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7.5 Different Ancient Ayurvedic Formulations
Prepared from Black Pepper
The antiasthmatic activity is reported to be enhanced by the combination of
Adhatoda vasica with Pippli (P. longum). As a part of Ayurveda, Bose first
introduced a concept known as ‘‘yogavahi’’ in 1929. This concept increases
the efficacy, tissue distribution, and bioavailability of drugs. Piperine is ex-
tensively used to improve the bioavailability of xenobiotic agen ts in the
treatment of the most serious of diseases.
4
Table 7.1 shows various Ayur-
vedic formulations based on P. nigrum and their therapeutic uses. Some
Ayurvedic formulations are mentioned, along with their composition. The
traditional use of Trikatu Churna, a mixture of black pepper, long black
pepper and ginger, is to treat Kapha, Vata and Pitta as well as a number of
other disorders. The bioavailability is enhanced with the use of vasicine and
spartine.
13
Pippalye
¨
dye
¨
sava is another Ayurvedic formulation containing
piper chaba, long pepper and black pepper and used to treat piles, urt icaria,
anaemia, and malabsorption syndrome.
14
Jawa rishai and thurushi contain
the ingredients black pepper, ginger, vidanga, peppermint, and lemon juice
and are used as stimulants, carminative expectorants, and for the treatment
of genitourinary diseases and gonorrhoea, and as a diuretic.
15
Furthermore,
Kanakasava contains the composition Pippali (Indian long pepper;
P. longum), dried ginger powder (ginger rhizome; Z. officinale), Mulethi
(liquorice), Vasaka (Malabar nut), thornapples (purified datura metal; all
parts) and is used as a bronchodilator, expectorant, analgesic, anti-
spasmodic, sedative, cardiac stimulant, soporific (sleep-inducing) and di-
gestive aid.
16
The Panchakola Churna and Vardhamana Pippali Rasayana
contain ingredients such as Indian long pepper (P. longum), Chavak (Piper
retrofractum), Ceylon (Plumbago zeylanica), dried ginger (Z. officinale), honey
and ghee (clarified butter) and are used in the treatment of bronchitis,
pulmonary tuberculosis, asthma, piles, anaemia, chronic rhinitis, intermit-
tent fever, splenic disorders, obstinate abdominal diseases, and rheumatoid
arthritis.
17
Avipattikara Churna contains a composition of P. nigrum, Z. of-
ficinale, Indian gooseberry (Emblica officinalis), Bhenda (Terminalia belerica),
Figure 7.3 Dried unripe black pepper fruit.
152 Chapter 7
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Table 7.1 Ayurvedic formulation, composition and its therapeutic uses.
Ayurvedic
formulation Composition Therapeutic uses Ref.
Trikatu Churna
(major decoction)
Black pepper (P. nigrum), long pepper (P. longum),
Ginger (Zingiber officinale Rosc.)
Traditionally used for the restoration of Kapha,
Vata and Pitta. In various other types of fevers,
disorders related to abdomen and gastrointestinal
tract, pyrexia, dysentery, bronchitis, asthma and
sleep disorders. As a bioavailability enhancer for
Vasicine, Sparteine
13
Pippalye
¨
dye
¨
sava Long pepper (P. longum), black pepper (P. nigrum),
Piper chaba
Malabsorption syndrome, abdominal lumps,
emaciation, phthisis, piles, urticaria, anaemia
14
Jawa rishai Thurushi Black pepper (P. nigrum), ginger (Zingiber officinale),
Embilia ribes,mint(Menthe sativa), and lemon juice
Stimulant, carminative, expectorant, genitourinary
diseases, diuretic, gonorrhoea
15
Kanakasava Pippali (long pepper) – P. longum, Sonth (ginger
rhizome) – Zingiber officinale, Mulethi – Glycyrrhiza
glabra, Vasaka – Adhatoda Vasica, Shuddha Datura
Panchang – Purified Datura Metal (All Parts)
Bronchodilator, expectorant, analgesic,
antispasmodic, sedative, cardiac stimulant,
soporific (sleep inducing), digestive
16
Panchakola Churna
Vardhamana Pippali
Rasayana
Pippali (P. longum), Pippalimoola (P. longum), Chavya
(Piper retrofractum), Chitraka (Plumbago zeylanica),
Shunti (Zingiber officinale) Pippali (P. longum), Honey,
ghee (clarified butter)
Bronchitis, asthma, piles, anemia, chronic rhinitis,
intermittent fever, splenic disorders, obstinate
abdominal diseases, rheumatoid arthritis
15
Avipattikara Churna Black pepper (P. nigrum), Ginger (Zingiber officinale),
Amla (Emblica officinalis), Behada (Terminalia
belerica), cardamom (Elettaria cardamomum),
Syzygium aromaticum
Diarrhoea, gastritis, heartburn, indigestion, ulcers,
peptic ulcers
16 and 17
Decoction (seeds) Piper guineense Linn. Fungal infections, asthma, antipsychotic,
respiratory infections, infertility (female),
bronchitis, syphilis
20–24
Cold maceration
(fruits and leaves)
Piper guineense Skin diseases, mouth infections 25
Talisapatradi churnam Talisa (Abies webbiana), Maricha (P. nigrum),
Shunti (Zingiber officinale), Pippali (P. longum),
Vamshalochana (Bambusa bambos)
Respiratory diseases, cough, cold, burning sensation
in palms and feet, low digestion strength, loss of
sensation in tongue, pain in abdomen and flanks,
anorexia, bleeding from the nose
23
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Badi Elaichi (Elettaria cardamomum) and Eugenia aromatica (Syzygium ar-
omaticum), which are used therapeutically in diarrhoea, gastritis, heartburn,
indigestion, ulcers and peptic ulcers.
18,19
A decoction (seeds) contains the
composition Piper guineense Linn. that is used therapeutically for fungal
infections, asthma, neuroleptic, breathing infections, sterility (female),
bronchitis and syphilis.
20–24
A cold maceration of the fruits and leaves
possesses the ingredients Piper guineense and is used therapeutically in skin
diseases and mouth infections.
25
Talisapatradi churnam (an Ayurvedic
powder form) Talisa (Himorinda), Maricha (P. nigrum), Shunti (Z. officinale),
Pippali (P. longum) and Vamshalochana (Bambusa arundinacea) are ther-
apeutically used in flanks, anorexia, and bleeding from the nose.
23
The Unani system of medicine regards P. nigrum, also known as filfil siyah,
as a vital component for treating various ailments. In addition, according to
the Siddha system of medicine, P. nigrum is the oldest spice and a vital
component of many Siddha medicines. Some Unani formulations are
mentioned, along with their composition and their therapeutic uses, that
contain black pepper, such as Azaaraaqi includes Kuchla Biryan, Mirch Siyan
(P. nigrum) Nervine tonic and stimulant, used explicitly in paralysis.
26
Ja-
warish Kamoni Sada contains the ingredients Berg Sadab (Ruta graveolence
leaf), Boora amreniac (Arminium bole), Filfil Siya (black pepper fruit), ginger
(Z. officinalis rhizome) and Zeera Siyah Mudabbar (Caraway detoxified), and
is used therapeutically in cases of constipation, stomach ache and colic pain,
and also improves digestion.
27
Habbe Kabid Naushadri contains Naushader
(ammonium chloride), Namak Tuam (NaCl), Namak Siyahm (Na
2
SO
4
with
NaCl), Namak lahori (sodium chlorate), Haleela Siyah (Haritaki unripe fruit),
Post Haleela Kabuli (Haritaki ripe fruit), Baobarang (mugwort seed), Filfil
Siyah (P. nigrum fruit), Zanjabil (Z. officinalis rhizome), Suhaga (Borax) and
Zaranbad (turmeric) and is used to treat hepatitis, dyspepsia, and consti-
pation.
28
Jawarish Zarooni Sada contains Maghz-Tukhm-Kharpazah, Maghz-
Tukhm-Kheyar, Tukhm-e-Karaf Post-Beekh-e-Karafs, Post-Beekh-e-Karafs,
Nankhah, Badiyan, Qaranfal and Filfi and is used therapeutically as a di-
uretic and neuroprotective, in treating kidney dysfunction, weakness of the
digestive system, liver dysfunction, indigestion, excessive urination and hy-
drospermia.
27
Habbe Gule Aakh contains Zanjabeel (Z. officinalis), FilfilSiyah
(P. nigrum), GuleMadar (Calotropis gigantea Linn.) and Barge Bans (Bambusa
arundinacea Wild) and is used therapeutically in cases of backache and
cervical spondylosis, and has antiinflammatory and analgesic activities.
27
Table 7.2 shows details of the Unani formulations of P. nigrum along with
their compositions and therapeutic uses.
Siddha formulations contain black pepper, including Trikadagu Choor-
nam possesses Chukku (Rhizome zingiberis), Milagu (long pepper) and
Thippili (long pepper) and are used therapeutically for their analgesic and
antiinflammatory properties and also in the treatment of indigestion, gas
trouble, constipation and bloating, and as a carminative.
28
Kesari Lehyam
contains lemon fruit, milagu (long pepper), daniya (coriander), koshtam
(spiral flag), chukku (dried ginger), thaleesapatri (yew), tippili (P. longum),
154 Chapter 7
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Table 7.2 Unani formulations containing piperine.
Formulations Compositions Therapeutic uses Ref.
Habb-e-Azaraqi Kuchla Biryan, Mirch Siyan (P. nigrum) Nervine tonic and stimulant. Specifically
used in paralysis
26
Jawarish Kamoni Sada Berg Suddab (Ruta graveolence leaf), Boora armani
(Arminium bole), Filfil Siyah (P. nigrum fruit),
Zanjabil (Zingiber officinalis rhizome), Zeera Siyah
Mudabbar (Carum carvi seed detoxified)
Stomachache, colic pain. Improves
digestion and resolves constipation
27
Habbe Kabid Naushadri Naushader (ammonium chloride) Namak Tuam
(sodium chloride) Namak Siyah (sodium sulphate
with sodium chloride) Namak lahori (sodium
chlorate) Haleela Siyah (Terminelia chebula unripe
fruit) Post Haleela Kabuli (Terminelia chebula ripe
fruit) Baobarang (Artemisia vulgaris seed) Filfil Siyah
(P. nigrum fruit) Zanjabil (Zingiber officinalis rhizome)
Suhaga (Borax) Zaranbad (Curcuma zedoria root)
Hepatitis, dyspepsia, constipation 28
Jawarish Zarooni Sada Maghz-Tukhm-Kharpazah, Maghz-Tukhm-Kheyar,
Tukhm-e-Karaf,Post-Beekh-e-Karafs, Post-Beekh-e-
Karafs, Nankhah, Badiyan, Qaranfal, Filfi
Diuretic and neuroprotective, kidney
dysfunction, weakness of the digestive
system, liver dysfunction, indigestion,
excessive urination and hypospermia
27
Habbe Gule Aakh Zanjabeel; Zingiber officinalis, FilfilSiyah; P. nigrum,
GuleMadar; Calotropis gigantea Linn., Barge Bans;
Bambusa arundinacea Willd.
Backache, cervical spondylosis,
antiinflammatory and analgesic activity
27
Most Modern Approach to the Phytochemical Evaluation 155
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jathikkai (Buah Pala), jathipathri (Mace), ghee and sugar, and is used ther-
apeutically for vomiting, dizziness, indigestion, anorexia, pitha diseases,
a loss of taste and flatulence.
29
Mezhugu contains Chukku (dried ginger),
Omam (ajwain), Manjal (turmeric), Vaividangam (false black pepper),
Vasambu (sweet-flag), Lavangam (cinnamon), Parangi pattai (acorn squash),
Seran kottai (bhallatak), Kadukkai thole (myrobalan Retz.), Karum seeragam
(black cumin), Kaattu seeragam (Kuntze.), Siruthekku (f. muell.), Thaalee-
sapathiri (yew), Thiraatchai (grape vine), Thippili (P. longum L.), Sitraraththai
(shell ginger) and kuth and is used therapeutically for painful conditions,
fissures, leprosy, scrofula, rashes, alopecia, itches, hot flush, glandular
enlargements, cancer infections, piles, severe pain in the legs, slipped discs,
back injury, skin diseases and psoriasis.
30
Amukkara choornam includes
Indian ginseng (Withania somnifera), ginger (Z. officinale), Thippili (long
pepper) ( P. longum), Milagu (black pepper) (P. nigrum), Elam (Badi Elaichi),
Sirunagapoo, Dalchini ( Cinnamomum verum) and Kirambu Laung (clove)
(Syzygium aromaticum).
29
Table 7.3 shows details of the Siddha formulations
of P. nigrum along with their compositions and therapeutic uses.
7.6 Different Modern Formulations Available
Containing Black Pepper
Cadila Pharmaceutics Ltd. in Ahmadabad manufactured the marketed for-
mulation risorine developed by Regional Research Laboratory, Jammu, and
marketed in India that contains about 200 mg rifampicin, 300 mg isoniazid,
and 10 mg piperine. This medication has been accepted for the treatmen t of
pulmonary tuberculosis. A study of the combination of isoniazid with pi-
perine showed the dose of rifampicin could be reduced to 200 mg which was
nearly half the original amount. A pilot study involved using risorine to treat
pulmonary tuberculosis in human volunteers. Risorine kit was used to treat
27 patients who had pulmonary tuberculosis. The medication contains ri-
sorine and ethambutol, at approximately 800 mg, as well as pyrazinamide,
approximately 750 mg, each per day for 2 months. The patients received one
risorine tablet per month for the following 4 months. Pure curcumin from
Simply Herbal is a concentrated form of curcumin with a combination of
400 mg of natural curcumin extract, 5 mg of piperine, and 395 mg of tur-
meric powder. It is prescribed as a powerful antioxidant and antiin-
flammatory compound. According to Gaurav Marketing, curcumin and
piperine capsules promote antiallergic effects, are natural detoxifiers, have
neuroprotective properties, cholesterol and hepatoprotective properties, and
increase gastric acid secretion. A Pukhraj product is also used ther-
apeutically to improve the health of the liver, aid digestion, and ease dis-
comfort. Curcumin 3 is a health supplement manufactured by Health Aid
containing biotin (1000 mg), bamboo extract (20 mg) and piperine (5 mg)
that is also found in Herbal’s premium Biotin capsules.
31
Other different
marketed formulations are listed in Table 7.4.
156 Chapter 7
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Table 7.3 Siddha formulations containing piperine.
Formulations Compositions Therapeutic uses Ref.
Trikadagu
Choornam
Chukku (dried ginger), Milagu (pepper) and Thippili (long
pepper)
Analgesic and antiinflammatory properties,
digestive, carminative and used in
treatment of indigestion, gas problems,
constipation and bloating
24
Kesari Lehyam Lemon fruit, Milagu (P. nigrum), Daniya (Coriandrum
sativum), Koshtam (Costus speciosus), Chukku (Dried
Ginger), Thaleesapatri (Taxus baccata), Tippili
(P. longum), Jathikkai (Myristica fragrans), Jathipathri
(Mace), ghee, sugar
Vomiting, dizziness, indigestion, anorexia,
pitha diseases, loss of taste and flatulence
29
Mezhugu Chukku (Zingiber officinale), Omam (Trachyspermum
ammi L.), Manjal (Curcuma longa L.), Vaividangam
(Embelia ribes Burm.f.), Vasambu (Acorus calamus L.),
Lavangam (Cinnamomum zeylanicum), Parangi pattai
(Cucurbita pepo L.), Seran kottai (Semecarpus anarcadium
L.), Kadukkai thole (Terminalia chebula Retz.), Karum
seeragam (Nigella sativa L.), Kaattu seeragam
(Centratherum anthelminticum L.), Siruthekku (Premna
herbacea Roxb.), Thaaleesapathiri (Taxus baccata),
Thiraatchai (Vitis vinifera L.), Thippili (P. longum)
Sitraraththai (Alpinia speciosa L.), Kottam
Painful conditions, fissures, leprosy, scrofula,
rashes, alopecia, itches, hot flush, glandular
enlargements, cancer, infections, piles,
excessive pain in the legs, slipped disc, back
injury, skin diseases and psoriasis
30
Amukkara
choornam
Ashwagandha (Withania somnifera), Chukku (Zingiber
officinale), Thippili (long pepper) (P. Longum), Milagu
(black pepper) (P. Nigrum), Elam (cardamom) (Elettaria
Cardamomum), Sirunagapoo; Dalchini (Cinnamomum
verum), Kirambu Laung (Clove) (Syzygium aromaticum)
Nervine tonic, antiinflammatory, antitussive,
Rasayana (rejuvenating), aphrodisiac,
antidepressant, immunomodulatory,
antioxidant, anodyne, cardioprotective,
mild antiasthmatic, mild anabolic effect
29
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Table 7.4 Herbal formulations containing piperine in the Indian pharmaceutical market.
Formulation Manufacturer Ingredients and quantity Therapeutic uses Ref.
Pure
curcumin(curcumin
and piperine extract)
Simply Herbal Turmeric powder (395 mg), natural
curcumin extract (400 mg) and
piperine (5 mg)
Antiinflammatory, powerful antioxidant,
prescribed as a dietary supplement
9
Curcumin and piperine
capsule
Gaurav
Marketing
Curcumin and piperine Antiallergic, natural detoxifier,
neuroprotective, cholesterol,
hepatoprotective, gastric acid secretion
Premium curcumin Pukhraj Not mentioned Weight loss, cancer, protects liver health,
aids digestion, eases discomfort,
inflammation and prevents arthritis
Curcumin 3 Health aid Curcumin, standardized piperine
(95%)
Health supplement
Premium biotin
capsules
Simply herbal Biotin (1000 mg), bamboo extract
(20 mg), piperine (5 mg)
Health supplement
158 Chapter 7
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7.7 Phytochemicals
Bioactive components are significant phytochemicals owing to their po-
tential for healing various ailments. Functional foods usually provide
additional physiological benefits or prevent chronic illness in addition to
basic nutrition. The antioxidant, antimicrobial, and gastro-protective
properties of black pepper (P. nigrum L.) make it an important food
source. Piperine is the active component in black pepper, which has rich
phytochemistry, including volatile oil, oleoresins, alkaloids, etc. Perakis
et al. evaluated the P. nigrum ground seed, peppercorn, or dried berry as
having 11 wt% oleoresins, 6 wt% piperine and 2% (v/w) essential oil.
32
Meanwhile, Singh et al.
33
evaluated and found the foremost compounds to
be piperine (34%), piperolein B (14%), anonymous alkaloid constituents
(6% and 7%) and other recognized piperamides (o4%) in P. nigrum es-
sential oil acetone extract.
33
Perakis et al.
32
demonstrated the supercritical
fluid extraction (SFE) of essential oil of P. nigrum seed and P. tuberculatum
leaf extract comprises five piperamides, together with piperine, commonly
existing and used as standards. The different chemical structures of
P. nigrum areillustratedinFigure7.4.
7.7.1 Whole Plant
The entire plant parts were individually extracted with petroleum ether,
chloroform, and butanol, sequentially, by Liu et al.
34
for the isolation of
compounds and their structured ethanol extracts. Additionally, chromato-
graphic analysis of chloroform fractions revealed various compounds such as
MS,
1
H-NMR and
13
C-NMR. Liu et al. carried out reported some of the com-
pounds such as (4E)-7-(4-hydroxy-3-methoxyphenyl)-1-phenylhept-4-en-3-one,
Aristolactam FI, isopiperine, cerulenin, 2-hepten-methylenealpha-(1-methy-
lethyl)-1H-indene-1-methanolmonodemethoxycurcumin.
34
7.7.2 Fruits
Different phytoconstituents including (2E,8E)-9-(2H-1,3-benzodioxol-5-yl)-N-(2-
methylpropyl)nona-2,8-dienamide, retrofractamide B, (E,E)-N-(2-methylpropyl)-
2,4-decadienamide2,4-decadienamide, pipyahyine, dehydropipernoline,
piperloein B, (2E,8E)-9-(1,3-benzodioxol-5-yl)-1-piperidin-1-ylnona-2,8-dien-1-
one and 1-piperoylpiperidine have been identified from the methanol extract
by mass spectroscopy. Additionally, dehydropipernoline, piperloein B and
(2E,8E)-9-(1,3-benzodioxol-5-yl)-1-piperidin-1-ylnona-2,8-dien-1-one had an in-
hibitory effect on Stat3-dependent luciferase activities induced by IL-6.
35
Sar-
mentine is a chemical compound derived from the ethanolic extract of
P. longum, which produces phytotoxic effects and functions as a herbicide.
36
On HL-60 cell lines, the moieties had cytotoxic activity.
37
Piperlongimin B
(2E-octadecenoylpiperidine), 2E,4E-N-isobutyl-dodecenamide and 2E,4E,12E,13-
(3,4-methylenedioxyphenyl)-trideca-trienoic acid isobutylamide were isolated
Most Modern Approach to the Phytochemical Evaluation 159
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moieties described by Sahi et al. as compounds that seemed to have activity
against Leishmania donovani.
38
A new alkaloid amide derivative called
P. longumide was identified by Ghosal et al. Furthermore, they developed
leishmanicidal promastigotes and axenic amastigotes of Leishmania dono-
vani.
39
Jiang et al.
40
evaluated the isolated amide alkaloids, P. longumamide A,
P. longumamide B and Piper longumamide C. The already identified com-
pounds which were isolated included piperine, (2Z,4E)-5-(1,3-benzodioxol-
5-yl)-1-piperidin-1-ylpenta-2,4-dien-1-one, cis-piperine, piperlonguminine,
Figure 7.4 The different chemical structures of Piper nigrum.
160 Chapter 7
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(2E,4E)-N-(2-methylpropyl)deca-2,4-dienamide,(2E,4E)-15-(1,3-benzodioxol-5-
yl)-N-(2 methylpropyl)pentadeca-2,4 dienamide, pipyahyine, piperchabamide
B, pipernonaline and piperolein B.
40
7.7.3 Roots
The syntheses of piperlongumine (Piplartine) and piperlonguminine, a rich
alkaloid of Piper longum L., were explored along with their anticancer
properties.
41
The ethanol extract of roots of P. longum yielded cefradine,
norcepharadione B and 2-hydroxy-1-methoxy-4H-dibenzo quinoline-4,5(6H)-
dione. Also, three new alkaloids were discovered: piperolactam A, piper-
olactam B and piperadione.
42
7.7.4 Different Habitats and Diversity in Phytochemicals
An established and widely distributed pantropical taxon of aromatic plants,
the Piper genus has historically been used both as a food and medicine.
Essential oils (EOs) are found in a wide range of tissues and organs of the
pepper plant, including the fruits, seeds, leaves, branches, roots and
stems.
43,44
Although the Piper species have been studied extensively since the
1960s, Dyer
45
claims that only 10% of the EOs have been phytochemically
studied. As a result of the variety of chemical components and the variety
of tissues from which Piper EOs are obtained, it is difficult to summarize
the nature of Piper EOs. Mgbeahuruioke et al.
46
identified more than 270
compounds in Piper EOs. Xiang et al.
47
stated in their review that over 80
compounds were found in Chinese Piper spp., and that these compounds
were mostly hydrocarbons, followed by aldehydes, alcohols, acids, ketones,
esters and phenols. The secondary metabolites in some species might ap-
pear simple, while those in others, such as P. nigrum, P. betle and P. auritum,
may contain large amounts of different compounds.
According to Mgbeahuruioke et al.
46
the African Piper spp. EOs show great
chemical diversity and presence of chemotypes. These authors cite seven
chemotypes of Piper guineense from Nigeria (b-caryophyllene/germacrene
D; asaricin; a-pinene/b-pinene/germacrene B; b-pinene/a-pinene/b-car-
yophyllene; b-pinene/a-pinene/1,8-cineole; linalool) and three chemotypes of
P. guineense from Cameroon (a-pinene/b-pinene; b-caryophyllene/limonene//
pinenes; b-caryophyllene).
25
In addition to chemical differences, many authors have claimed that
chemotypes are responsible for these differences. As suggested by da Silva
et al., at least seven species of neotropical insects exhibit chemotypes.
Notable differences between neotropical and African general compositions
are the greater quantitative importance of the monoterpene hydrocarbons
(b-pinene, a-phellandrene and (Z)-b-ocimene) and of the sesquiterpene
hydrocarbons (b-elemene, b-sesquiphellandrene, (Z)-b-bisabolene, (Z, Z )-a-
farnesene, ar-curcumeme, a-zingiberene and d-cadinene). On the other
hand, the African species are less rich in the monoterpene hydrocarbons
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