08. MP and MPM that contain triterpenoid saponins

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Transcript 08. MP and MPM that contain triterpenoid saponins

Herbs and herbs raw stuff that
contain triterpenoid saponins
Glycyrrhizae radices, EuPh
Liquoritiae radices
Liquorice root
Glycyrrhiza glabraFabaceae
Content: minimum 4 % of glycyrrhizic
acid
IDENTIFICATION
A. The root has few branches. Its bark is brownishgrey or brown with longitudinal striations and bears
traces of lateral roots. The cylindrical stolons are 12 cm in diameter; their external appearance is
similar to that of the root but there are occasional
small buds. The fracture of the root and the stolon is
granular and fibrous. The cork layer is thin; the
secondary phloem region is thick and light yellow
with radial striations. The yellow xylem cylinder is
compact, with a radiate structure. The stolon has a
central pith, which is absent from the root. The
external part of the bark is absent from the peeled
root.
B. Fragments of yellow thick-walled
fibres, 700-1200 μm long and 10-20
μm wide with a punctiform lumen,
often accompanied by crystal
sheaths containing prisms of calcium
oxalate 10-35 μm, long and 2-5 μm
wide. The walls of the large vessels
are yellow, 5-10 μm thick, lignified and
have numerous bordered pits with a
slit-shaped aperture; fragments of cork
consisting of thin-walled cells and
isolated prisms of calcium oxalate
occur as well as fragments of
parenchymatous tissue. Fragments of
cork are absent from the peeled root.
Simple, round or oval starch granules,
2-20 μm in diameter.
C. Thin-layer chromatography
Reference solution. Dissolve 5.0 mg of glycyrrhetic acid R and 5.0 mg of thymol R in
5.0 ml of ether R.
TESTS
Loss on drying (2.2.32) : maximum 10.0 per cent, determined
on 1.000 g of powdered drug (355) (2.9.12) by drying in an
oven at 105 °C for 2 h.
Total ash (2.4.16) : maximum 10.0 per cent for the unpeeled
drug and maximum 6.0 per cent for the peeled drug.
Ash insoluble in hydrochloric acid (2.8.1) : maximum
2.0 per cent for the unpeeled drug and maximum 0.5 per
cent for the peeled drug.
ASSAY
Liquid chromatography (2.2.29)
Monoammonium glycyrrhizate

Constituents. 5 to 8% of glycyrrhizin, an intensely sweet, watersoluble principle consisting of the potassium and calcium salts of
glycyrrhizinic acid; glycyramarin (a bitter principle) occurring mostly
in the bark; mannite, volatile oil, resin, starch, sucrose, glucose,
flavonoid glucosides, calcium oxalate, pectinic substances etc.
Glycyrrhetic acid
Uses. Demulcent, expectorant and flavouring agent. The powdered root
is extensively employed as a pill excipient and the fluid extract to
disquise the taste of nauseus preparations. Most of the licorice imported
is used by the tobacco manufacturers in the flavouring of tobacco.
Preparations: Glycyrrhiza extract, Glycyrrhiza syrup, elixir. Glycyrram
is used for the treatment of bronchial asthma and kidney disorders.
Glycyrrhinol used for trichomonadal colpitis.
At bronchial asthma, allergy dermatitis, other allergic
condition
Mineralcorticoid effects: Licorice inhibits the enzyme
1l-β-hydroxysteroid dehydrogenase in the kidney, which leads
to decreased transformation of cortisol into cortisone.The
mineralocorticoid action of Cortisol causes a decrease in
serum potassium and an increase in serum sodium
concentration resulting in retention of water, causing
weight increase and hypertension. Glyclrrhetic acid, the
hydrolpic metabolite of glycerrhizic acid causes the inhibition
of peripheral metabolism of cortisol and produces a pseudoaldosterone like effect.
Araliae mandshuricae radices
Aralia mandshuricaManchurian aralia
Araliaceae
 Constituents. Volatile oil
(0.33%); a glycosidal saponin
called aralin; resin (3%),
starch, tannin, pectin, sugar,
etc.
 Uses. Stimulant and
diaphoretic. Preparations:
tincture and saparal (tablets)
are used to treat nervous
disorders, hypotension and
depression. It is a component
of the antidiabetic herbal
composition ‘Arfazetin’
Asthenic neurotic
symptoms, physical fatigue
and mental fatigue,
impotence, hypotension
Orthosiphonis folia, EuPh
Orthosiphon stamineus- Java tea
Lamiaceae
Content : minimum 0.05 per cent of
sinensetin (C20H20O7 ; Mr 372.4) (dried
drug).
IDENTIFICATION
A. The leaves are friable, up to 7.5 cm in length and 2.5 cm
in width. The petiole is short. The lamina is oval to
lanceolate, the apex acuminate and the base cuneate. The
abaxial surface of the leaves is light greyish-green and
the adaxial surface is dark green to brownish-green. The venation is pinnate with few
secondary veins. Examined under a lens (x 10), the secondary veins, after running
parallel to the midrib, diverge at an acute angle. The margin is irregularly and roughly
dentate, sometimes crenate and the abaxial surface is slightly curved. The petioles are
thin, quadrangular, 4 mm to 8 mm long and, like the primary venation, usually violetcoloured. Occasionally, inflorescences in clusters of bluish-white to violet flowers, not
yet opened, are found.
B. The powder shows fragments of epidermis, with cells with sinuous
outlines bearing unicellular or bicellular conical covering trichomes and
articulated uniseriate trichomes up to 450 μm long, consisting of 3 to 8
cells with thick pitted walls ; capitate trichomes with unicellular or
bicellular heads; secretory trichomes with unicellular stalks and usually
tetracellular heads; diacytic stomata (2.8.3), which are more numerous on
the lower epidermis.
C. Thin-layer chromatography (2.2.27).
Reference solution. Dissolve 1 mg of sinensetin R in methanol
R and dilute to 20 ml with the same solvent
ASSAY
Liquid chromatography (2.2.29).
Constituents. Leaves contain triterpene spononins- αamyrin derivatives, ursolic acid, flavonoids, ether oil,
organic acids.
Diterpenes: numerous closely related pimarane-type
diterpenes, including orthosiphonones A and B,
orthosiphols A, B, E to I, M, N, P, R, S, T, stiminol A neoorthosiphols A and B, neo-orthosiphone A;
Essential oils: 0.02-0.7 % of various compounds: including
belemene, p-caryophyllene, o-humulene, palmitic acid.
Flavonoids: sinensetin, tetramethylscutellarein. eupatorin,
salvigenin, trimethylapigenin. Phenylpropanoids: rosmarinic
acid (major), caffeoyl tarlrate, dicaffeoyltartrate, four
caffeic acid depsides.
Uses. Java Tea has been shown in human and animal tests to
be a mild diuretic. The essential oil of the drug, which contains
sesquiterpenes, is antimicrobial, antiphlogistic and possibly
antitumoral. It is used for infections of the urinary tract,
kidney and bladder stones
Ginseng radices - Ginseng root, EuPh
Ginseng- Panax ginseng
Araliaceae
Five-fingers, Red berry, American
ginseng, Chinese ginseng, Oriental
ginseng
Definition
Whole or cut dried root, designated white
ginseng; treated with steam and then dried,
designated red ginseng, of Panax ginseng
C. A. Meyer.
Content : minimum 0.40 per cent for the sum of
ginsenosides Rg1 (C42H72O14,2H2O; Mr 837)
and Rb1 (C54H92O23,3H2O; Mr 1163) (dried
drug).
IDENTIFICATION
A. The principal root is fusiform or cylindrical, sometimes
branched, up to about 20 cm long and 2.5 cm in diameter, and
may be curved or markedly re-curved. The surface is pale
yellow to cream in white ginseng, brownish-red in red ginseng
and shows longitudinal ridges. Stem scars may be seen at the
crown. The fracture is short. The transversely-cut surface
shows a wide outer zone with scattered orange-red resin canals
and a finely radiate inner region. The rootlet, numerous in the
lower part of white ginseng, are normally absent in red
ginseng.
B. Reduce to a powder (355) (2.9.12). The powder shows the
following characters : abundant fragments of thin-walled
parenchymatous cells and fragments of large secretory canals
containing yellowish-brown resin, non-lignified tracheids and
partially-lignified vessels with spiral or reticulate thickening,
isolated or in groups; scattered cluster crystals of calcium
oxalate. The starch granules are very abundant, simple or 2 or
3 compound, and range from 1 μm to 10 μm in diameter. In
red ginseng the starch granules are often deformed and
destroyed by treating with steam, or may be absent.
C. Thin-layer chromatography (2.2.27).
Reference solution. Dissolve 5.0 mg of aescin R and 5.0 mg of arbutin R
in 1 ml of methanol R.
TESTS
Panax quinquefolium. Examine the chromatograms
obtained in the assay. The chromatogram obtained with the
test solution shows a peak due to ginsenoside Rf (see Figure
1523.-1). In the case of a substitution by Panax quinquefolium
no peak due to ginsenoside Rf is present.
Loss on drying (2.2.32) : maximum 10.0 per cent,
determined on 1.000 g of the powdered drug (355) (2.9.12) by
drying in an oven at 105 °C.
ASSAY
Liquid chromatography
Reference solution. Dissolve 3.0 mg of ginsenoside Rg1 R, 3.0
mg of ginsenoside Re R, 3.0 mg of ginsenoside Rf R and 3.0
mg of ginsenoside Rb1 R in methanol R and dilute to 10.0 ml
with the same solvent.
Constituents. Ginseng contains a complex mixture of
triterpenoid saponins, these glycosides have been categorised
into 3 series- the panaxosides, the ginsenosides. One or more
of these groups of glycosides appear to account for the
biologic properties of ginseng. It also contains volatile oils,
resin, a phytosterin, mucilage, sugar, starch, etc.
Uses. Ginseng is used by the laity as a stimulant and aromatic
bitter. The Chinese also employ it as an aphrodisiac and heart
tonic but without scientific justification. Ginseng is a favourite
remedy in Chinese medicine and is considered to have tonic,
stimulant, diuretic and carminative properties. It reportedly
reduces the blood glucose concentration and acts favourably
on metabolism, the central nervous system, and endocrine
secretions. It is employed in the Orient in the treatment of
anaemia, diabetes, insomnia, neurasthenia, gastritis and
especially sexual impotence. Medicines- tincture, fluid extract,
yokhimbe-extract and others.
Panaxadiol
Erectile dysfunction and low libido
Adaptogenic and
tonic tool is used at
hipotention, fatigue,
neurasthenia .
Astragali dasyanthi herba
Astragalus dasyanthus- Milk vetch
Fabaceae
 Constituents. Herb
contains flavonoids (mainly
quercetin), triterpenic
glycosides and tannins.

Uses. Water infusion is used
for treatment of
hypertension, cardiovascular
insufficiency, chronic
nephritis.
Echinopanacis rhizomata cum radicibus
Oplopanax elatus- Devil’s club, wolfberry
Araliaceae

Constituents.
Triterpenoid saponins
called echinoxosides (up
to 7%), volatile oils,
flavonoids, alkaloids.

Uses. Analogically to
radix Ginseng.
Hippocastani semina
Hippocastani folia
Aesculus hippocastanum
Hippocastanaceae
Horse chestnut
Constituents. Seeds contain
many triterpenoid saponins which
come under the name aescin.
General content of saponins is 313%. Also contain
hydroxycoumarins; the chief
component is aesculin, in adion
fraxin and scopolin, scopoletin;
flavonoids: including rutin,
quercitrin, and isoquercitrin;
Uses. Traditionally, horse-chestnut has been used for the treatment of
varicose veins, haemorrhoids, phlebitis, diarrhoea, fever and enlargement
of the prostate gland. The German Commrssion E approved use for
treatment of chronic venous insufficiency in the legs.
As found in different animal tests and preclincal investigations,
the principal ingredient of Horse Chestnut seed extract, triterpene
glycoside mixture (aescin) has an anti-exudative, vascular tightening
effect, and reduction of vascular permeability, which result in an
antieodemic effect. The yein-toning properties of the Horse Chestnut
extract also demonstrated improvement ofvenous return flow. Treatment
of symptoms found in pathological conditions ofthe veins ofthe legs
(chronic venous insufficiency), for example, pain and a sensation of
heaviness in the legs, nocturnal cramps in the calves, pruritis and
welling of the legs. Drugs are Venostasin, Retardkapseln, Noricaven,
Rexiluven, Aescusan, Hoevenol, etc.
Homoeopathic treatments include haemorrhoids, lumbar and low
back pain, venous back pressure.
Calendulae flores , EuPh
Calendula officinalis L.
Pot Marigold or Scotch Marigold
Asteraceae
Content : minimum 0.4 per cent of
flavonoids, expressed as hyperoside
(C21H20O12 ; Mr 464.4) (dried drug).
IDENTIFICATION
A. The ligulate florets consist of a yellow or orange-yellow ligule, about
3-5 mm wide and about 7 mm in the middle part, with a 3-toothed apex
and a hairy, partly sickle-shaped, yellowish-brown or orange-brown tube
with a projecting style and a bifid stigma occasionally with a partly bent
yellowish-brown or orange-brown ovary. The tubular florets, about 5 mm
long, are present and consist of the yellow, orange-red or reddish-violet
5-lobed corolla and the yellowish-brown or orange-brown tube, hairy in
its lower part, mostly with a partly bent yellowish-brown or orangebrown ovary.
B. Examine under a microscope using
chloral hydrate solution R. The powder
shows : fragments of the corollas
containing light yellow oil droplets.
A and B. Epidermis of the corolla
G. Fragment of the stigma
C. Epidermis at the apex of the corolla
showing anomocytic stomata
H. Covering trichome (usually only
fragments observed)
D. Fragments of vessel tissue attached to
parenchyma cells
containing cluster crystals of calcium
oxalate
J. Cells from the base of the corolla and
glandular trichomes
E and F. Pollen grains
K. Glandular trichome
C. Thin-layer chromatography
Reference solution. Dissolve 1.0mg of caffeic acid R, 1.0 mg
of chlorogenic acid R and 2.5 mg of rutin R in 10 ml of
methanol R.
TESTS
Foreign matter (2.8.2) : maximum 5 per cent of bracts and
maximum 2 per cent of other foreign matter.
Loss on drying (2.2.32) : maximum 12.0 per cent,
etermined on 1.000 g of the powdered drug (500) (2.9.12) by
drying in an oven at 105 °C for 2 h.
Total ash (2.4.16) : maximum 10.0 per cent.
ASSAY
Calculate the percentage content of flavonoids, expressed as
hyperoside.
Chemical constituents. Flowers contain
triterpenoids, flavonoids, carotenoids (up to 0.03%),
ether oils, ascorbic acid, phenol acids, sterols and
sesquiterpenoids lactones of bitter taste (calendine).
Triterpenoid saponins belong to derivatives of
oleanolic acid- calendulosides A and B.
Medicines. Infusion, tincture, ointment “Calendula”.
“Caleflon” (purified extract) used for treatment of
mouth ulcers, “Carofilen” has anti-inflammation
activity.
Application. Marigold is used for the
treatment of skin disorders and pain, also as
bactericide, antiseptic and anti-inflammatory
agent. The petals and pollen contain
triterpenoid esters (anti-inflammatory action)
and the carotenoids (antioxidants and the
source of yellow-orange coloration).
Calendulosides reduce cholesterol level in
blood.
Plant extracts are also widely used by cosmetics,
presumably due to presence of compounds
such as saponins, resins and essential oils.
