid to control nanomaterial-based infection against numerous challenging pathogens in addition to improved drug delivery, targeting, and pharmacokinetic (PK) profiles, and thus, efficient antimicrobials have been fabricated using diverse components (metals, metal oxides, synthetic and semisynthetic polymers, natural or biodegradable polymers, etc). The present review covers several nanocarriers delivered through various routes of administration, highlighting major findings to control microbial infection as compared to using the free drug. Results over the past decade support the consistent development of various nanomedicines capable of improving biological significance and therapeutic benefits against an array of microbial strains. Depending on the intended application of nanomedicine, infection control will be challenged by various factors such as weighing the risk-benefits in healthcare settings, nanomaterial-induced (eco)toxicological hazards, frequent development of antibiotic resistance, scarcity of in vivo toxicity data, and a poor understanding of microbial interactions with nanomedicine at the molecular level. This review summarizes well-established informative data for nanomaterials used for infection control and safety concerns of nanomedicines to healthcare sectors followed by the significance of a unique "safe-by-design" approach.


Assuntos
Controle de Infecções , Nanomedicina/métodos , Animais , Anti-Infecciosos/farmacologia , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Humanos , Nanoestruturas/química , Nanoestruturas/ultraestrutura
12.
Comput Biol Chem ; 78: 217-226, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30579134

RESUMO

An attempt toward screening of phytoconstituents (Arisaema genus) against herpes viruses (HSV-1 and HSV-2) was carried out using in silico approaches. Human HSV-1 and HSV-2 are accountable for cold sores genital herpes, respectively. Two drug targets, namely thymidine kinase (TK; PDB: 2ki5) serine protease (PDB: 1at3) were selected for HSV-1 and HSV-2. Initially, molecular docking tool was employed to screened apex hits phytoconstituents against herpes infections. ADME-T studies of top ranked were also further highlighted to achieve their effectiveness. Following, molecular dynamics studies were also examined to further optimize the stability of ligands. Glide scores and binding interactions of phytoconstituents were compared with Acyclovir, the main drug used in treatment of HSV, the screened top hits exhibited more glide scores and better binding for both HSV-1 and HSV-2 receptors. Additionally, ADME-T showed an ideal range for top hits while molecular dynamics results also illustrated stability of models. Ultimately, the whole efforts reveal to top three most promising hits for HSV-1 (39, 21, 19) and HSV-2 (20, 51, 19) receptors which can be explored further in wet lab experiments as promising agents against HSV infections.


Assuntos
Antivirais/farmacologia , Arisaema/química , Herpesvirus Humano 1/metabolismo , Herpesvirus Humano 2/metabolismo , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Antivirais/química , Antivirais/metabolismo , Arisaema/genética , Domínio Catalítico/efeitos dos fármacos , Humanos
13.
Curr Pharm Des ; 24(30): 3576-3586, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30345913

RESUMO

The present study focused to optimize dual coated multiparticulates using Box-Behnken Experimental Design and in-silico simulation using GastroPlusTM software. The optimized formulations (OB1 and OB2) were comparatively evaluated for particle size, morphological, in vitro drug release, and in vivo permeation studies. In silico simulation study predicted the in vivo performance of the optimized formulation based on in-vitro data. Results suggested that optimized formulation was obtained using maximum content of Eudragit FS30D and minimum drying time (2 min). In vitro data corroborated that curcumin release was completely protected from premature drug release in the proximal part of gastro intestinal tract and successfully released to the colon (95%) which was closely predicted (90.1 %) by GastroPlusTM simulation technique. Finally, confocal laser scanning microscopy confirmed the in-vitro findings wherein maximum intensity was observed with OB1 treated group suggesting successful delivery of OB1 to the colon for enhanced absorption as predicted in regional absorption profile in ascending colon (30.9%) and caecum (23.2%). Limited drug absorption was predicted in small intestine (1.5-8.7%). The successful outcomes of the research work minimized the release of curcumin in the upper gastric tract and the maximized drug access to the colon (pH 7.4) as prime concern.


Assuntos
Colo/metabolismo , Simulação por Computador , Curcumina/administração & dosagem , Curcumina/farmacocinética , Desenho de Fármacos , Intestino Delgado/metabolismo , Animais , Liberação Controlada de Fármacos , Feminino , Masculino , Tamanho da Partícula , Ratos , Ratos Wistar , Software , Propriedades de Superfície
14.
BMC Complement Altern Med ; 18(1): 233, 2018 Aug 07.
Artigo em Inglês | MEDLINE | ID: mdl-30086745

RESUMO

BACKGROUND: Bombax ceiba is used traditionally to treat bone disorders, rheumatism, and joint pain. The aim of the study is to carry out osteogenic activity in-vitro and anti-osteoporotic activity in-vivo of stem bark of B. ceiba in surgical ovariectomy model in female rats. METHODS: Plant drug: B. ceiba stem bark was extracted with solvents petroleum ether and methanol using Soxhlet extraction. In-vitro osteoblastic proliferation study was performed using UMR-106 cell lines. Both the extracts were undergone to acute toxicity study as per OECD423 guidelines. Female Wistar albino rats 180-240 g were used (n = 6). Surgical ovariectomy was performed under anesthesia to induce bone porosity and loss in all animals except normal control and sham control. Each extract was administered at two dose level: 100 and 200 mg/kg and the standard Raloxifene was given at 1 mg/kg orally for 28 days. The phytochemical study of both the extracts was performed using HPLC and HPTLC. RESULTS: A significant osteoblast cell proliferation and alkaline phosphatase activity were observed with B. ceiba extracts in UMR-106 cell lines. Surgical removal of ovaries produced significant (p < 0.05) decline in bone mineral density, bone breaking strength, serum ALP, calcium, phosphorus, and estradiol level and marked bone tissue destruction in histology. Administration of petroleum ether and methanolic extract for 28 days significantly (p < 0.05) ameliorated the consequences of ovariectomy induced bone porosity and restored the normal architecture of bone, as compared to OVX control. The phytochemical screening of both the extracts were also carried out. The quantification of phytoconstituents showed the presence of ß-sitosterol and lupeol in petroleum ether extract, whereas the lupeol is also quantified in the methanolic extract. The presence of gallic acid was quantified in methanolic extract using HPLC. CONCLUSION: B. ceiba: stem bark ameliorated the state of bone fragility and fracture possibly due to estrogenic modulation, as also confirmed by in-vitro osteogenic activity which may be due to the presence of lupeol, gallic acid and ß-sitosterol constituents of the plant.


Assuntos
Bombax/química , Proliferação de Células/efeitos dos fármacos , Ácido Gálico/farmacologia , Osteoblastos/efeitos dos fármacos , Osteoporose/metabolismo , Triterpenos Pentacíclicos/farmacologia , Sitosteroides/farmacologia , Animais , Peso Corporal/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Fina , Feminino , Ácido Gálico/análise , Ovariectomia , Triterpenos Pentacíclicos/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Sitosteroides/análise
15.
Pharmacogn Mag ; 13(Suppl 4): S780-S785, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29491633

RESUMO

BACKGROUND: To date, efforts for the prevention and treatment of human respiratory syncytial virus (RSV) infection have been still vain, and there is no safe and effective clinical accepted vaccine. Arisaema genus has claimed for various traditional bioactivities, but scientific assessments are quite limited. OBJECTIVE: This encouraged us to carry out our present study on around 60 phytoconstituents of different Arisaema species as a natural inhibitor against the human RSV. MATERIALS AND METHODS: Selected 60 phytochemical entities were evaluated on the docking behavior of human RSV receptor (PDB: 4UCC) using Maestro 9.3 (Schrödinger, LLC, Cambridge, USA). Furthermore, kinetic properties and toxicity nature of top graded ligands were analyzed through QikProp and ProTox tools. RESULTS: Notably, rutin (glide score: -8.49), schaftoside (glide score: -8.18) and apigenin-6,8-di-C-ß-D-galactoside (glide score - 7.29) have resulted in hopeful natural lead hits with an ideal range of kinetic descriptors values. ProTox tool (oral rodent toxicity) has resulted in likely toxicity targets of apex-graded tested ligands. CONCLUSION: Finally, the whole efforts can be explored further as a model to confirm its anti-human RSV potential with wet laboratory experiments. SUMMARY: Rutin, schaftoside, and apigenin-6,8-di-C-ß-D-galactoside showed promising top hits docking profile against human respiratory syncytial virusMoreover, absorption, distribution, metabolism, excretion properties (QikProp) of top hits resulted within an ideal range of kinetic descriptorsProTox tool highlighted toxicity class ranges, LD50 values, and possible toxicity targets of apex-graded tested ligands. Abbreviations used: RSV: Respiratory syncytial virus, PRRSV: Porcine respiratory and reproductive syndrome virus, ADME-T: Absorption, distribution, metabolism, excretion, and toxicity.

16.
Pharmacogn Mag ; 13(Suppl 4): S786-S790, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29491634

RESUMO

BACKGROUND: Globally, reactive oxygen species have served as an alarm predecessor toward pathogenesis of copious oxidative stress-related diseases. The researchers have turned their attention toward plant-derived herbal goods due to their promising therapeutic applications with minimal side effects. Arisaema tortuosum (Wall.) Schott (ATWS) is used in the traditional medicine since ancient years, but scientific assessments are relatively inadequate and need to be unlocked. OBJECTIVE: Our aim was designed to validate the ATWS tuber and leaf extracts as an inhibitor of oxidative stress using computational approach. MATERIALS AND METHODS: The reported chief chemical entities of ATWS were docked using Maestro 9.3 (Schrödinger, LLC, Cambridge, USA) tool and further ATWS extracts (tubers and leaves) were validated with 2,2'-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), ferric-reducing ability of plasma (FRAP), and sulforhodamine B assays experimentally. RESULTS: In silico results showed notable binding affinity of ATWS phytoconstituents with the receptor (PDB: 3ERT). Experimentally, butanolic tuber fraction confirmed promising antioxidant potential (ABTS: IC50: 271.67 µg/ml; DPPH: IC50: 723.41 µg/ml) with a noteworthy amount of FRAP (195.96 µg/mg), total phenolic content (0.087 µg/mg), and total flavonoid content (7.5 µg/mg) while chloroform fraction (leaves) showed considerable reduction in the cell viability of MCF-7 cell line. CONCLUSION: The current findings may act as a precious tool to further unlock novel potential therapeutic agents against oxidative stress. SUMMARY: Quercetin showed top.ranked glide score with notable binding toward 3ERT receptorAmong extracts, butanolic tubers confirmed as promising antioxidant with remarkable amount of TPC and TFCIn addition, chloroform fraction (leaves) revealed considerable decline in the cell viability of MCF-7 cell line. Abbreviations used: ATWS: Arisaema tortuosum (Wall.) Schott, DPPH: 2,2'-diphenyl-1-picrylhydrazyl, ABTS: 2,2'-Azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt, FRAP: Ferric-reducing ability of plasma, TPC: Total phenolic content, TFC: Total flavonoid content, SRB: Sulforhodamine B.

17.
Nat Prod Res ; 31(22): 2604-2611, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28278665

RESUMO

Phytochemical analyses of the chloroform extract of Piper betle L. var. birkoli, Piperaceae, leaves led to the isolation of two new phenylpropanoid analogues: bis-chavicol dodecanoyl ester (2) and bis-hydroxychavicol dodecanoyl ester (3), along with one known compound: allyl-3-methoxy-4-hydroxybenzene (1) on the basis of spectroscopic data 1D (1H and 13C) and 2D (1H-1H COSY and HMBC) NMR, as well as ESI-MS, FT-IR, HR-ESI-MS and LC-ESI-MS. Compound 2 and 3 exhibited excellent antioxidant DPPH radical scavenging activity with IC50 values of 12.67 µg/mL and 1.08 µg/mL compared to ascorbic acid as a standard antioxidant drug with IC50 value of 6.60 µg/mL. Evaluation of cytotoxic activity against two human oral cancer cell lines (AW13516 and AW8507) showed significant effect with GI50 values of 19.61 and 23.01 µg/mL for compound 2 and 10.25 and 13.12 µg/mL for compound 3, compared to Doxorubicin® as a standard cytotoxic drug with GI50 value of < 10 µg/mL.


Assuntos
Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Piper betle/química , Compostos Alílicos/química , Compostos Alílicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Cromatografia Líquida , Dodecanol/química , Dodecanol/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Neoplasias Bucais/tratamento farmacológico , Fenóis/química , Fenóis/farmacologia , Folhas de Planta/química , Espectrometria de Massas por Ionização por Electrospray , Espectroscopia de Infravermelho com Transformada de Fourier
18.
Pharmacogn Rev ; 9(17): 45-54, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26009693

RESUMO

Sugarcane (Saccharum officinarum Linn.) is an important perennial grass of Poaceae family, indigenous to tropical South Asia and Southeast Asia. It is cultivated worldwide due to the economical and medicinal value of its high yielding products. Sugarcane juice is well known as a raw material for the production of refined sugar and its wax is considered as a potential substitute for the expensive carnauba wax, which is of cosmetic and pharmaceutical interest. Refined sugar is the primary product of sugarcane juice, but during its processing, various other valuable products are also obtained in an unrefined form, such as, brown sugar, molasses, and jaggery. Sugarcane juice is widely used in India in the treatment of jaundice, hemorrhage, dysuria, anuria, and other urinary diseases. Herein, we have summarized the different phytoconstituents and health benefits of sugarcane and its valuable products. The phytochemistry of sugarcane wax (obtained from the leaves and stalks of sugarcane), leaves, juice, and its products has revealed the presence of various fatty acid, alcohol, phytosterols, higher terpenoids, flavonoids, -O- and -C-glycosides, and phenolic acids. The future prospective of some of the sugarcane products has been discussed, which needs a phytopharmacological study and has a great potential to be a valuable medicinal product.

19.
Nat Prod Commun ; 5(4): 575-9, 2010 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-20433076

RESUMO

Abhayarishta is an Ayurvedic formulation prepared traditionally by the fermentation of the decoction of Terminalia chebula (pericarp), Vitis vinifera (fruits), Embelia ribes (fruits) and Madhuca indica (flowers). In the present communication, chemical changes occurring during fermentation in Abhayarishta have been studied for the purpose of its standardization. An HPLC-DAD method for quantitative estimation of selected marker constituents in the formulation has been developed and validated. A comparison of decoction and final processed formulation revealed that major polyphenolics (chebulagic and chebulinic acid) of T. chebula were hydrolyzed to their respective monomers and, consequently, there was an increase in the amount of chebulic acid, gallic acid, ellagic acid and ethyl gallate after fermentation. 5-Hydroxymethyl furfural (5-HMF) was also found in the formulation. Thus, emphasis is laid upon consideration of processing methods of formulation which has been lacking in the standardization of most of Ayurvedic formulations.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Taninos Hidrolisáveis/metabolismo , Extratos Vegetais/análise , Benzopiranos/análise , Ácido Elágico/análise , Fermentação , Furaldeído/análogos & derivados , Furaldeído/análise , Ácido Gálico/análogos & derivados , Ácido Gálico/análise , Glucosídeos/análise , Ayurveda , Reprodutibilidade dos Testes
20.
Nat Prod Commun ; 5(11): 1767-70, 2010 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-21213976

RESUMO

Jirakadyarishta, an Ayurvedic formulation prepared by the fermentation of a decoction of Cuminum cyminum (seeds) is traditionally used for intestinal disorders. RP-HPLC analysis of the decoction and the final processed formulation revealed that apigenin-7-O-[galacturonide (1 --> 4)-O-glucoside] and luteolin-4'-O-glucoside-7-O-galacturonide) were the two major constituents of the decoction of C. cyminum. Selective hydrolysis of 7-O-glucosides of luteolin and apigenin during fermentation resulted in an increase in the amount of luteolin and apigenin. The 4'-O-glucoside-7-O-galacturonide of luteolin and galacturonide derivative of apigenin were not hydrolyzed during fermentation. Monomeric phenolics, together with 5-hydroxymethyl furfural (5-HMF), were also introduced into the formulation through the jaggery and other plant materials during fermentation. This communication highlights the importance of the ancient processing methods used in Ayurveda.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Cuminum/metabolismo , Ayurveda , Antioxidantes/química , Cuminum/química , Fermentação
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