Content uploaded by Dr. Devang J. Pandya
Author content
All content in this area was uploaded by Dr. Devang J. Pandya on Feb 25, 2021
Content may be subject to copyright.
A preview of the PDF is not available
BIOACTIVITY-GUIDED ISOLATION, CHARACTERIZATION & ESTIMATION OF PHYTOCONSTITUENTS FROM LEAVES AND ROOTS OF LAUNAEA PINNATIFIDA CASS., A SPECIES OF THE CONTROVERSIAL DRUG GOJIHVA
Figures
Figures - uploaded by Dr. Devang J. Pandya
Author content
All figure content in this area was uploaded by Dr. Devang J. Pandya
Content may be subject to copyright.
ResearchGate has not been able to resolve any citations for this publication.
Oxidative stress (OS) appears to be an important determinant during the different stages of progression of Alzheimer’s Disease (AD). In particular, impaired antioxidant defense mechanisms, such as the decrease of glutathione (GSH) and nuclear factor erythroid 2 (NF-E2)-related factor 2 (Nrf2), a master regulator of antioxidant genes, including those for GSH, are associated with OS in the human AD brain. Among the neuropathological hallmarks of AD, the soluble oligomers of amyloid beta (A) peptides seem to promote neuronal death through mitochondrial dysfunction and OS. In this regard, bifunctional antioxidants can exert a dual neuroprotective role by scavenging reactive oxygen species (ROS) directly and concomitant induction of antioxidant genes. In this study, among natural coumarins (esculetin, scopoletin, fraxetin and daphnetin), we demonstrated the ability of esculetin (ESC) to prevent and counteract ROS formation in neuronal SH-SY5Y cells, suggesting its profile as a bifunctional antioxidant. In particular, ESC increased the resistance of the SH-SY5Y cells against OS through the activation of Nrf2 and increase of GSH. In similar experimental conditions, ESC could also protect the SH-SY5Y cells from the OS and neuronal death evoked by oligomers of A1–42 peptides. Further, the use of the inhibitors PD98059 and LY294002 also showed that Erk1/2 and Akt signaling pathways were involved in the neuroprotection mediated by ESC. These results encourage further research in AD models to explore the efficacy and safety profile of ESC as a novel neuroprotective agent.
Meda Dhatu (Adipose tissue) was considered as inert tissue that stores fat only but now it is an endocrine gland which controls coagulation, appetite regulation, immunity, glucose and lipid metabolism, reproduction, angiogenesis, fibrinolysis, body weight homeostasis and vascular tone control. Meda is the fourth dhatu (stable constituent of body) as per Ayurveda doctrine and resemble with the adipose tissue. Meda can create not only Sthyaulya (Obesity) in general but also organ specific disorders like- Medaja granthi , Medaja Masurika, Medaja galaganda, Medaja vridhi etc. Yakrimeda is also found in Sanskrit literature. But Medaja Yakritdalludara or Yakrit Vikar is not enumerated in classical Ayurveda literature. Strong evidences suggested that accumulation of lipids in non-adipose tissues can contribute to cellular dysfunction and cell death, a phenomenon that is called lipotoxicity. Various components of Meda and its function found in Ayurveda literature are discussed. Multiple factors hit hypothesis for samprapti (pathogenesis) of Medaja Yakrut vikara( Fatty liver disorders) and its progression with preventive and curative strategies are described with scientific evidences.
Glycolysis can improve the tolerance of tissue cells to hypoxia, and its intermediates provide raw materials for the synthesis and metabolism of the tumor cells. If it can inhibit the activity of glycolysis-related enzymes and control the energy metabolism of tumor, it can be targeted for the treatment of malignant tumor. The target proteins phosphoglycerate kinase 2 (PGK2), glycerol-3-phosphate dehydrogenase (GPD2), and glucose-6-phosphate isomerase (GPI) were screened by combining transcriptome, proteomics, and reverse docking. We detected the binding constant of the active compound using microscale thermophoresis (MST). It was found that esculetin bound well with three potential target proteins. Esculetin significantly inhibited the rate of glycolysis, manifested by differences of cellular lactate production and glucose consumption in HepG2 cells with or without esculetin. It was found that GPD2 bound strongly to GPI, revealing the direct interaction between the two glycolysis-related proteins. Animal tests have further demonstrated that esculetin may have anticancer effects by affecting the activity of PGK2, GPD2, and GPI. The results of this study demonstrated that esculetin can affect the glucose metabolism by binding to glycolytic proteins, thus playing an anti-tumor role, and these proteins which have direct interactions are potential novel targets for tumor treatment by esculetin.
Background:
Esculetin, the main active ingredient in the Chinese herbal medicineCortex Fraxini, has been shown to possess antitumor activity. However, the effect of esculetin on clear cell renal cell carcinoma (ccRCC) has not been investigated.
Methods:
MTS assays and colony formation assays were used to study the cytotoxicity of esculetin. The effects of esculetin on cell cycle and apoptosis were analyzed by flow cytometry. Western blot was used to detect cell cycle-, apoptosis-, and EMT-related proteins. Wound-healing assays and transwell assays were performed to study the effect of esculetin on cell migration and invasion in the ccRCC cell lines 786-O and SN12-PM6.
Results:
Esculetin exerted cytotoxic activities in 786-O and SN12-PM6 cells in a dose- and time-dependent manner. The compound arrested the cell cycle in G0/G1 and G2/M phase with down-regulation of Cyclin D1, CDK4, CDK6, and c-Myc expression. Esculetin also induced apoptosis and the expression of cleaved caspase 3 increased. Additionally, esculetin significantly inhibited 786-O and SN12-PM6 cell migration and invasion, the expression of E-Cadherin increased, and the expression of N-cadherin and vimentin decreased.
Conclusion:
Taken together, these results suggest that esculetin inhibits proliferation, migration, and invasion of ccRCC and is a potential novel therapeutic agent for the treatment of ccRCC.
Symphytum officinale (comfrey), Tussilago farfara (coltsfoot) and Borago officinalis (borage) have long histories of therapeutic use, but their safety has been questioned due to the presence of unsaturated pyrrolizidine alkaloids (PAs). The evidence base underlying these concerns relies in part on case reports. This systematic review assesses these case reports for their reliability to inform this debate.
Method:
Study selection was restricted to case reports describing possible pyrrolizidine alkaloid related harm and ingestion of comfrey, coltsfoot or borage. An extensive search of academic databases was conducted. Papers meeting the criteria were critically appraised.
Results:
The search resulted in 11 appropriate case reports, none of which involved borage. Nine reports were assessed for causality and indicated some degree of association between the material ingested and the adverse event. Lack of unequivocal identification of the species ingested compromised attribution and was a significant source of uncertainty. Three levels of identity confusions were found; misidentification or substitution at the level of the whole herb; omission of appropriate botanical identification and attribution of a specific PA to either comfrey or coltsfoot when it is a constituent found in other plants of established toxicity.
Conclusion:
These cases are an unreliable body of evidence on which to draw conclusions about oral consumption of Symphytum officinale and Tussilago farfara. With insufficient evidence to differentiate the relative risk of one PA-containing plant from another; toxicological studies based on oral ingestion of phytochemically complex preparations of these herbs may be the most accurate methodology for assessing clinical risk.
India's medical heritage across its two streams of experiential knowledge viz. the classical (codified) and folk (oral) reveals an incredible range and depth of knowledge of medicinal plants. In the classical stream of Ayurveda, across the period from 1500 BCE to 1900 CE, there is information of more than 12,000 distinct Sanskrit plant names with overlaps across texts. This information is captured in more than 200 texts viz. 6 samhitas, 57 nighantus and 140 vyakhyas. The information about plants has three major dimensions in codified literature viz. morphological description (rupa gnana), pharmacology (dravya guna shastra) and pharmacy (bhaishajya kalpana). The morphological information is however sketchy and wholly inadequate for establishing botanical identity. Thus despite the huge corpus of plant names backed by sophisticated understanding of pharmacology and pharmacy there is the fact of controversial identities of medicinal plants. Why is this the case? The author believes that the gap in morphological detailing is due to the 'experiential' pedagogy of India's health tradition. While knowledge transmission of plants included theoretical propositions and sophisticated logic related to pharmacology, it also assumed an oral, practical and experiential system of learning about the identity of plants through field work. The purpose of this research is to understand the range and depth at which we have understood the problem of controversial identities of medicinal plants, to analyze work done in the field and to propose a Trans disciplinary approach to solve the problem of controversial identities of medicinal plants in Ayurveda.
Background:
Conventional cancer therapeutics have enormous toxicity and severe side effects that generate multi-drug resistance. Therefore, an urgent need exists for new alternative therapeutic agents for cancer treatment. Cepharanthin(CEP) has anticancer potential but has poor aqueous solubility, which limits its clinical use. Nano suspensions (NS) are attractive as insoluble drug delivery systems.
Objectives:
In this study, we used D-alpha tocopherol acid polyethylene glycol succinate (TPGS), polyvinylpyrrolidone (PVP) VA64, and croscamellose sodium (CCS) as stabilizers to produce TPGS-CEP-NS, PVP VA64-CEP-NS, and CCS-CEP-NS by wet-milling technology, and then characterized the NS and evaluated their functional activities in vitro.
Methods:
CEP nano suspensions (CEP-NS) were prepared by a wet-milling method. The prepared NS were characterized by particle size distribution, zeta potential, morphology, surface properties, and molecular interactions. The NS were evaluated for their effects on Hep G2 cells in vitro. The evaluations included assessment of cellular cytotoxicity, cellular apoptosis, NS uptake by cells, and mitochondrial membrane potential changes.
Results:
CEP-NS showed appropriate particle size and were physically stable. All CEP-NS exhibited Hep G2 enhanced anti-proliferative effects by reducing cell viability, enhanced cellular uptake, induced cellular apoptosis, and mitochondrial membrane potential loss.
Conclusion:
CEP-NS may be effective therapeutic agents for treatment of hepatocellular carcinoma.
Medicinal plant has been applied as an alternative strategy for antibiotics and chemotherapeutics for controlling the outbreak of diseases in tilapia farming. In this study, five doses of Elephantopus scaber extract (ESE) were added to the basal diet at 0, 2.5, 5, 10, and 20 g kg-1 feed of Nile tilapia fingerlings (13.92 ± 0.06 g initial weight) in triplicate. After 4- and 8- weeks post-feeding, fish were sampled to determine the effects of the ESE supplemented on fish’s growth performance, humoral, and skin mucus immune response. After 8 weeks post-feeding, a challenge test against Streptococcus agalactiae was carried out using 10 fish from each tank. Fish fed ESE showed significantly increased serum lysozyme (SL), serum peroxidase (SP), alternative complement (ACH50), phagocytosis (PI), and respiratory burst (RB) compared to the control group (P<0.05). The skin mucus lysozyme (SMLA) and skin peroxidase (SMPA) were stimulated in fish fed ESE diets. Dietary inclusion of ESE significantly (P<0.05) promoted final body weight (FW), weight gain (WG), and specific growth rate (SGR); while a reduction in feed conversion ratio (FCR) was observed in fish fed 5 g kg-1 ESE, after 8 weeks post-feeding. The challenge study indicated that the relative percent survival (RSP) was 38.10%, 76.19%, 66.67%, and 47.62% in Diet 2, Diet 3, Diet 4, and Diet 5, respectively. Among the supplemented groups, dietary of 5 g kg-1 ESE showed significantly higher RPS and the highest resistance to S. agalactiae in comparison with other groups. In conclusion, supplementation of ESE (5 g kg-1) enhanced the humoral and mucosal immunity, promoted growth performance, and improved disease resistance of Nile tilapia against Streptococcus agalactiae.