Research Update:Coleus forskohlii,Forskolin.

  seminal trace...Coleus Forskohlii.Makandi Root,Forskolin.5:1;10:1Extract....

 


   Phytochemical info of Coleus Forskohlii

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 Definition:Coleus Forskohlii are majorly composed of
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   Research Update:Coleus forskohlii,Forskolin.

  Two minor diterpene glycosides and an eudesman sesquiterpene from Coleus forskohlii:Chem Pharm Bull. 2007 Mar;55(3):376-81.Shan Y, Wang X, Zhou X, Kong L, Niwa M.Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, The People's Republic of China.

 Two new labdane diterpene glycosides, forskoditerpenosides A, B (1, 2) and a new eudesmane sesquiterpene, 4beta,7beta,11-enantioeudesmantriol (3), were isolated from the ethanol extract of the whole plant of Coleus forskohlii. Their structures and stereochemistry were elucidated by extensive spectroscopic analysis and chemical methods. The structure of compound 3 was confirmed by X-ray diffraction. This is the first report about the occurrence of glycosides derived from the kind of labdane diterpene, 8,13-epoxy-labd-14-en-11-one, in the nature. Compounds 1 and 2 showed relaxative effects on isolated guinea pig tracheal spirals in vitro.

  Identification of a forskolin-like molecule in human renal cysts:J Am Soc Nephrol. 2007 Mar;18(3):934-43. Epub 2007 Jan 24.Putnam WC, Swenson SM, Reif GA, Wallace DP, Helmkamp GM Jr, Grantham JJ.Midwest Research Institute, Kansas City, Missouri, USA.

 Renal cyst enlargement is increased by adenosine cAMP, which is produced within mural epithelial cells. In a search for modulators of cAMP synthesis cyst fluids from 18 patients with autosomal dominant or recessive polycystic kidney disease (PKD) were analyzed, and in 15 of them, a stable lipophilic molecule that increased cAMP levels, stimulated transepithelial chloride and fluid secretion, and promoted the proliferation of human cyst epithelial cells was characterized. With the use of HPLC-mass spectrometry, a bioactive lipid with the same mass spectral fingerprint, the same chromatographic retention time, and the same biologic properties as forskolin, a widely known, potent adenylyl cyclase agonist, has been isolated and identified within the cyst fluid. Forskolin is synthesized by the plant Coleus forskohlii, but its appearance or compounds like it have not been reported in animals. The origin of forskolin in patients with PKD was not revealed by this study. Synthesis by mural cyst epithelial cells or an exogenous source are the most likely possibilities. Forskolin is sold for weight management and as a cardiovascular tonic in health stores and through the Worldwide Web. It is concluded that forskolin may have a role in promoting the enlargement of cysts in autosomal dominant PKD and recommended that patients avoid oral and parenteral preparations that contain this compound.

  A forskolin derivative, FSK88, induces apoptosis in human gastric cancer BGC823 cells through caspase activation involving regulation of Bcl-2 family gene expression, dissipation of mitochondrial membrane potential and cytochrome c release.:Cell Biol Int. 2006 Nov;30(11):940-6. Epub 2006 Jul 5.Li Z, Wang J.State Key Laboratory of Biomembrane and Membrane Biotechnology, Institute of Zoology, Chinese Academy of Sciences, 25 Beisihuan Xi Road, 100080 Beijing, China. lizhhai@gmail.com

 FSK88, a forskolin derivative, was extracted and purified from cultured tropical plant roots, Coleus forskohlii. Our previous studies have demonstrated that FSK88 can inhibit HL-60 cell proliferation and induce the differentiation of HL-60 cells to monocyte macrophages. In this study, we showed that FSK88 can induce apoptotic death of human gastric cancer BGC823 cells in a dose- and time-dependent manner. Results showed that FSK88-induced apoptosis was accompanied by the mitochondrial release of cytochrome c and activation of caspase-3 in BGC823 cells. Furthermore, treatment with caspase-3 inhibitor (z-DEVD-fmk) was capable of preventing the FSK88-induced caspase-3 activity and apoptosis. FSK88-induced apoptosis in human gastric cancer BGC823 cells was also accompanied by the up-regulation of Bax, Bad and down-regulation of Bcl-2. Theses results clearly demonstrated that the induction of apoptosis by FSK88 involved multiple cellular and molecular pathways and strongly suggest that pro- and anti-apoptotic Bcl-2 family genes, mitochondrial membrane potential (Deltapsi(m)), cytochrome c, and caspase-3, participate in the FSK88-induced apoptotic process in human gastric cancer BGC823 cells.

  Three new diterpenoids from Coleus forskohlii Briq.:J Asian Nat Prod Res. 2006 Jun;8(4):355-60.Yang QR, Wu HZ, Wang XM, Zou GA, Liu YW.HuBei College of Traditional Chinese Medicine, Key Laboratory of Phytochemistry, 430061, Wuhan, China.

 Three new diterpenoids, forskolin G(2), forskolin H(3), forskolin I(4), were isolated from the whole plant of the Coleus forskohlii Briq., and their structures were elucidated as 1alpha,6beta-diacetoxy-8,13-epoxylabd-14-en-11-one, 1alpha-hydroxy-6beta,7beta-diacetoxy-8,13-epoxylabd-14-en-11-one, and 1alpha,9alpha-dihydroxy-6beta,7alpha-diacetoxy-8,13-epoxylabd-14-en-11-one on the basis of spectral data.

  Antioxidant, anticlastogenic and radioprotective effect of Coleus aromaticus on Chinese hamster fibroblast cells (V79) exposed to gamma radiation:Mutagenesis. 2006 Jul;21(4):237-42. Epub 2006 May 30.Rao BS, Shanbhoge R, Upadhya D, Jagetia GC, Adiga SK, Kumar P, Guruprasad K, Gayathri P.Department of Radiobiology, Life Sciences Center, Manipal 576104, Karnataka, India. raokmc@yahoo.com

 Coleus aromaticus (Benth, Family: Laminaceae), Indian Oregano native to India and Mediterranean, is well known for its medicinal properties. A preliminary study was undertaken to elucidate in vitro free radical scavenging potential and inhibition of lipid peroxidation by C.aromaticus hydroalcoholic extract (CAE). Anti-clastogenic and radioprotective potential of CAE were studied using micronucleus assay after irradiating Chinese hamster fibroblast (V79) cells. CAE at 10, 20, 40, 60, 80, 100 and 120 mug/ml resulted in a dose-dependent increase in radical scavenging ability against various free radicals viz., 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), superoxide anion (O(2)(*-)), hydroxyl (OH(*)) and nitric oxide (NO(*)) generated in vitro. A maximum scavenging potential was noticed at 100 mug/ml and a saturation point was reached thereafter with the increasing doses of CAE. The free radical scavenging potential of the extract was in the order of DPPH > ABTS > Superoxide > Hydroxyl > Nitric oxide. CAE also exhibited a moderate inhibition of lipid peroxidation in vitro, with a maximum inhibition at 60 mug/ml (33%), attaining saturation at higher doses. The extract also rendered protection against radiation induced DNA damage, as evidenced by the significant (P < 0.05) decrease in the percentage of radiation-induced micronucleated cells (MN) and frequency of micronuclei (total). A maximum anticlastogneic effect/ radioprotection was noticed at a very low concentration i.e., 5 mug/ml of CAE, treated 1 h prior to 2 Gy of gamma radiation. A significant (P < 0.0001) anticlastogenic/radioprotective effect was also observed when the cells were treated with an optimum dose of CAE (5 mug/ml) 1 h prior to 0.5, 1, 2 and 4 Gy of gamma radiation compared with the respective radiation control groups. Overall, our results established an efficient antioxidant, anticlastogenic and radioprotective potential of CAE, which may be of great pharmacological importance.


  Tracheid analysis and modeling of the minor veins of the coleus and smilax leaves:Planta. 2006 Sep;224(4):915-23. Epub 2006 Mar 24.Korn R.Department of Biology, Bellarmine University, 2001 Newburg Road, Louisville, KY 40205, USA. rkorn@bellarmine.edu

 Tracheid analysis was carried out on the veinlets and minor veins of the coleus (Solenostemon scutellarioides [L.] Codd) leaf. Third- to fifth-order, or minor, veins average 3.4 tracheids in tandem and they bipartition islets when these enclosed islets reach a critical size; both these features of vein length and islet size contribute to a self-similar process of vein pattern generation. An areole was calculated to be initially comprised of about ten cells making the patterning event for vein formation requiring only a few cells. An algorithmic model developed here for minor vein formation includes five production rules, and this computer model explains the 3-4 tracheids per minor vein, presence of isolated tracheids, the structure of veinlets, and the elaborate branching patterns of veinlets in coleus and other plants.

  Studies on the chemical constituents in root of Coleus forskohlii:Zhongguo Zhong Yao Za Zhi. 2005 Nov;30(22):1753-5. Chinese.Xu LL, Lu J, Li WJ, Kong LY. Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210038, China.

 OBJECTIVE: To study the chemical constituents in root of Coleusforskohlii. METHOD: The chemical constituents were isolated by column chromatography. The structures were elucidated on the basis of IR, MS, 1H-NMR, 13C-NMR and 2D-NMR experiments. RESULT: Six compounds were obtained and the structures were identified as 14-deoxycoleon U (1), demethylcryptojaponol (2), alpha-amyrin (3), betulic acid (4), alpha-cedrol (5) and beta-sitosterol (6). CONCLUSION: Compounds 1 and 2 were isolated from the genus Coleus for the first time. Compounds 3 and 4 were isolated from C. forskohlii for the first time.

  Simple and rapid method for the isolation of forskolin from Coleus forskohlii by charcoal column chromatography.:J Chromatogr A. 2006 Jan 6;1101(1-2):313-4. Epub 2005 Dec 1.Saleem AM, Dhasan PB, Rafiullah MR.Department of Pharmacognosy, C.L. Baid Metha College of Pharmacy, Thoraippakkam, Chennai 600096, India. saleemskma@rediffmail.com

 A simple, safe, rapid and economical method was developed for the isolation of high-purity forskolin from Coleus forskohlii roots using activated charcoal as an adsorbent in a column. The elution was carried out under reduced pressure to make the process rapid. Activated charcoal acted as a reversed phase adsorbent and allowed elution of forskolin without much impurities. The residue, obtained from the eluate was purified and crystallized using different solvent mixtures to obtain pure forskolin. The forskolin isolated was analyzed and characterized by UV, IR, RP-HPLC, electrospray ionization MS, 1H NMR and 13C NMR. The yield was 0.097% w/w (RSD 5.6%). The purity was 96.9% w/w (RSD 0.3%) as determined by RP-HPLC. The present method enables researchers to produce high-purity forskolin in their labs by using common chemicals.

  Two new diterpenoids from Coleus forskohlii.:J Asian Nat Prod Res. 2005 Dec;7(6):811-5.Shen YH, Xu YL.State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, Yunnan, China.

 Two new diterpenoids, forskolins I and J, have been isolated in our further investigation on Coleus forskohlii (Willd.) Briq. collected in Yunnan Province. Their structures have been determined as 1alpha,6beta-diacetoxy-7beta,9alpha-dihydroxy-8,13-epoxylabd-14-en-11-one (1) and 1alpha,9alpha-dihydroxy-6beta,7beta-diacetoxy-8,13-epoxylabd-14-en-11-one (2) by spectral methods (including 1D and 2D NMR techniques).

  Influence of different AM-fungi on the growth, nutrition and forskolin content of Coleus forskohlii:Mycol Res. 2005 Jul;109(Pt 7):795-8.Sailo GL, Bagyaraj DJ. Department of Agricultural Microbiology, University of Agricultural Sciences, GKVK Campus, Bangalore-560 065, India. g.sailo@coventry.ac.uk

 A glasshouse investigation was conducted to study the effectiveness of 11 arbuscular mycorrhizal (AM) fungi on the medicinal plant Coleusforskohlii. Coleus plants raised in presence of most of the AM fungi in polythene bags showed an increase in plant growth (height, number of branches and biomass), P, and forskolin contents over those grown in the absence of soil inoculation with AM fungi. The extent of growth, P, and forskolin status varied with the AM fungi used. Based on the plant biomass, P uptake and forskolin content per plant, Glomus bagyarajii was found to be the best AM symbiont for inoculating C. forskohlii, the next being Scutellospora calospora.


  Water-soluble extract of Coleus barbatus modulates weight gain, energy utilization and lipid metabolism in secondary biliary cirrhosis: an experimental study in young rats.:Acta Cir Bras. 2005 May-Jun;20(3):229-36.Battochio AP, Sartori MS, Coelho CA.Department of Pediatrics, Botucatu School of Medicine, the S?o Paulo State University. apbattochio@ig.com.br

 PURPOSE: To test if a water extract of Coleus barbatus (WEB) has any effect on weight gain, food energy utilization and lipid metabolism in young rats with obstructive cholestasis. METHODS: Forty 21 day old (P21) Wistar rats, in groups of 10, were submitted to one of the following treatments: a sham operation with daily water or WEB administration, double ligature and resection of the bile duct with daily water or WEB administration. At P49 they were submitted for euthanasia when the following were determined: ingested feed (IF), energy utilization (EU) and weight gain (WG) from P29 to P49, together with total serum cholesterol (TC) and triacylglycerol (TG) concentrations, liver wet weight (LWW) and fat content (LFC). Two Way ANOVA and the S.N.K. test for paired comparisons were employed to study the effects of cholestasis and those of WEB and their interactions (p < or = 0.05). RESULTS: Cholestasis, independently of WEB, and WEB, independently of cholestasis both reduced IF, EU, and WG but there was no significant interaction between the two factors. Cholestasis, independently of WEB, increased LWW, LFC, the TC and TG The WEB, independently of cholestasis, reduced these values, and there was a significant interaction between the two factors; such that these effects were more accentuated in animals with cholestasis. CONCLUSION: The WEB reduced IF, WG, and EU, both in the presence and absence of cholestasis in the same proportion. It also partially inhibited the increase in LWW, LFC, TC and TG caused by cholestasis.

  Effects of Coleus forskohlii on fat storage in ovariectomized rats.:Yakugaku Zasshi. 2005 May;125(5):449-53.Han LK, Morimoto C, Yu RH, Okuda H. Department of Environmental and Symbiotic Sciences, Prefectural University of Kumamoto, 3-1-100 Tsukide, Kumamoto 862-8502, USA. hanlikun@hotmail.com

 The antiobesity effects of Coleus forskohlii were investigated in ovariectomized (ovx) rats. Eight-week-old female Wistar rats were assigned to four groups: a sham-operated group fed the control diet (MF, sham-m) ; an ovx-m group fed the control diet; a sham-operated group fed the control diet containing 50 g/kg of Coleus forskohlii extract (sham-c) ; and an ovx-c group fed the control diet containing 50 g/kg of Coleus forskohlii extract. The body weight, adipose tissues, and cell diameter were investigated in ovx rats after Coleus forskohlii extract treatment. Administration of Coleus forskohlii extracts reduced body weight, food intake, and fat accumulation in ovx rats. Our results suggest that Coleus forskohlii may be useful in the treatment of obesity.

  Quantitative analysis of forskolin in Coleus forskohlii (Lamiaceae) by reversed-phase liquid chromatography.:J AOAC Int. 2003 May-Jun;86(3):467-70.Schaneberg BT, Khan IA.National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, The University of Mississippi, School of Pharmacy, University, MS 38677, USA.

 A rapid method was developed for the evaluation of forskolin in Coleus forskohlii Briq. (Lamiaceae). Forskolin was quantitated in the root and stem of dried C. forskohlii and in 17 market products by reversed-phase liquid chromatography (LC) with a photodiode array detector at 210 nm. The temperature was held constant at 30 degrees C, and the retention time of forskolin was approximately 6.8 min. The samples were extracted with acetonitrile by sonication. The precision of the method was confirmed by a standard deviation < 5.0% (n = 3), and forskolin recovery was 99.1%. Limit of detection was 1.5 microg/mL, and the response was linear through zero from 6.3 to 630 microg/mL with a correlation coefficient (R2) of 0.9998. Identity of the marker compound was confirmed by an LC/mass spectrometry experiment. The method was successful in the qualitative and quantitative evaluation of the marker compound in C. forskohlii plant material and in market products claiming to contain C. forskohlii.

  Insulin and glucagon releasing activity of coleonol (forskolin) and its effect on blood glucose level in normal and alloxan diabetic rats.:Acta Diabetol Lat. 1991 Jan-Mar;28(1):71-7.Ahmad F, Khan MM, Rastogi AK, Kidwai JR.Division of Biochemistry, Central Drug Research Institute, Lucknow, India.

 Colenol, a diterpenoid isolated from the roots of Coleus forskohlii stimulates the release of insulin and glucagon from the islets both in vitro and in vivo. Colenol-stimulated release of glucagon from islets in vitro is much more pronounced as compared to that of insulin. Glucose concentration of 5.6 mM in the medium is required for the colenol stimulation of insulin release. Feeding of coleonol to alloxan diabetic rats cause 36.5% increase in blood glucose level as compared to alloxan diabetic control. Oral feeding of coleonol for 7 days to normal rats causes increase in blood glucose, serum insulin, glucagon and free fatty acid levels with corresponding increase in glucose-6-phosphatase activity and depletion of liver glycogen. Predominant stimulation of A-cells by coleonol is suggested for the above effects.


  Scientific References:

  1.Research Update:Coleus forskohlii,Forskolin.