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It is plant known since the 19 th century, native of the forest regions of Central and Southern United States which has traditionally been used for anti-spasmodic treatment, dysmenorrhea and other pains caused by contractions of smooth muscles. Also at threats of premature birth and to increase the uterine tone after the surgical removal of fibromas.
It belongs to the family of Caprifoliaceae which has 15 different genus . The prescription of V. prunifolium is frequently interchanged with V. opulus as its therapeutic effect is similar, however, the active antispasmodic elements of V. prunifolium are the cumarins while the antispasmode of V. opulus is viopudial. |
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Description
A bush with a straight stem. Green, soft, finely serrated leaves, opposed, elliptic to oval. Small white flowers in racemes of with a width of 10 cmts. The fruits are edible black-blue berries.
Used Parts
The bark of the stem, the branches and the root.
Traditional Uses
The Viburnums has traditionally been used for the treatment of dysentery and to stop uterine hemorrhage. Today, it is considered a specific treatment to soothe menstrual pain due to its contents of scopoletin, a cumarin with antispasmodic and sedative effects on smooth muscles and salycine a recognized analgesic.
The bark of the stem and of the roots is antispasmodic. An infusion is used orally for the treatment of painful or profuse menstruations, uterine prolapse, to stop the contractions of early birth and to soothe the spasms after giving birth. Also for other colic pains like the ones that affect the bile ways or the asthmatic bronchospasm.
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Active Elements
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• Cumarines, including scopoletine, scopoline, and sculetine.
• Flavonoids (amentoflavone).
• Beta-sitosterol.
• Iridoids Glucosides.
• Triterpenes and triterpenic acids.
• Organic acids, including acetic, capronic, caprilic, citric, isovaleric, linoleic, malic, myristic, oleic, oleanolic, oxalic, palmitic, ursolic and valeric. |
SCOPOLETINE |
• Derivates of hydroxinamic acids like: cafeic, chlorinogenic and isochlorinogenic acids.
• Triterpenes: alpha and beta-amirine.
• Tannins (2%).
• Salicylic acid, Salicyne. Some investigators consider that the plant does not contain salicyne and that this element has been mistaken for Arbutine.
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| Mechanisms of Action:
Its cumarinic derivates have a spasmolytic effect by the inhibition of the mobilization of the intercellular calcium and by the inhibition of the synthesis of nitric oxide.
The salicylic acid and the salicyne give it analgesic properties.
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SPASMOLYTIC |
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| Indications
1) Treatment of bile, intestinal, uterine, genitourinary or bronchial colics.
2) Dysmenorrhea.
3) Threat of abortion or early birth.
4) Hemorrhage after giving birth.
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| Doses:
2 capsules of 350 mg of Viburnum spp. powder with every meal.
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| Adverse Effects:
At the recommended doses there is no adverse secondary effect
Counterindications:
Should not be taken by persons who are allergic against salicylates.
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References
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2: Woodbury RA, 1951, 'The Viburnums ', Drug Standards 19(7-8), pp. 143-152.
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3: Youngken HW, 1932, 'The pharmacognosy , chemistry and pharmacology of Viburnum III. History, botany and pharmacognosy of Viburnum opulus L var americanum (Miller) Ait ', J Am Pharm Assoc 22, pp. 444-62.
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7. Launert E. Edible and Medicinal Plants. Hamlyn
9. Uphof J. C. Th. Dictionary of Economic Plants. Weinheim 1959
12. Ovodova RG, Golovchenko VV, Popov SV. [The
isolation, preliminary study of structure and physiological activity
of water-soluble polysaccharides from squeezed berries of Snowball
tree Viburnum opulus ] Bioorg Khim . 2000 Jan ;26 (1):61-7.
13. Jarboe CH, Zirvi KA, Schmidt CM. 1-methyl 2
,3 -dibutyl hemimellitate . A novel component of Viburnum prunifolium
. J Org Chem . 1969 Dec ;34 (12):4202-3.
14. Horhammer L, Wagner H, Reinhardt H. [On new
substances contained in the back of Viburnum prunifolium L. (American
guelder -rose) and Viburnum opulus L (common guelder -rose)]. Z
Naturforsch B. 1967 Jul ;22 (7):768-76.
15. Nicholson JA, Darby TD, Jarboe CH. Viopudial
, a hypotensive and smooth muscle antispasmodic from Viburnum opulus
. Proc Soc Exp Biol Med 1972 Jun;140(2):457-461
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16: Biochem Pharmacol . 2003 Jun 1 ;65 (11):1897-905.
Esculetin inhibits Ras -mediated cell proliferation and attenuates vascular restenosis following angioplasty in rats.
Pan SL, Huang YW, Guh JH, Chang YL, Peng CY, Teng CM.
Pharmacological Institute, College of Medicine, National Taiwan University, Taipei, Taiwan, ROC. |
| The proliferation of vascular smooth muscle cells ( VSMCs ) induced by injury to the intima of arteries is an important etiologic factor in vascular proliferative disorders such as atherosclerosis and restenosis . Esculetin , derived from the Chinese herb Artemisia scoparia , is well known as a lipoxygenase inhibitor. We have investigated the inhibitory effects of esculetin on VSMC proliferation and intimal hyperplasia by balloon angioplasty in the rat. We determined, using [3H ] thymidine incorporation and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, that esculetin inhibited the proliferation of VSMCs via a lipoxygenase -independent pathway. Three predominant signaling pathways were identified to be inhibited by esculetin : (a) the activation of p42/44 mitogen -activated protein kinase (MAPK) and the downstream effectors of c- fos and c- jun immediate early genes by means of western and reverse transcription-polymerase chain reaction (RT-PCR) analyses; (b) the activation of nuclear factor- kappaB (NF- kappaB ) and activator protein-1 (AP-1), using the electrophoretic mobility shift assay; and (c) the activation of phosphoinositide 3-kinase (PI 3-kinase) and cell cycle progression, by western blot analysis and flow cytometric detection. Furthermore, esculetin also profoundly inhibited Ras activation, a shared upstream event of the above signaling cascades. In vascular injury studies, intraperitoneal administration of esculetin significantly suppressed intimal hyperplasia induced by balloon angioplasty. We conclude that esculetin blocks cell proliferation via the inhibition of an upstream effector of Ras and downstream events including p42/44 MAPK activation, PI 3-kinase activation, immediate early gene expression, as well as NF- kappaB and AP-1 activation. It also inhibits intimal hyperplasia after balloon vascular injury in the rat, indicating the therapeutic potential for treating restenosis after arterial injury. |
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17: Planta Med. 2001 Oct ;67 (7):605-8.
Intracellular calcium mobilization as a target for the spasmolytic action of scopoletin .
Oliveira EJ, Romero MA, Silva MS, Silva BA, Medeiros IA.
Laboratorio de Tecnologia Farmaceutica , Universidade Federal da Paraiba , Brazil .
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| The coumarin scopoletin was isolated in a pure form from the roots of Brunfelsia hopeana Benth . ( Solanaceae ). In isolated rat aortic rings, scopoletin (26-520 microM ) inhibited to approximately the same extent the contractions induced by a variety of substances, including phenylephrine , potassium chloride, serotonin and PGF( 2) (alpha). The effect of the coumarin on phenylephrine -induced contractions was not affected by endothelium removal or NO- synthase blockade by L-NAME (100 microM ). Scopoletin (78 - 590 microM ) antagonized in a concentration-dependent manner ( IC( 50) = 300 +/- 20 microM , n = 5), transient contractions in Ca(2+)-free media induced by noradrenaline , but not those induced by caffeine. Also, scopoletin did not interfere with the refilling of noradrenaline -sensitive intracellular calcium stores. It is suggested that the non-specific spasmolytic action of scopoletin can be attributed, at least in part, to its ability to inhibit the intracellular calcium mobilization from the noradrenaline -sensitive stores. |
18: Planta Med. 1999 Jun ;65 (5):400-3.
Scopoletin : an inducible nitric oxide synthesis inhibitory active constituent from Artemisia feddei .
Kang TH, Pae HO, Jeong SJ, Yoo JC, Choi BM, Jun CD, Chung HT, Miyamoto T, Higuchi R.
College of Pharmacy, Wonkwang University, Iksan , Korea.
Bioassay-guided fractionation of an H2O extract of Artemisia feddei has furnished an inducible nitric oxide synthase ( iNOS ) inhibitory coumarin , scopoletin (1) and one of the inactive sesquiterpenes , achillin (2). Compound 1 showed inhibition of nitric oxide (NO) synthesis in a dose-dependent manner in murine macrophage-like RAW 264.7 cells stimulated with interferon-gamma (IFN-gamma) plus lipopolysaccharide (LPS). The inhibition of NO synthesis of 1 was due to suppression of iNOS mRNA and iNOS protein, as determined by Northern and Western blotting, respectively. |
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19: Pharmacol Res. 1989 Mar-Apr ;21 (2):183-92.
Effects of esculetin (6 ,7 -dihydroxycoumarin) on guinea-pig tracheal chains in vitro.
Ragazzi E, Froldi G, Fassina G .
Department of Pharmacology, University of Padova , Italy .
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| Esculetin (6 ,7 -dihydroxycoumarin) was tested in isolated guinea-pig tracheal chains from normal and ovalbumin -sensitized animals. The drug showed a concentration-dependent relaxant effect, with an EC50 of 60 microM . Pretreatment with esculetin (30-60 microM ) was not able to reduce the contractile response induced by either carbachol (0.1 microM ), histamine (10 microM ), BaCl2 ( 10 mM ) or K+ ( 80 mM ). Esculetin increased the contraction evoked by PGF2 alpha and by histamine, but reduced A23187-induced contraction. Mepacrine (10 microM ), a phospholipase A2 inhibitor, reduced the relaxant effect of the lower esculetin concentrations (3-60 microM ). Indomethacin (0.1 microM ) increased the relaxation induced by esculetin (3-10 microM ). In tracheal chains from ovalbumin -sensitized guinea-pigs, esculetin (60 microM ) significantly reduced the duration of the recovery phase after antigen challenge contraction. In conclusion, in our in vitro conditions, this natural coumarin derivative seems to act by interfering with the arachidonic acid cascade. |
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20: Pharmacol Res Commun . 1988 Dec ;20 Suppl 5:83-5.
Anti-inflammatory and peripheral analgesic activity of esculetin in vivo.
Tubaro A, Del Negro P, Ragazzi E, Zampiron S, Della Loggia R.
Institute of Pharmacology and Pharmacognosy , University of Trieste, Italy.
Esculetin determined a reduction in oedema and granulocyte infiltration in the Croton oil ear test in vivo. The drug was able to inhibit Acethylcholine -writhing test and showed a LD50 of 1450 mg/kg i.p . and greater than 2000 mg/kg by mouth. In our experimental conditions, esculetin has an anti-inflammatory and analgesic effect. |
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21: Biochim Biophys Acta . 1983 Aug 29 ;753 (1):130-2.
Inhibitory effect of esculetin on 5-lipoxygenase and leukotriene biosynthesis.
Neichi T, Koshihara Y, Murota S. |
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Esculetin (6 ,7 -dihydroxycoumarin) showed inhibitory effects on 5- and 12-lipoxygenases of cloned mastocytoma cells. The half-inhibition dose (ID50) for each enzyme was 4 X 10(-6) and 2.5 X 10(-6) M, respectively. No inhibition at all, but rather a stimulating effect on prostaglandin synthesis, was observed, especially at higher doses of esculetin . Leukotriene synthesis by mouse mast tumour cells was also reduced in the presence of esculetin in parallel with 5-lipoxygenase inhibition. From these results, esculetin may be useful as a tool for research on regulatory mechanisms or physiological functions of leukotrienes. |
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22: Poceedings of the Societa Italiana di Fitochimica 9th National Congress, May 1998, Societa Italiana di Fitochimica , Florence , p 115-6.
Iridoid glucosides from Viburnum prunifolium and preliminary pharmacological studies',
Tomassini L, Cometa MF, Palmery M, Nicoletti M.
In this study it was shown that total V. prunifolium extract, ethyl acetate, and butanol fractions inhibited spontaneous contractions of isolated rat uteri by approximately 50%. Additionally, inhibition of the rise in tone and reduction of the ampitude of acetylcholine-induced contractions was observed. |
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23: Med Plants Phytother 17(3), pp 123-32.
Criteres de choix d'un extrait de viburnum , Viburnum prunifolium L., en fonction de ses actions toniveineuse et spasmolytique
Balansard G, Chausse D, Boukef K.
In this study it was reported that a 30% ethanol extract of V. prunifolium elicited a spasmolytic activity that was five times greater than a 60% ethanol extract. It was concluded that while the spasmolytic activity was clearly less than that of papaverine , it was nevertheless significant. |
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24: Proceedings of the Society for Experimental Biology and Medicine, June, 1972, Vol. 110, No. 2, pp. 457-461
Viopudial , a Hypotensive and Smooth Muscle Antispasmodic
Nicholson, J. A., Darby, T. D., and Jarboe , C. H.
The American variety of Viburnum opulus , native to the northern and eastern United States , is commonly referred to as the "Cranberry Bush" or "High Bush Cranberry" . At this time we wish to report a second active constituent of V. opulus , a nonalkaloidal material isolated from plant bark. This substance has also show striking cardiovascular effects on the rat, cat and dog, in addition to antispasmodic effects on in vitro rat uteri. . In vivo rat experiments showed hypotensive effects at an iv dose of 250 µg/kg. At 1 mg/kg these effects became somewhat sustained and the decrease in blood pressure was accompanied by a decrease in heart rate. . Summary. The administration of viopudial a Viburnum opulus component, produces bradycardia , hypotension, and some decrease in myocardial contractility. Experimental evidence indicates that viopudial's mechanism of action is partly due to its effects on cholinesterase. In vitro demonstrations of a competitive inhibitory effect on both acetylcholinesterase and butyrylcholinesterase showed viopudial to be relatively weak when compared to know potent inhibitor, physosgitmine . Additional mechanistic effects, such as a direct musculotrophic action, may also be responsible for the overall activity. |
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25: Nature. 1966 Nov 19; 212(64): 837.
Uterine Relaxant Properties of Viburnum
Jarboe , C. H., Schmidt C. M., Nicholson, J. A., and Zirvi , K. A. |
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Several species have been mentioned repeatedly as uterine relaxants and general antispasmodics. Those most commonly cited are V. opulus (Cramp Bark) . These results obtained from know material and uteri in a known state of oestrus show that there is no doubt as to the uterine antispasmodic properties of Viburnum opulus . Our investigations of the chemistry of Viburnum have been restricted to the historical examples, V. prunifolium and V. opulus . Using column and thin layer chromatography we have isolated from these two species a minimum of four very active uterine relaxants and are involved in structural and mechanistic analyses. The mechanism studies lead us to postulate that these substances are not sympathomimetic in action, but selective uterine relaxants which act directly on the muscle. |
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