Rutin Isolated from Chrozophora tinctoria

Osteoporosis is a chronic disease in which the skeleton loses a weighty proportion of its mineralized mass and mechanical pliability. Currently available antiosteoporotic agents suffer adverse effects that include elevated risk of thrombosis and cancer. Phytochemicals may constitute a safer and effective option. In the current work, six flavonoids were obtained from Chrozophora tinctoria and identified as amentoflavone (1), apigenin-7-O-β-D-glucopyranoside (2), apigenin-7-O-6′′-E-p-coumaroyl-β-d-glucopyranoside (3), acacetin-7-O-β-d-[α-l-rhamnosyl(1→6)]3′′-E-p-coumaroyl glucopyranoside (4), apigenin-7-O-(6′′-Z-p-coumaroyl)-β-d-glucopyranoside (5), and rutin (6). An extensive review of the literature as well as NMR and mass spectral techniques was employed in order to elucidate the compound structures. Proliferation was enhanced in MCF7, MG-63, and SAOS-2 cells after exposure to subcytotoxic levels of the tested flavonoids. Rutin was chosen for subsequent studies in SAOS-2 cells. Rutin was not found to cause any alteration in the index of proliferation of these cells, when examining the cell cycle distribution by DNA flowcytometric analysis. Rutin was, however, found to increase osteocyte and osteoblast-related gene expression and lower the expression of RUNX suppressor and osteoclast genes. When examining the influence of rutin on vitamin D levels and the activity of alkaline phosphatase enzyme, it was found to enhance both, while decreasing acid phosphatase which is a marker of osteoporosis. Thus, rutin enhances proliferation and ossification markers in bone cells

Therapeutic potential of active components of saffron in post-surgical adhesion band formation

Background Abdominal adhesions are common and often develop after abdominal surgery. There are currently no useful targeted pharmacotherapies for adhesive disease. Saffron and its active constituents, Crocin and Crocetin, are wildly used in traditional medicine for alleviating the severity of inflammatory or malignant disease. Purpose The aim of this study was to investigate the therapeutic potential of the pharmacological active component of saffron in attenuating the formation of post-operative adhesion bands using different administration methods in a murine model. Material method saffron extract (100 mg/kg), Crocin (100 mg/kg), and Crocetin (100 mg/kg) were administered intraperitoneally and by gavage in various groups of male Wistar rat post-surgery. Also three groups were first treated intra-peritoneally by saffron extract, Crocin, and Crocetin (100 mg/kg) for 10 days and then had surgery. At the end of the experiments, animals sacrificed for biological assessment. Result A hydro-alcoholic extract of saffron and crocin but not crocetin potently reduced the adhesion band frequency in treatment and pre-treatment groups in the mice given intra-peritoneal (i.p) injections. Following the saffron or crocin administration, histological evaluation and quantitative analysis represented less inflammatory cell infiltration and less collagen composition, compared to control group. Moreover, the oxidative stress was significantly reduced in treatment groups. Conclusion These findings suggest that a hydro-alcoholic extract of saffron or its active compound, crocin, is a potentially novel therapeutic strategy for the prevention of adhesions formation and might be used as beneficial anti-inflammatory or anti-fibrosis agents in clinical trials. Taxonomy Abdominal surgeries/post-surgical adhesions

Role of natural phenolics in hepatoprotection: A mechanistic review and analysis of regulatory network of associated genes

The liver is not only involved in metabolism and detoxification, but also participate in innate immune function and thus exposed to frequent target Thus, they are the frequent target of physical injury. Interestingly, liver has the unique ability to regenerate and completely recoup from most acute, non-iterative situation. However, multiple conditions, including viral hepatitis, non-alcoholic fatty liver disease, long term alcohol abuse and chronic use of medications can cause persistent injury in which regenerative capacity eventually becomes dysfunctional resulting in hepatic scaring and cirrhosis. Despite the recent therapeutic advances and significant development of modern medicine, hepatic diseases remain a health problem worldwide. Thus, the search for the new therapeutic agents to treat liver disease is still in demand. Many synthetic drugs have been demonstrated to be strong radical scavengers, but they are also carcinogenic and cause liver damage. Present day various hepatic problems are encountered with number of synthetic and plant based drugs. Nexavar (sorafenib) is a chemotherapeutic medication used to treat advanced renal cell carcinoma associated with several side effects. There are a few effective varieties of herbal preparation like Liv-52, silymarin and Stronger neomin phages (SNMC) against hepatic complications. Plants are the huge repository of bioactive secondary metabolites viz; phenol, flavonoid, alkaloid etc. In this review we will try to present exclusive study on phenolics with its mode of action mitigating liver associated complications. And also its future prospects as new drug lead

Assessment of acute and subacute toxic effects of the Saudi folk herb Retama raetam in rats

Background: Retama raetam (RR) fruit is used in traditional Saudi folk medicine as a hypoglycemic herb. However, the potential toxicity of RR has not been fully investigated. The current study aimed to explore the potential acute and subacute toxicities of the methanolic extract of RR fruit in male and female rats. Methods: The extent of acute toxicity of RR was tested 14 days after a single oral dose was administered (250 mg/kg, 500 mg/kg, or 750 mg/kg). Additionally, subacute toxicity was tested 28 days after an oral dose of 250 mg/kg/d, 500 mg/kg/d, or 750 mg/kg/d was administered for 4 weeks. Results: Subsequent to variable dosage testing, oral LD50 of RR was found to be 1995 mg/kg in rats. Oral doses of 500 mg/kg and 750 mg/kg significantly decreased body weight gain. Subacute administration (750 mg/kg) was associated with significant manifestations of toxicity. Additionally, subacute administration of the extract at doses of 500 mg/kg or 750 mg/kg significantly elevated alanine transaminase and aspartate transaminase activities. Hepatotoxicity of RR was confirmed with histopathological findings. Subacute administration of RR (500 mg/kg) showed histopathological changes in the liver as indicated by degenerated hepatocytes and early fibrosis, while a dosage of 750 mg/kg showed congested central vein and vascular degeneration. Moreover, subacute administration of the extract at doses of 250 mg/kg, 500 mg/kg, or 750 mg/kg showed histopathological alterations in rat kidney that ranged from mild interstitial congestion to tubular degeneration. The extract showed positive result in the Ames test. Conclusion: Repeated administration of methanolic extract of RR (250 mg/kg) has a low nephrotoxic subacute toxicity potential, while it might have hepatotoxic, nephrotoxic, and mutagenic effects at higher doses

Antifibrotic effects of crocin on thioacetamide-induced liver fibrosis in mice

Liver fibrosis is a major health concern that results in significant morbidity and mortality. Up-to-date, there is no standard treatment for fibrosis because of its complex pathogenesis. Crocin is one of the main nutraceuticals isolated from the stigma of Crocus sativus with antioxidant and anti-inflammatory activities. The current study aimed at evaluating the potential antifibrotic activity of crocin against thioacetamide (TAA)-induced liver fibrosis in mice as well as the underlying mechanism using silymarin as a reference antifibrotic product. Crocin at two doses (25 and 100 mg/kg) significantly ameliorated the rise in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities, and total bilirubin (TB). Further, the high dose significantly protected against the increase in serum total cholesterol (TC) and triglycerides (TG). These effects were confirmed by light microscopic examinations. Crocin antioxidant activities were confirmed by the observed inhibition of reduced glutathione depletion (GSH), super oxide dismutase (SOD) exhaustion and malondialdehyde (MDA) accumulation in liver tissue. The antifibrotic effects of crocin were explored by assessing fibrosis related gene expression. Administration of crocin (100 mg/kg) hampered expression of tumor growth factor-β (TGF-β), α alpha smooth muscle actin (α-SMA) and collagen 1-α expression and significantly raised gene expression of matrix metalloproteinase-2 (MMP-2). Further, it reduced protein expression of nuclear factor-κB (NF-κB) and cyclooxygenase-2 (COX-2) as assessed immunohistochemically. These anti-inflammatory effects were confirmed by the observed protein expression of interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α). Thus, it can be concluded that crocin protects against TAA-induced liver fibrosis in mice. This can be ascribed, at least partly, to its antioxidant and anti-inflammatory effects. Keywords: Liver fibrosis, Thioacetamide, Crocin, Silymarin, Mic

Management of the noxious weed; Medicago polymorpha L. via allelopathy of some medicinal plants from Taif region, Saudi Arabia

Germination bioassay was carried out to test the biological activity of Achillea santolina L. (ASAE), Artemisia monosperma Del. (AMAE), Pituranthus tortuosus L. (PTAE) and Thymus capitatus L. (TCAE) aqueous extracts (collected from Taif region, KSA) on germination percentage (GP), plumule (PL) and radicle (RL) lengths (mm) besides seedling dry weight (SDW) (mg/seedlings) of Medicago polymorpha L. The inhibitory effect of P. tortuosus was insignificant compared to the other three donor species which attained the strongest allelopathic potential in the following order: A. santolina > A. monosperma > T. capitatus. Growth experiment using crude powder of the four donor species was conducted to examine their effects on leaf area index (LAI), photosynthetic pigments, total available carbohydrates (TAC) and total protein (TP). It is worth mentioning that each of the four donor species crude powders mixed with clay loam soil appeared to have a great inhibitory allelopathic effect on LAI, total photosynthetic pigment and chlorophyll a (Chl a) while carotenoids exhibited a slight increase with the application of the four donor species crude powders. TAC and TP were significantly decreased with increasing the crude powder concentrations while a slight decrease was recorded for carbon/nitrogen (C/N) ratio. There is possibility of using these allelochemicals directly or as structural leads for the discovery and development of environmentally friendly herbicides to control weeds. The study recommended that these species must be phytochemically examined in future for their allelochemicals in order to provide information on the possibilities of using one or more of these species as bioherbicides. Keywords: Achillea santolina, Artemisia monosperma, Pituranthus tortuosus, Thymus capitatus, Bioherbicide

<i>Alcyonium</i> Octocorals: Potential Source of Diverse Bioactive Terpenoids

Alcyonium corals are benthic animals, which live in different climatic areas, including temperate, Antarctic and sub-Antarctic waters. They were found to produce different chemical substances with molecular diversity and unique architectures. These metabolites embrace several terpenoidal classes with different functionalities. This wide array of structures supports the productivity of genus Alcyonium. Yet, majority of the reported compounds are still biologically unscreened and require substantial efforts to explore their importance. This review is an entryway to push forward the bio-investigation of this genus. It covers the era from the beginning of reporting metabolites from Alcyonium up to March 2019. Ninety-two metabolites are presented; forty-two sesquiterpenes, twenty-five diterpenes and twenty-five steroids have been reported from sixteen species

Multimechanistic antifibrotic effect of biochanin a in rats: implications of proinflammatory and profibrogenic mediators.

Biochanin A (BCA) is an isoflavone found in red clover and peanuts. Recently, it drew much attention as a promising anticancer and antioxidant. Due to its diversity in pharmacological actions, we were encouraged to investigate its potential as an antifibrotic, elucidating the different molecular mechanisms involved.Rats were pretreated with BCA, then injected with carbon tetrachloride (CCl4) for 6 weeks. Changes in liver weight and histology were examined and levels of aspartate and alanine aminotransferases, cholesterol, triglycerides, alkaline phosphatase and total bilirubin measured. To assess hepatic efficiency, indocyanine green was injected and its clearance calculated and albumin, total proteins and insulin-like growth factor-1 expression were measured. Cytochrome P4502E1 activity, cytochrome P4501A1 expression, in addition to sulfotransferase1A1 expression were determined to deduce the effect of BCA on hepatic metabolism. As oxidative stress markers, lipid peroxides levels, reduced glutathione, superoxide dismutase and catalase activities, as well as the total antioxidant capacity, were assessed. Nitric oxide, inducible nitric oxide synthase and cyclooxygenase-2 were used as indicators of the inflammatory response. Signaling pathways involving tumor necrosis factor-alpha, nuclear factor-kappa B, transforming growth factor-beta1, matrix metalloproteinase-9 and alpha-smooth muscle actin were investigated accordingly. Extent of fibrosis was examined by Masson's stain and measuring hydroxyproline levels.BCA pretreatment significantly protected against the chronic damage of CCl4. Liver injury, oxidative stress, inflammation and fibrosis markers decreased, while hepatic efficiency improved.Our findings suggested that BCA administration protects against fibrotic complications, a property that can be contributed to the multimechanistic approach of the drug

Representative images of liver sections of different experiments.

<p>(<b>A–E</b>): Immunohistochemical detection of COX-2, iNOS, NF-κB, MMP-9 and α-SMA (x100). Control gp: minimal expression; CCl₄ gp: extensive expression; BCA+CCl₄ gp: less than CCl₄ gp; BCA gp: minimal expression. Image analysis was performed by examining 6 fields/slide. (<b>F</b>): Masson trichrome stain (x40). Control gp: shows absence of collagen fibers (stained blue) between hepatic lobules; CCl₄ gp: extensive fibers deposition with pseudolobules formation (bridging fibrosis); BCA+CCl₄ gp: less fibers than CCl₄ gp; BCA gp: absence of fibers. The bar chart represents levels of hydroxyproline expressed as µg/gm of wet tissue measured by Reddy’s method. <i>a</i>: significantly different from control gp. <i>b</i>: significantly different from CCl₄ gp.</p