medicinal properties of aconitum spicatum(bikh) with its chemical constituent.

1. Pokhara University
School of Health and Allied Sciences
Shailendra Shah
Department of pharmaceutical science
Pokhara University
Aconitum spicatum(Bikh)

2. Pokhara University
School of Health and Allied Sciences
Topics under discussion
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• Nomeclauture
• Biological source
• Habitat
• Cultivation and collection
• Microscopic and macroscopic examination
• Chemical constituent
• Pharmacological action
• Pharmacopoeial standard
• References
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3. Pokhara University
School of Health and Allied Sciences
Introduction
• The genus Aconitum, belonging to the family Rannunculaceae,
is widely distributed in alpine and subalpine regions, it is
distributed from the west to east Nepal and from temperate
to alpine zones (1800-4200m elevation). It is commonly known
as bikh in Nepal and monk’s hood or aconite in english.
• These are the herbaceous perennial plants growing in
moisture retentive but well draining soils of mountain
meadows. Aconite is well known to the ancients as a powerful
poison, but was the first employed as a medicine by Baron
Storck, of Vienna, whose experiments were published in the
year 1762 (Harvey et al. 1898).
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School of Health and Allied Sciences
Nomeclature
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• Kingdom: Plantae
• Division: Tracheophyta
• Class: Magnoliopsida
• Order: Ranuculales
• Family: Ranunculaceae
• Subfamilia: Ranunculodeae
• Genus: Aconitum
• Species: Aconitum spicatum
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Biological source
Bikh is the biological source for its products like root extract,
tubers extract.
Habitat
It is a perenial herb of about 2m in height found in Himalayan
region. In Nepal , it is distributed throughout the country up to
an altitude of 1800-4200m.
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School of Health and Allied Sciences
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Cultivation and collection
• Cultivation : It is propagated by seeds and the daughter
root. Best grown in cool, moist, fertile soil under partial
shade. It can also tolerate in moist soils and full sun.
• Collection: It is collected when flower begins to expand, the
alkaloid content in the roots and tubers are found to be the
highest concentration at the flowering seasons.
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• Drying: Roots and tubers are sliced longitudinally or
transversely to facilitate drying. The drying period ranges from
10 days to 3 weeks.
• Storage: Dry containers do not expose to light. The active
constituents may be decomposed due to action of light.
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Macroscopic identification
• Root: tuberous, paired, conical, 4 to 10 cm long and 1-2 cm in
diameter at the crown, root tubers are the largest in the
genius aconitum, externally dark brown or grayish-brown,
smooth or longitudinally wrinkled.
• Stem: erect, smooth below, finely hairy above, branched in
upper part.
• Leaves: alternate, deeply lobed, 6-12cm across, lobes, ovate
and toothed, soft and hairy.
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• Inflorescence: raceme, terminal spike, 15-40cm long.
• Flowers: purple to greenish , 2-2.5cm in size.
• Fruits: follicle, wrinkled and pubescent
• Seeds: black with pitted test
• Flowering: July to August
• Medicinally important plants: roots
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Microscopic examination
• Chromosomes number:2n=32
• T.S of tuber:
 Transverse section of mature tuber shoes single layered
epidermis consisting of light tubular compressed cells with
cork rupturing.
 Cortex consists of 8-15 rows of round, thin walled
parenchymatous cell containing both simple and compound.
 Starch grains bundle arranged in ring with characteristics of
more or less star shaped cambium ring.
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• Pith composed of large, starch-bearing parenchyma cells as in
cortex and central position of the tuber is fissured . In young
roots, the vascular bundles are nearer the center than in old
ones
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• Powdered microscopy: The powdered drug is grayish brown
with numerous simple and compound starch grain of
spherical or plano-convex shape. The size is 0.003-0.0015mm.
Few cork fragments and parenchymous cells are present.
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Organoleptic properties
• Color: Blackish-brown, sometimes whitish
• Odour: Odourless or feeble earthy odor
• Taste: Slightly bitter taste, followed by peculiar sense of
numbness and tingling sensation in the lips, cheeks and
tongue.
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Chemical constituents
• Important chemical constituents are Bikhaconitine.
• Other alkaloids found are aconitine, aconine and
pseudoconitine, spicatine A11, spicatine B11.
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Phytoconstituents reported in Aconitum spicatum
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Secondary metabolites Phyto-constituents
Alkaloids Benzoyl mesaconine,
mesaconitine, hypaconitine,
heteratisine, heterophyllisine,
heterophylline,
heterophyllidine, isotisine,
hetidine, hetsinone
Flavonoids Quercetin 7-0-beta
glucopyranosyl, alpha
rhamnopyranoside-3-0-beta-
glucopyranoside
Free fatty acids Linoleic acid, palmitic acid and
oleic acid
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Ethno medicinal uses
• Generally used for poisons.
• Paste is useful in neuralgia, muscular rheumatism, nasal
catarrh and tonsilities.
• Tubers are used to poison arrows and are extensively used
medicinally.
• It is used in congestion and swelling attended with severe
itching and burning sensation in reaction to cold.
• Tubers are diaphoretic, diuretic, anti pyretic, anodyne, anti-
diabetic and used in cough, asthma and snakebites.
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Pharmacological action
1. Cardiac effect:The initial research focused on the
cardiovascular (arrhythmogenic) toxicity of Aconitum
alkaloids and especially AC.The marked cardiac activity of
diterpene alkaloids is mainly due to their effect on the
voltage-gated Na+ channels.(source: Dzhakhangiror FN et al.
(1997) Depending on their mechanism of action, the
Aconitum alkaloids action on cardiac function can be
subdivided into arrhythmogenic and anti-arrhythmic
alkaloids.
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• Alkaloids with arrhythmogenic activity
Arrhythmogenic alkaloids induce their effect by delaying the
final repolarization phase of action potential in cardiac cells,
which initiates premature or triggered excitations. The final
inexcitability of the cells may cause heart arrest.(source:Ameri
A.(1998)
• Alkaloids with anti-arrhythmic activity
Anti-arrhythmic compounds are based on a variety of
diterpene skeletons. Regarding the mechanism of action,
inhibition of the voltage-dependent Na+ channels and blocking
of the delayed rectifier K+ current are the key compund.
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2 . Effects on the nervous system:
Recent experimental findings indicate that some diterpene
alkaloids act as selective antagonists on the
bungarotoxinsensitive nicotinic acetylcholine receptors
(nAChR) or inhibit the delayed rectifier K+ current. Several
diterpene alkaloids also have either anti-epileptic or
epileptiform effects, which are also related to the effect on
the Na+ channels. The analgesic and anti-epileptiform action
of the Aconitum alkaloids have been the most studied.
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Analgesic effect:
• Alkaloids that activate voltage-dependent Na+ channels
are antinociceptive and have the potential to depolarize
neurons permanently and hence block the neuronal
conduction.[63] Na+ channel blockers possess antinociceptive
activity by inhibiting neuronal activity.( source: Polyakov NE et
al.(2005)
• Although certain lipophilic alkaloids can integrate into the
cellular membrane, the antinociceptive effect is likely to be a
result of interaction with channel proteins because the use-
dependent inhibition of evoked potentials was observed in rat
hippocampal slices.
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Anti-epileptiform effect
• The anti-epileptiform activity of diterpene alkaloids is in line
with the blockade of the Na+ channels because Na+ channels
are known to be involved in the genesis of abnormal activity in
epilepsy.
• Na+ channel-blocking compounds (e.g. lappaconitine) inhibit
experimentally induced epileptiform activity frequency
dependently by sparing the normal neuronal activity.(source:
Ameri A(1998)
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• Antimicrobial activity
The antiprotozoal activity of 43 C-19 diterpene alkaloids
were tested on the extracellular and intracellular stages of
the parasite. From among the tested compounds, three
atisine-type Aconitum alkaloids inhibited the growth of L.
infantum similarly to the reference drug,without being toxic
to the host cells.(source: Gonzalez P et .al 2005) Two
atisinetype C-20 diterpene alkaloids inhibited the growth of
T. cruzi epimastigotes with activity levels similar to that of
the reference drug, with no toxicity to the host cells.
(source:Gonzalez Pp et al. (2006)
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Pharmacopeial standards
• Foreign matter: Not more than2%
• Total moisture content: 18.26%
• Total ash: Not more than 4%
• Acid insoluble ash: Not more than 1%
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Commercial value
• Bikh has high commercial value. Its every part has commercial
importance as each part has medicinal as well as domestic
use. The total value of medicinal products traded through
Hille and Basantpur in the 1991/92 trading season was
estimated to be NPR 18 180 000 (USD 350 000).Its root and
tubers cost Rs.55/kg. Nowadays pharmaceutical companies
use bikh as the raw material for production of the drugs.
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Formulations
• Aconite is available as a homeopathic remedy or in dried bulk
form. Some of formulations are Tribhuwan kriti ras, Shree
Mrityunjaya ras, Ananda Bhairab ras.
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• Side effects: The therapeutic dose is closed to lethal dose.
So, a very small dose causes fetal cardiac depression. The
overexposure cause Nausea, Vomiting, diarrhea, ataxia,
vertigo, dyspnoea, hypothermia, convulsion etc. Direct
contact may cause numbeness and tingling sensation.
• Toxicity: Aconite tubers are deadly poisonous although used
for various medicinal purposes. It is detoxified by the boiling
with the extract of Terminlia chebula. Foilage may irritate
sensitive skin.
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References
• Nyirimigabo E, XU V al (2014) , A review of phytochemistry,
pharmacology, toxicology studies of Aconitum, Journal of
pharmacy and pharmacology ,page(1-19)
• Shyaula S(2011), Phytochemicals, traditional use and
processing of Aconitum species in Nepal, Nepal Journal of
science and technology, page(171-178)
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