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Abstract

Earthen hemisphere is gifted with varieties of large number of medicinal herbs. Herbs are natural remedies for the disease with higher safety profile and efficacy. The country like India has got variety of climatic conditions and seasons favorable for growth of many species of plants. Amongst the large number of herbal drugs existing in India, very few have been studied systematically so far. The list of drugs is very meticulous and diversified hence extensive efforts are required for their correct recognition. Piper longum is a highly valuable drug and is one of the essential ingredients in the most of the compound preparations included in Ayurvedic literature. Further, the use of the plant as a bioavailability enhancer has immensely increased its importance in the field of Ayurveda. Hence, an attempt has been made to address the chemistry and pharmacology of the plant P. longum. Commonly the plant P. longum is known as long pepper, species of the genus Piper belonging to family piperaceae of the unique order piperales of the verticillate of dicotyledones.
Volume 5, Issue 1, November – December 2010; Article-010 ISSN 0976 – 044X
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Maitreyi Zaveri1*, Amit Khandhar3, Samir Patel4, Archita Patel2
1. Maitreyi Zaveri, Head and Assistant Professor, Dept. of Pharmacognosy, K.B. Institute of Pharmaceutical
Education and Research, Gandhinagar, India.
2. Archita Patel, Lecturer, Dept. of Pharmaceutical Chemistry, K.B. Institute of Pharmaceutical Education and
Research, Gandhinagar, India.
3. Amit Khandhar, Sr.Scientist, Analytical research laboratory, Zydus Cadila Ltd., Ahmedabad, India.
4. Samir Patel, Sr. Lecturer, Dept. of Pharmaceutical Chemistry, Ramanbhai Patel College of Pharmacy College,
Changa, India. *Corresponding author’s E-mail: khandharmaitreyi@yahoo.com
Received on: 08-09-2010; Finalized on: 03-11-2010.
ABSTRACT
Earthen hemisphere is gifted with varieties of large number of medicinal herbs. Herbs are natural remedies for the disease with
higher safety profile and efficacy. The country like India has got variety of climatic conditions and seasons favorable for growth of
many species of plants. Amongst the large number of herbal drugs existing in India, very few have been studied systematically so far.
The list of drugs is very meticulous and diversified hence extensive efforts are required for their correct recognition. Piper longum is
a highly valuable drug and is one of the essential ingredients in the most of the compound preparations included in Ayurvedic
literature. Further, the use of the plant as a bioavailability enhancer has immensely increased its importance in the field of
Ayurveda. Hence, an attempt has been made to address the chemistry and pharmacology of the plant P. longum. Commonly the
plant P. longum is known as long pepper, species of the genus Piper belonging to family piperaceae of the unique order piperales of
the verticillate of dicotyledones.
Keywords: Piper longum, Piperaceae, piperine.
INTRODUCTION
Plants have been the source of medicines since thousands
of years. Species of the genus Piper are among the
important medicinal plants used in various systems of
medicine1, 2. Piper longum L. (Piperaceae), commonly
known as “long pepper”, is widely distributed in the
tropical and subtropical regions of the world, throughout
the Indian subcontinent, Sri Lanka, Middle Eastern
countries and the Americas. It is said that the Roman
emperors valued it even more highly than black pepper
due to its high commercial and economical importance.
Synonyms: Piper latifolium Hunter, P. saramentosum
Wall. , Chavica roxburghii Miq, C.
Vernacular names: English: Long pepper, Hindi: Pippali,
Sanskrit: Pipali
Habitat: The native of plant is considered to be South Asia
and is found both wild as well as cultivated, throughout
the hotter parts of India from central to the north-eastern
Himalayas. The herb also grows wild in Malaysia,
Singapore, Bhutan, Myanmar and elsewhere1.
Ayurvedic properties:
Rasa: Katu (pungent)
Guna: Laghu (light), snigdha (unctuous), tikshna (sharp)
Veerya: Anushnashita (slight cold)
Vipaka: Madhur (sweet)
Dosha: Pacifies kapha and vata
Botanical description:
It is having slender, aromatic, perennial climber, with
woody roots and numerous wide ovate, cordate leaves.
The inflorescence is a cylindrical, pedunculate spike, the
female flower is up to 2.5 cm long and 4-5 mm in
diameter but the male flower is larger and slender. The
fruits are small, ovoid berries, shiny blackish green,
embedded in fleshy spikes3.
PHARMACOGNOSTICAL CHARACTERISTICS:
Flowering plant
Unripe fruit
CHEMISTRY AND PHARMACOLOGY OF PIPER LONGUM L.
Review Article
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Dried mature fruits
Plant of Piper longum L.
ROOT
Bisht4 had described complete pharmacognosy of the
root and stem of P.longum Winton and winton5 had
described the morphological and microscopical characters
of P. longum roots. Joshi6 had studied the structure and
development of the ovule and Embryo sac of P.
longum. The root in a transverse section showed thick
walled parenchyma, simple or compound starch grains,
lignified and striated stone cells, resinous cells in the
cortex, perivascular fibres in the phloem, and radical
strips of xylem which meet at the center. Pith was found
to be absent. The stem had a secretory cavity in the
center. The cortex showed starch grains as well as
resinous and some stone cells. The phloem was capped
by perivascular fibres and xylem arranged in V-shaped
groups7. The detailed microscopical study of root of Piper
longum is shown in Figure -1.
Figure 1: Piper longum L. root
FRUIT
Mehra and Puri8 described the fruiting spike of P. longum
as black, cylindrical, irregular, up to 2 to 5 cm long, and
compact. The fruits are one seeded with three-layered
pericarp. Winton and winton5 described the
morphological and microscopical characters of P. longum
fruits. Endocarp is wavy in outline, which is a
distinguishing character. Das Gupta and Dutta9 while
giving details of anatomy of the fruits, described the fruit
let of P. longum as thick-walled with heavy brown
contents in the outermost layer, mesocarp with thickened
cells, endocarp and seed coat fused to form a deep zone
with hyaline content in the outer layers, and orange-red
pigment.
STEM
Atal and Banga10 reported detail pharmacognosy of
the stem pieces of P.longum. The detailed
microscopical study of stem of Piper longum is shown in
Figure -2.
Figure 2: Piper longum L. stem
Traditional uses:
Parts used: Immature spikes, roots and seeds
Dried unripe fruits are used as an alternative to tonic.
Decoction of immature fruits and roots is used in chronic
bronchitis, cough and cold. Roots and fruits are also used
as anti-dote in snake biting and scorpion sting11. An equal
part of powdered seeds of Embelia ribes, fruit of P.
longum L. and borax powder has been used as an
Ayurvedic contraceptive12. P. longum L. has been used in
traditional remedies as well as in the Ayurvedic system of
medicine against various disorders13, 14.
Ethanoveterinary use: A decoction of the roots is given
for swellings of the joints of cattle in the north-western
Himalayan regions.
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PHYTOCHEMISTRY:
The Chemical Constituents of Pepper:
Piperine is the major and active constituent of long
pepper (Piper longum). The piperine content is 3-5% (on
dry weight basis) in P. longum.
Isolation and extraction of Piperine from Piper species:
Piperine can be isolated from the oleoresin of P. nigrum
or P. longum. The powdered fruits of the plant are
extracted with dichloromethane at room temperature
with stirring for 12 hours. The extract is filtered,
concentrated in vacuum, and then the residue is purified
on an alumina column. Pure piperine can also be obtained
by crystallization from ethanol, which may be required for
food and/or medicinal usages. Piperine is obtained
directly from the crude residue in lesser amounts by
extraction in alcohol, filtration and successive
crystallization.
Properties of piperine15:
*Chemical names:
a. 1- piperoyl piperidine
b. (E, E) 1-[5-(1, 3-Benzodioxol-5-yl)-1-oxo-2, 4-
pentadienyl] piperidine
*Molecular weight: 285.33
*Percentage composition: C= 71.55%, H=6.71%, N=4.91%
and O=16.82%.
Piperine
The fruits gave positive tests for the presence of volatile
oil, starch, protein and alkaloids, saponins, carbohydrates,
and amygdalin and negative test for tannins9. Sylvatine
and dieudesmin were present in the seeds of P. longum
16. Fatty acids of crushed seeds were reported to be
palmitic, hexadecenoic, stearic, linoleic, oleic, higher
saturated acids, arachidic, and behenic acids17.
Alkaloids and amides
The fruit of P. longum contains a large number of
alkaloids and related compounds, the most abundant of
which is piperine, together with methyl piperine,
iperonaline, piperettine, asarinine, pellitorine,
piperundecalidine, piperlongumine, piperlonguminine,
refractomide A, pregumidiene, brachystamide,
brachystamide-A, brachystine, pipercide, piperderidine,
longamide and tetrahydropiperine, terahydro
piperlongumine, dehydropipernonaline piperidine,
piperine, terahydropiperlongumine and trimethoxy
cinnamoyl-piperidine and piperlongumine have been
found in the root of P. longum 18-28 .
O
O
O
O
H
HO
O
(+)-Asarinine
Lignans
Sesamin, pulvuatilol, fargesin and others have been
isolated from the fruit of P. longum 19, 20, 22, 29.
Esters
The fruit of P. longum contains tridecyl-dihydro-p-
coumaarate,eicosanyl-(E)-p-coumarate and Z-12-
octandecenoic –glycerol-monoester19,20,22,28.
Volatile oil
The essential oil of the fruit P. longum is a complex
mixture, the three major components of which are
(excluding the volatile piperine) caryophyllene and
pentadecane (both about 17.8%) and bisaboline (11%).
Others include thujine, terpinoline, zingiberine, p-
cymene, p-methoxy acetophenone and dihydrocarveol19,
20, 22, 28, 3 0-32. Long pepper contains less essential oil than
its relatives (about 1%), which consists of sesquiterpene
hydrocarbons and ethers (bisabolene, β-caryophyllene, β-
caryophyllene oxide, each 10 to 20%; α-zingiberene, 5%),
and saturated aliphatic hydrocarbons such as 18%
pentadecane, 7% tridecane, 6% heptadecane33.
The volatile constituents and microbiological studies on
Kaempheria galanga, Hibiscus abelmoschus, and Piper
longum revealed presence of over 15 components which
were further identified by GC-MS of the volatile oil of
Piper longum. The variations in the piperine content with
maturity were also monitored. The P. longum and H.
abelmoschus seed oil had only antibacterial activities34. By
using a systematic bioassay guided fractionation method
pipataline, pellitorine, sesamin, brachystamide B and
guineensine active principles were isolated. A reversed-
phase high-performance liquid chromatography method
was developed to quantify these active principles in the
plant material 35. In the chromatogram of P. longum
fruits, retrofractamides B and D, and N-isobutyl-2E, 4E-
octadecadienamide can be detected. The HPLC-
chromatogram of P.longum showed a homogeneous
distribution of numerous peaks, with piperine and
pellitorine as the predominant compounds36. A simple
and convenient HPTLC method was developed for
standardization of the plant material using the two major
constituents, pellitorine and dihydropiperlonguminine, as
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markers at 260 nm37. The hexane extract of dried fruits of
P. longum on fractionation afforded a new alkamide,
isodihydropiperlonguminine and two phenyl propanoic
acid derivatives. The structures of these compounds were
established based on spectroscopic evidence and
synthesis38. Thymoquinol and 6-Hydroxydopamine were
also identified in Piper longum39.
MEDICINAL AND PHARMACOLOGICAL ACTIVITIES:
Insecticidal and acaricidal activity:
The essential oil of the fruits showed insecticidal and
insect-repellant activity 40.Toxicities of two piperidine
alkaloids, pipernonaline and piperoctadecalidine, isolated
from P. longum were determined against five species of
arthropod pests. Both of the alkaloids showed insecticidal
activity 41.
Antifungal activity:
The essential oil of the fruits showed fungicidal activity of
P. longum L. The fruit-derived materials was tested
towards six phytopathogenic fungi, Pyricularia oryzae,
Rhizoctonia solani, Botrytis cineria, Phytophthora
infestans, Puccinia recondita, and Erysiphe graminis using
a whole plant in vivo method 42-44. A piperidine alkaloid,
pipernonaline, was isolated from the hexane fraction of
P.longum showed a potent fungicidal activity against P.
recondita with 91% and 80% control values at the
concentration of 0.5 and 0.25 mg ml−1, respectively45.
Antiamoebic activity:
The anti-amoebic effects of crude methanol extract of
Piper longum fruit, Piper sarmentosum root and Quercus
infectoria nut gall against Entamoeba histolytica infecting
the caecum of mice were studied. The severity of caecal
wall ulceration was reduced in mice which received the
plant extract and metronidazole as compared to the
control animals46.The activities of n-hexane,
dichloromethane and methanol extracts from five anti-
diarrheic Thai medicinal plants, Acacia catechu
(Fabaceae) resin, Amaranthus spinosus (Amaranthaceae)
whole plant, Brucea javanica (Simaroubaceae) seed, P.
longum (Piperaceae) fruit and Quercus infectoria
(Fagaceae) nut gall were tested against the in vitro
growth of fresh isolates of the intestinal protozoan
parasite Blastocystis hominis. All extracts showed
inhibitory activity with reference to metronidazole47. Both
the root and fruit of P. longum possess antiamoebic
activity approximately to the same extent48. The ethanolic
extract, hexane fraction, n-butanol soluble fraction
exerted in vitro amoebicidal action at 1000
micrograms/mL and the chloroform fraction showed the
same at 500 micrograms/mL. The ethanolic extract and
piperine, a pure compound, from this plant material
cured 90% and 40% of rats with caecal amoebiasis
respectively 49, 46.
Antimicrobial activity:
Various extracts of P. longum were prepared and
evaluated against bacterial pathogens, such as S. albus, S.
typhi, P. aeruginosa, E. coli and B. megaterium and one
fungus, A. niger. Compared to streptomycin all the
extracts exhibited a good antibacterial activity50. The
isolated constituents and n-hexane extract were found to
show varying degree of antibacterial activity against all
the tested bacteria. However, the aqueous extract did not
show antibacterial activity against the tested bacteria51.
Effect on respiratory system:
Isolated piperine showed a central stimulant action in
frogs, mice, rats and dogs along with increased hypnotic
response in mice. It antagonized respiratory depression
induced by morphine or pentobarbitone in anesthetized
dogs52. A petroleum ether extract of the fruits
antagonized morphine-induced respiratory depression in
mice53. A comparative study conducted with piperine and
nalorphine, for effects against morphine-induced
respiratory depression and analgesia, revealed that both
reversed morphine-induced respiratory depression but,
unlike nalorphine, piperine did not antagonize morphine-
induced analgesia in rats54. Petroleum ether extract of P.
longum produced respiratory stimulation in smaller dose
but higher dose cause convulsion in laboratory animals.
This may be due to presence of some medullary stimulant
factors in the extract55, 56. The crude extract of P. longum
as well as piplartine, one of its alkaloids, suppressed the
cilliary movements of the esophagus of the frog, which
may be due to the suppression of cough reflex57.
Antiasthmatic activity:
An extract of the fruits in milk reduced passive cutaneous
anaphylaxis in rats and protected guinea pigs against
antigen-induced bronchospasm55, 56.
Effect on cardiovascular system:
Bioassay-guided isolation of chloroform extract of the
fruits of P. longum is using an in vitro DGAT inhibitory
assay, lead to isolation of a new alkamide together with
four known alkamides. Pharmacological inhibition of acyl
CoA: diacylglycerol acyl transferase by alkamides
emerged as a potential therapy for the treatment of
obesity and type 2 diabetes58. Guineensine, isolated from
chloroform extract inhibited ACAT activity in a dose-
dependent manner59. An amide namely
dehydropipernonaline having coronary vaso-relaxant
activity was isolated from the fruit of Piper longum 60.
Methanolic extract from dried fruits, roots and nutgalls of
Piper longum, Piper sarmentosum, Quercus infectoria
respectively, were examined for their spasmolytic
activities using isolated rat or guinea pig ileum and
compared with a reference anti-diarrheal drug such as
loperamide and an L-type calcium channel blocker such as
verapamil. All extracts and both drugs suppressed the
contraction in rat ileum showing the same potency for P.
longum and P. sarmentosum which was more than seen
for Q. infectoria61.
The effects of the several extracts of Piper longum on
rabbit platelet function were examined. The ethanol
extracts inhibited platelet aggregation induced by U46619
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in a concentration-dependent manner and by thrombin
weakly. It was concluded that P. longum contains a
constituent(s) that inhibits platelet aggregation as a non-
competitive thromboxane A2 receptor antagonist62. Four
acidamides, piperine, pipernonaline, piperoctadecalidine,
and piper longumine, isolated from the fruits of P. longum
showed dose-dependent inhibitory activities on washed
rabbit platelet aggregation induced by collagen,
arachidonic acid (AA), and platelet-activating factor (PAF),
except for that induced by thrombin. piperlongumine, in
particular, showed stronger inhibitory effects than other
acidamides to rabbit platelet aggregation induced by
collagen, AA and PAF63. A pilot study was carried out on
the breast development in female wistar rats using an
indigenous herbal preparation by topical application
containing Piper longum that showed an increase in the
appetite64.
Antidiabetic activity:
The antihyperglycemic and antilipidperoxidative effects of
ethanolic extract of Piper longum dried fruits in alloxan-
induced diabetic rats were studied 65. The blood glucose
level, carbohydrate metabolizing enzymes and the status
of lipid peroxidation and antioxidants were assayed using
specific colorimetric methods. Oral administration of
dried fruits has shown significant anti-hyperglycemic, anti-
lipidperoxidative and antioxidant effects in diabetic rats
comparable to that of the standard reference drug
glibenclamide66.
Hypochoesterolaemic activity:
Methyl piperine significantly inhibited the elevation of
total serum cholesterol, and the total cholesterol to HDL-
cholesterol ratio, in rats fed with a high cholesterol diet67.
The unsaponificable fraction of the oil of P. longum also
significantly decreased total serum cholesterol and
hepatic cholesterol in hypercholesterolaemic mice68.
Antioxidant activity:
A combination of spices (Piper nigrum, Piper longum and
Zingiber officinale), herbs (Cyperus rotundus and
Plumbago zeylanica) and salts make up Amrita Bindu
were tested for anti-oxidant activity. The analysis
revealed the antioxidant potential of the ingredients in
the following order: Piper nigrum > Piper
longum > Cyperus rotundus > Plumbago zeylanca >
Zingiber officinale69.
Analgesic activity:
P. longum root for opioid type analgesia using rat tail-flick
method and for NSAID type analgesia using acetic-acid
writhing method by using pentazocine and ibuprofen as
drug controls. An aqueous suspension of P. longum root
powder was given orally to mice and rat. The study
accomplished that P. longum root had weak opioid but
potent NSAID type of analgesic activity70.
Anti-inflammatory activity:
The fruit decoction showed anti-inflammatory activity
against carrageenin induced rat paw edema71.
Immunomodulatory activity:
The immunoregulatory potential of P. longum and
piperinic acid, one of its active constituent, in Balb/C mice
(in vivo) and human PBMCs (in vitro) models showed a
dose dependent decrease of lymphocytes (CD4+ and
CD8+ T cells) and cytokine levels in sensitized Balb/C mice
with a marked inhibition72. Alcoholic extract of the fruits
of P. longum and its component piperine was studied for
their immunomodulatory and antitumor activity.
Alcoholic extract of the fruits and piperine were found to
be cytotoxic73. An aqueous extract of P. longum fruit
powder showed 100% giardicidal activity13. P. longum was
found to offer protection against externally induced
stress. A famous Ayurvedic preparation containing long
pepper in pippli rasyana was tested in mice infected with
Giardia lamblia and found to produce significant
activation of macrophages, as shown by an increased
MMI and phagocytic activity74.
Anti-cancer activity:
Piper longum is reported to exhibit significant anti-
tubercular activity 75, 76. The effect of piperine on the
inhibition of lung metastasis induced by B16F-10
melanoma cells was studied in C57BL/6 mice.
Simultaneous administration of the compound with
tumor induction produced a significant reduction (95.2%)
in tumor nodule formation along with reduced lung
collagen hydroxyproline, uronic acid and hexosamine
content in the piperine-treated animals. Piperine, an
alkaloid present in plants such as P. nigrum and P. longum
showed significant anti-metastasis activity77. Piperine has
chemopreventive effects when administered orally on
lung cancer bearing animals78. Piperlonguminine showed
an inhibitory effect on α-MSH-induced tyrosinase
synthesis79. It was found that oral administration of
ethanolic extract protected the cell surface and
maintained the structural integrity of the cell membranes
during DMBA induced hamster buccal pouch
carcinogenesis80. The two active principles, ethyl 3', 4’, 5’-
trimethoxycinnamate and piperine were isolated and
characterized from the combined hexane and chloroform
extracts of Piper longum. The extracts significantly
blocked the adhesion of neutrophils to endothelium in a
time- and concentration-dependent manner81. Piplartine
and piperine alkaloidal amides were isolated from Piper.
It showed cytotoxic activity towards several tumor cell
lines82. The study clearly demonstrated that piperine has
the anti-oxidative, anti-apoptotic, and restorative ability
against cell proliferative mutagenic response and
phenotypic alterations by piperine, suggesting its
therapeutic usefulness in immunocompromised
conditions83.
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Anti-depressant activity:
Treatment with piperine (6.25–25 µM) for 72 h reversed
the (corticosterone) CORT-induced reduction of BDNF
mRNA expression in cultured hippocampal neurons84. A
bioassay-guided isolation of the ethanol extract from the
fruits of P. longum yielded a known piperidine alkaloid,
piperine having potent antidepressant-like properties
which are mediated in part through the inhibition of MAO
activity, and therefore represent a promising
pharmacotherapeutic candidate as an antidepressant
agent85.
Antiulcer activity:
The water decoction of ginger making up one of the
constituents of Mahakasyaya drugs along with water
decoction of P. longum and colloidal solution of Ferula
asafoetida has been reported to protect against CRS-,
ASP- and PL- induced gastric ulcers in rats86. Piperine, an
alkaloid of long peppers, inhibited gastric emptying (GE)
of solids/liquids in rats and gastrointestinal transit (GT) in
mice in a dose and time dependent manner. GE inhibitory
activity of piperine is independent of gastric acid and
pepsin secretion87.
Effect on Reproductive system:
The benzene extract of P. longum in combination with
methanol extract of Embelia ribes berries lead to
inhibition of pregnancy in 80% of animals88. The exposure
to pippaliyadi does not have any adverse effect on the
postnatal development and reproductive performance of
the F1 progeny89. Piperine showed marked increase in
serum gonadotropins and a decrease in intratesticular
testosterone concentration, despite normal serum
testosterone titres90. The crude extract of Piper longum
and its hexane fraction exhibited 100 and 86% efficacy
respectively in female rats91. The reproductive toxicity of
piperine was studied in Swiss albino mice. Piperine
increased the period of the diestrous phase, which
seemed to result in decreased mating performance and
fertility. The results showed that piperine interferes with
several crucial reproductive events in a mammalian
model92. An ayurvedic contraceptive — pippaliyadi vati,
containing equal parts of powdered seeds or fruit berries
of Embelia ribes, fruit of P. longum and borax powder was
fed orally to two groups of pregnant rats and humans to
study embryotoxicity and teratogenicity. The fetuses of
mothers fed with pippaliyadi had low birth weights and
were smaller in length with less weight gained during
gestation93.
Bioavailability enhancement:
Piperine was found to enhance the bioavailability of
structurally and therapeutically diverse drugs, possibly by
modulating membrane dynamics due to its easy
partitioning and increase in permeability of other drugs
such as vasicine, indomethacin, diclofenac sodium
etc.94,95. It was suggested that piperine might be inducing
alterations in membrane dynamics and permeation
characteristics, along with induction in the synthesis of
proteins associated with cytoskeletal function, resulting in
an increase in the small intestine absorptive surface, thus
assisting efficient permeation through the epithelial
barrier96, 97. The study showed that piperine enhances the
serum concentration, extent of absorption and
bioavailability of curcumin in both rats and humans with
no adverse effects98.
Hepatoprotective activity:
The fruit extract improved the regeneration process by
restricting fibrosis, but offered no protection against
acute damage or against cirrhotic changes in rodents99.
Treatment with the ethanol extract of P. longum inhibits
liver fibrosis induced by carbon tetrachloride (CCl4)100.
Piperine exerted a significant protection against tert-butyl
hydroperoxide and carbon tetrachloride hepatotoxicity by
reducing both in vitro and in vivo lipid peroxidation,
enzymatic leakage of GPT and AP, and by preventing the
depletion of GSH and total thiols in the intoxicated mice.
Piperine showed lower hepato-protective potency than
silymarin101.
Safety profile:
Since, it is widely used in cooking and traditional
medicine, it is generally assumed to be safe in moderate
doses. However, as the fruits are reported to have
contraceptive activity in experimental models its use
during pregnancy and lactation should be avoided. In the
evaluation of antifertility activity, long pepper at a dose of
1gm/kg body weight was found to be an effective
contraceptive agent without toxic or teratogenic
effects102. Acute and chronic oral toxicity studies on the
ethanolic extracts of common spices Cinnamomum
zeylanicum bark and P.longum fruits were carried out in
mice showed no significant acute or chronic mortality
compared to the control during this study103. The radio
protective property of an ethanolic extract of P. longum
fruits reduced the elevated levels of glutathione pyruvate
transaminase (GPT), alkaline phosphatase (ALP), and lipid
peroxidation (LPO) in liver and serum of radiation treated
mice. The extract administration also increased the
reduced glutathione (GSH) production to offer the
radioprotection104. Piperine might interfere with
enzymatic drug biotrasformations resulting in the
inhibition of hepatic aryl hydrocarbon hydroxylase (AHH)
and UDP-glucuronyltransferase and altered the
pharmacokinetic parameters of barbiturates and
phenytoin103, 105,106.
CONCLUSION
Here, an attempt was made to address chemistry and
pharmacology of the P. longum. Therefore, the review of
plant Piper longum revealed that it has got a variety of
pharmacologically and medicinally significant
constituents, which are being utilized in the field of
Ayurveda. It is a plant of high commercial and economical
importance and its use as a bioavailability enhancer can
be explored in various formulations. The above review
provides information of its phytopharmacolgy, which may
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be useful for further study of Ayurvedic drugs of folk
medicinal practice of present era.
REFERENCES
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************
... The male flower is larger and slender whereas the female flower is up to 2.5 cm long and 4-5 mm in diameter. The fruits, embedded in fleshy spikes, are small, ovoid berries, and shiny blackish-green in appearance (Zaveri et al., 2010). Fruits are globose with pungent taste and aromatic odor. ...
... It is known as "pipali" in Sanskrit. According to Ayurvedic medicine, it has properties as follows: rasa-katu, i.e., pungent; veerya-Anushnashita, i.e., slightly cold; vipaka-Madhur, i.e., sweet; gunasnigdha, i.e., unctuous; Laghu, i.e., light; tikshna, i.e., sharp; and dosha, i.e., calms vata and kapha (Zaveri et al., 2010). Stems and roots of long pepper are used as medicine in Ayurveda and Arabian medicine. ...
... Antigen-induced bronchospasm, which can be the cause of asthma was reduced by the usage of extracts of long pepper fruit administered with milk to guinea pigs (Zaveri et al., 2010). Root 474324.indb ...
Chapter
Medicinal plants have been used for the treatment of many diseases since ancient time. In traditional medicine two plants that are long pepper or pipli (Piper longum) and giloy or heart-leaved moonseed (Tinospora cordifolia) have huge importance. They have properties which give strength and protection to various systems of the body. These plants contain various phytochemicals which act against various ailments. Long pepper or pipli contains chemical compounds such as piperine, alkaloids, saponins, starch, protein, volatile oils, amygdalin and many more. These compounds show various properties such as anti-diabetic, anti-hyperlipidemic, hepatoprotective, neuroprotective, cardioprotective, anti-bacterial, aphrodisiac. It also shows effects against diseases like gonorrhoea, paralysis of the tongue, diarrhoea, cholera, chronic bronchitis, asthma, constipation etc. Giloy or heart-leaved moonseed contains phytochemicals such as steroids, sesquiterpenoids, tinocordifolin, jatrorrhizine, tinosporic acid, alkaloids etc. Giloy shows activities like antioxidant activity, antimicrobial activity, antibacterial activity, antifungal activity, anti-diabetic activity, antistress activity, hypolipidemic effect, hepatic disorder, anticancer, anti-HIV potential, antiosteoporotic effects, antitoxic effects, wound healing, anticomplementary activity, and immunomodulating activity, systemic infection and Parkinson’s disease etc. For the treatment of these and many more diseases these herbs can be used. This chapter discusses traditional knowledge, bioactive compounds and medicinal properties of P. longum and T. cordifolia.
... This study provided some evidences that PLA protected dopaminergic cells from MPTP neurotoxicity by ameliorating behavioral abnormalities, reducing 258 loss of TH-positive neurons in substantia nigra, increasing levels of DA and its associated metabolites, and enhancing antioxidative defence system by increasing enzymes activity, e.g., GSH and SOD activity, resulted into decreased MDA levels. The phytochemicals of P. longum, e.g., alkaloids possess protective effects in PD models including MPTP, 6-OHDA rat/mouse models (Zaveri et al., 2010;Subburaman et al., 2010;Liu et al., 2011). It was reported (Pal and Choudhary, 2012) the effect of piperine on 3T3-L1 cell lines by inhibiting the expression of PPAR-, thus it can be used in treatment of various diseases. ...
... Piperine have the ability to inhibit intestinal and hepatic hydroxylation and glucuronidation of aryl-hydrocarbon, thus preventing the degradation of drugs in the gut and improve their bioavailability. For example, co-administration of piperine enhances the bioavailability of curcumin in vivo by 2000% in humans and 154% in rats (Zaveri et al., 2010). Studies have shown that curuminderivatized with piperic acid (obtained by the base hydrolysis of piperine) forming di-piperoylcurcu-mindiester, showed improved protection against oxidative and nitrosative stress in vitro and against toxin induced cell death in dopaminergic cells (Harish et al., 2010;Mythri et al., 2011). ...
Article
Parkinson's disease (PD) is second most common neurodegenerative disorder, which is a progressive motor disease that affects 10 million people worldwide and around 5.5 million Indian. The hallmark neuropathology in PD are damage to dopaminergic neurons located in the pars compacta of the substantia nigra (SN) that project to the striatum and alpha synuclein containing inclusion bodies in the surviving neurons, resulting in motor impairments, e.g., tremors, bradykinesia (slow movement), poor balance, rigidity and difficulty in walking, as well as non-motor impairments including constipation, autonomic, psychiatric as well as cognitive impairments. The only pharmacology therapy for PD is levodopa but chronic use of this medicine has many side effects. Hence, these impairments are pressing issues that need to be addressed. This review article attempts to describe the usage of Indian traditional medicines to treat PD. In India, the references to the curative properties of dietary spices in the Rigveda and Atharvaveda arguably seem to be the earliest records of the use of herbs in medicine.
... This study provided some evidences that PLA protected dopaminergic cells from MPTP neurotoxicity by ameliorating behavioral abnormalities, reducing 258 loss of TH-positive neurons in substantia nigra, increasing levels of DA and its associated metabolites, and enhancing antioxidative defence system by increasing enzymes activity, e.g., GSH and SOD activity, resulted into decreased MDA levels. The phytochemicals of P. longum, e.g., alkaloids possess protective effects in PD models including MPTP, 6-OHDA rat/mouse models (Zaveri et al., 2010;Subburaman et al., 2010;Liu et al., 2011). It was reported (Pal and Choudhary, 2012) the effect of piperine on 3T3-L1 cell lines by inhibiting the expression of PPAR-, thus it can be used in treatment of various diseases. ...
... Piperine have the ability to inhibit intestinal and hepatic hydroxylation and glucuronidation of aryl-hydrocarbon, thus preventing the degradation of drugs in the gut and improve their bioavailability. For example, co-administration of piperine enhances the bioavailability of curcumin in vivo by 2000% in humans and 154% in rats (Zaveri et al., 2010). Studies have shown that curuminderivatized with piperic acid (obtained by the base hydrolysis of piperine) forming di-piperoylcurcu-mindiester, showed improved protection against oxidative and nitrosative stress in vitro and against toxin induced cell death in dopaminergic cells (Harish et al., 2010;Mythri et al., 2011). ...
... Piper longum (long pepper), of the Piperaceae family, is used as a spice and as a medicine in Asia, particularly in South Asia. 15 Various studies have reported the potential of the plant parts of this species, especially the fruit, for pharmaceutical use due to their pharmacological activities such as antioxidant, antimicrobial, and anti-inflammatory activities, among others. 16,17 The anatomy of the fruit consists of pericarp and multiple seeds inside the fruit spike, and the lining of the seeds is surrounded by the hardened endocarp fused with the seed coat. ...
... These herbal formulations are the property or knowledge of the old ages of every home. Herbal drugs also have a huge holistic believes like Holi tulsi, Ficus tree etc. 1 Digestive tablets have become a popular demanding material now a days. Ayurveda shows that herbal digestive tablets can contain pomegranate seeds, cumin seeds, black pepper, dalchini, cardamom, asafoetida, salt, black pepper, sipernate, chhoti pippali, rock salt, ginger, black salt, and other excipients. ...
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Herbal digestive tablets are meant for treating indigestion problems. The indigestion problem is one of the major problems of all (the) ages of human beings. As trends for eating fast foods is increasing, simultaneously the improper digestion also tends to increase. There are a number of digestive tablets in the market but in attempt to improve their taste the actual motto behind their use is masked. To combat the indigestion problems, in the present study an attempt has been made to formulate, develop and evaluate herbal digestive tablets. The formula of the digestive tablet has been decided after deep review of Ayurvedic formulary of India. The ingredients of this formulation have been procured from authentic sources. The wet granulation method was used to prepare the granules for punching the tablets. After preparation, the herbal digestive tablets were subjected to various pharmaceutical evaluations and quality control evaluations as per the guidelines from World Health Organization (WHO). The formulation was also subjected to antioxidant screening using Phosphomolybdenum method. The digestive tablets are obtained as light brown-colored round tablets with pleasant odour and spicy taste with an average size of 8mm and smooth edges. Maximum extractive value was observed as 34% in methanol with a total ash value of 10.16%. Other parameters reported as bitterness value- 0.69 units, volatile oil content-8%, loss on drying- 12.3%, swelling and foaming index of 0.27 and less than 100 respectively. The tablets showed a total antioxidant potential of 0.51mg/mg as Ascorbic acid equivalent. Tablets also pass various pharmaceutical evaluation parameters like hardness, friability, weight variation, and disintegration test. Herbal digestive tablets have very excellent taste due to less bitter drugs. The tablet formula can be applied to prepare large scale production of digestive tablets.
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The gastrointestinal tract (GIT), one of the essential organs of the human body is susceptible to various diseases. GI disorders such as constipation, diarrhea, GI reflux disease, gastric ulceration, Crohn’s disease, irritable bowel syndrome (IBS), also in addition to some other functional disorders, have become prevalent in a large part of the world population. Majority of the world’s population relies on herbal medicines nowadays for the management and treatment of GI diseases. However, the use of herbal medicines in various manifestations are traditionally derived, and further controlled trials suggest certain benefits of using ginger in nausea and vomiting, extract of licorice in peptic ulcers, Chinese herbal medicine in IBS, opium derivatives in diarrhea, and senna and ispaghula in constipation. The presence of various bioactive components in herbal preparations makes them suitable for potential therapeutic effects in GIT problems. In this chapter, we have discussed a number of single herbal formulations or herbal combinations for the treatment of different types of GIT ailments.
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Long pepper (Piper longum Linn.) is widely used as a medicinal substance in traditional Ayurvedic medicine. Its major alkaloid piperine is the main active constituent with various therapeutic activities and has low solubility in water. In this study, a soluble new derivative of a piperine alkaloid, named N-leucinylpiperamide was synthesized. The animal experiment showed that N-leucinylpiperamide has more hypolipidemic effects than commercially available simvastatin and piperine in modulating serum lipids in Wistar male rats. At the amount of 10 mg/kg bw, it significantly reduced TC (-52.4%), TG (-61.7%), and LDL-C (-27.8%), respectively, and increased HDL-C (+147.4%) in the serum of the high-lipid model group. Furthermore, the synthesized N-leucinylpiperamide had no noticeable cytotoxicity against HepG2 cell line in vitro. Thus, our study shows that N-leucinylpiperamide has an ability to improve serum lipid profile in hyperlipidemic model rats and could be a valuable promising agent for the preventing hyperlipidemia.
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The SARS-CoV-2 was identified in December 2019 and spread quickly around the globe. Around 218 countries with 61,468,916 cases have been diagnosed as of November 27, 2020. The epidemic quarantine and symptomatic care plan control are the first step of the treatment in the absence of medicines and vaccines. The need for treatments/therapeutics is in high demand. Pharma companies are working around the clock to develop these treatments/therapeutics. Several traditional medicines are also followed as the treatments/therapeutics across the globe. In India, the traditional medicine system ranks to be one of the topmost promising treatments/therapeutics for ages. In COVID-19, the medicinal products for treatment, prophylaxis, and convalescence were listed based on the Siddha Medicine advisory provided by the Ministry of AYUSH. These drugs are recommended for the treatment and prophylaxis of symptoms. In reality, however, these medications have been in vogue for infectious diseases like Dengue and Chikungunya for the past two decades. In parallel, the in silico studies are positively helping in the drug discovery and unravel the drug mechanisms. The computational protein modeling techniques also play a significant role in identifying all the reference genome's proteins. This chapter discussed Siddha and Quarantine's traditional insight in viral diseases, Virus-based drug repurposing for coronaviruses, and various treatment, including significant drug repurposing and BSAA combination therapy. We have also used computational modeling techniques to identify and model the individual protein structures from the whole genome of SARS CoV-2. Finally, this chapter will explain the steps taken to develop and repurpose Kabasura Kudineer as a drug to inhibit the COVID-19 pandemic.
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Background: Currently, the Coronavirus disease (COVID-19) pandemic is posing a serious threat to global health. Although approved COVID-19 vaccines have been claimed to provide a high degree of protection against getting seriously ill and dying from the disease, they are not in the approach of all people especially those from the least developed countries like Nepal. Desperation within people has led to increased use of medicinal plants to cure the miscellaneous symptoms of COVID-19 and to prevent infection without proper knowledge of their phytochemical and pharmacological properties. Methods: Based on the online and interpersonal inquiries with 59 COVID-19 survivors and 111 inhabitants of Buddhabhumi Municipality, Kapilvastu, Nepal, the ethnomedicinal data were collected and summarized using descriptive statistics like frequency, percentage tables, and graphs. For each medicinal plant species, the frequency of citation (FC) and relative frequency of citation (RFC) were calculated along with a radar chart for the top 15 cited species with their phytochemical and pharmacological properties. Results: This study documented 41 species of medicinal plants belonging to 24 different families and 37 genera were used. Herbs were predominant among other life-forms and leaves were highly used among other plant parts. Turmeric (Curcuma longa, with the highest frequency of citation of 0.80) was the most frequently used species. Most of the respondents (44%) obtained medicinal plants from their home gardens. Family, friends, and neighbors were the primary sources of information the respondents followed. Interestingly, all of the 15 most frequently cited medicinal plants were reported to have both antiviral and anti-inflammatory properties and 14 of them were proclaimed to be immunomodulatory. Conclusion: Therefore, we conclude from the survey and available literatures that medicinal plants play a significant role against viral infections.
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Studies were carried out on the chemical composition of long pepper and the results showed that long pepper contained about 1% volatile oil, 1.25% piperine and 40% starch. As compared to black pepper, long pepper was poor in essential oil and piperine and the volatile oil was dextrorotatory, while that of black pepper was levorotatory. The GC-MS analysis of the essential oil showed the presence of 48 components, out of which 44 were identified for the first time. The three major components of the oil, identified were β-caryophyllene (17%), pentadecane (17.8%) and p-bisabolene (11.16%).