Article

Analysis of Pogostemon cablin from pharmaceutical research to market performances

Abstract and Figures

Introduction: Pogostemon cablin (P. cablin), called Ciruicao or Guanghuoxiang, is a well-known Chinese materia medica in southeast Asia that is widely used in gastrointestinal disease and exterior syndromes, being confirmed by both in vitro and in vivo studies. To exploit this traditional medicine that adequately fits modern drugs, however, a comprehensive review about its pharmacy research and market performance is extremely necessary. Areas covered: This article reviews various components extracted from this plant as well as the biological activities derived from those chemical compositions. The authors summarize the quality evaluation and highlight the therapeutic effects of P. cablin, such as antiviral activities, antioxidation effect, antiinflammatory, analgesic activities, and intestinal barrier function protection. The preparation profile of P. cablin and some future related research were also described in this review. Last but not least, a market performance analysis was conducted. Expert opinion: P. cablin has beneficial therapeutic potential as an effective adaptogenic herbal remedy in clinic. Molecular mechanisms and active targets of P. cablin compounds, the qualitative and quantitative standard of P. cablin, as well as novel drug delivery systems of P. cablin, would be developed.
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1. Introduction
2. Chemical components
3. Quality evaluation
4. Pharmacological activities
5. Preparation profile
6. Market performance analysis
7. Conclusions
8. Expert opinion
Review
Analysis of Pogostemon cablin
from pharmaceutical research
to market performances
Meiwan Chen, Jinming Zhang, Yunfeng Lai, Shengpeng Wang, Peng Li,
Jian Xiao, Chaomei Fu, Hao Hu & Yitao Wang
University of Macau, Institute of Chinese Medical Sciences, State Key Laboratory of Quality
Research in Chinese Medicine, Macao, China
Introduction: Pogostemon cablin (P. cablin), called Ciruicao or Guanghuox-
iang, is a well-known Chinese materia medica in southeast Asia that is widely
used in gastrointestinal disease and exterior syndromes, being confirmed by
both in vitro and in vivo studies. To exploit this traditional medicine that
adequately fits modern drugs, however, a comprehensive review about its
pharmacy research and market performance is extremely necessary.
Areas covered: This article reviews various components extracted from this
plant as well as the biological activities derived from those chemical composi-
tions. The authors summarize the quality evaluation and highlight the thera-
peutic effects of P. cablin, such as antiviral activities, antioxidation effect,
antiinflammatory, analgesic activities, and intestinal barrier function protec-
tion. The preparation profile of P. cablin and some future related research
were also described in this review. Last but not least, a market performance
analysis was conducted.
Expert opinion: P. cablin has beneficial therapeutic potential as an effective
adaptogenic herbal remedy in clinic. Molecular mechanisms and active targets
of P. cablin compounds, the qualitative and quantitative standard of P. cablin,
as well as novel drug delivery systems of P. cablin, would be developed.
Keywords: chemical composition, market performances, pharmacological effect,
Pogostemon cablin, quality evaluation
Expert Opin. Investig. Drugs [Early Online]
1. Introduction
Pogostemon cablin (Blanco) Benth., belonging to the genus Pogostemon in Lamiaceae,
is a very important traditional Chinese materia medica [1,2]. It has been cultivated in
southern China since the Song Dynasty after being introduced from southeast Asia
(e.g., the Philippines, Malaysia, and India) more than 1,000 years ago. To distin-
guish with Agastache species named Huoxiang in Chinese, growing in northern
area of China, P. cablin is also called Guanghuoxiang in Chinese in both traditional
TCM classics and modern Chinese Pharmacopoeia. Today, commercial herbs of
P. cablin in China are categorized according to their different distributions.
P. cablin is widely used to remove dampness, regulate gastrointestinal functions,
and relieve superficies syndrome [3] in southeast Asian areas, particularly, in Guang-
dong Province, Hong Kong, and Macao. To date, P. cablin’s dry stem and leaf have
been used as the main compositions in more than 40 kinds of traditional Chinese
medicine (TCM) preparations [3] on the market for dispelling dampness in the
middle-energizer, summer heat and dampness, acedia, fullness in the chest,
hypochondrium issues, cramps, diarrhea, and so on. Additional uses of it include
making herbal tea and cooking soup using P. cablin to deal with the muggy and
moisture weather in southeast Asia. Interestingly, patchouli essential oil is also
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used in cosmetics, deodorants and insecticides. Recently,
essential oil produced by P. cablin (Blanco) Benth is thought
as the most important bioactive material which contains
various sesquiterpenes and hydrocarbons, such as patchouli
alcohol (patchoulol), patchoulene, bulnesene, guaiene,
caryophyllene, elemene, and copaene [4].
Herein, the present paper first gives an overview of
patchouli’s chemical components and quality evaluation. In
particular, the bioactive compounds contained in essential oil
and some nonvolatile chemical compounds, such as flavonoids
and glycosides, in P. cablin are summarized. Furthermore, we
highlight the pharmacological activities of P. cablin derived
from the above chemical compositions. Finally, we discuss
P. cablin’s market profile and identify 41 kinds of preparations
containing P. cablin that are available on the market, including
pills, tablets, granules, capsules, liquids, and medicinal wine,
made by five kinds of extraction methods.
2. Chemical components
Now, rapid advancements have been made in chemical
constituent analysis of P. cablin, generally dividing it into vol-
atile and nonvolatile compounds. First, focus has been on the
volatile oil from its leaves and stems, as the main active ingre-
dient, and it has been discovered that there are several kinds
of compounds including monoterpene, sesquiterpene and
micromolecular alcohol. Ling et al. [1] identified 33 com-
pounds from volatile oil of P. cablin for the first time, which
mainly contained patchouli alcohol (31.86%), seychellene
(9.58%), a-guaiene (8.82%), d-guaiene (8.65%), a-patchou-
lene (8.48%), b-patchoulene (6.91%), pogostone (3.83%),
using gas chromatography-- mass spectrometry (GC-MS).
Similarly, 24 compounds were reported by Zhang et al. whose
content were mostly 96% of total volatile oil. Some volatile
oil compounds, including geranium ketone, 7-patchoulene,
a-patchoulene, a-bulnesene, 5-cedrol and eucalyptus oil
ketene. Additionally, four new patchoulene derivatives, namely
8a,9a-dihydroxypatchoulol, 3a,8a-dihydroxypatchoulol,
6a-hydroxypatchoulol and 2b, 12-dihydroxypatchoulol, were
isolated from the aerial part of P. cablin (Labiatae)’s, four
sesquiterpenoids: namely (5R)-5-hydroxypathoulol, (9R)-
9-hydroxypatchoulol, (8S)-8-hydroxypatoulol and (3R)-
3-hydroxypathoulol [7]. The structures of main terpenoid
compounds in volatile oil of P. cablin are shown in Figure 1.
Although most studies focused on the analysis of volatile
compounds, nonvolatile compounds in P. cablin are still
increasingly reported. Guan et al. [8] obtained two flavones,
retusine (1) and pachypodol (2), from P. cablin. And
then, several flavones in the nonvolatile constituents, including
5-hydroxy-3,4¢,7-trimethoxyflavone (3), 5-hydroxy-4¢,7-dime-
thoxyflavone, 5¢-hydroxy-3¢,4¢,7-trimethoxyflavanone, 3,3¢,4¢,
5,7-pentahydroxyflavone (4), 3,5-dihydroxy-4¢,7-dimethoxy-
flavone (5), 4¢,5-dihydroxy-7¢-methoxyflavone (6), ombuine
(7), apigeni n (8), rhamnetin (9), apigetrin (10), apigenin
7-O-b-D-(-6¢-p-coumaroyl)-glucoside (11), respectively were
isolated by Zhang et al. [9] and Itokawa et al. [10] using column
chromatography. Additionally, Huang et al. [11] totally isolated
four flavonoid glycosides, including isorhamnetin-3-O-b-D-
galactoside (12), hyperoside (13), 3,5,8,3¢,4¢-pentahydroxy-
7-methoxyflavone-3-O-b-D-galactoside (14) and isisolidone-
7-O-a-L-rhamnopyranoside from the ethanol extract of stem
leaf of P. cablin. Meanwhile, some flavonoids isolated from P.
cablin and identified by spectrum were reported [12] as follows:
4¢,5-dihydroxy-3¢, 7-dimethoxyflavanone (I), 5-hydroxy-7, 3¢,
4¢-trimethoxyflavanone (II), 3, 5-dihydroxy-7, 4¢-
dimethoxyflavone (III), 5-hydroxy-3, 7, 4¢-trime-
thoxyflavone (IV), 5-hydroxy-3, 7, 3¢,4¢-tetrameth-
oxyflavone (V), 5, 4¢-dihydroxy-3, 7, 3¢-trimethoxyflavone
(VI), 5, 4¢-dihydroxy-7-methoxyflavone (VII), 3, 5, 7, 3¢,4¢-
pentahydroxyflavone (VIII), 5, 7, 4¢-trihydroxyflavone (IX),
and 3, 5, 4¢-trihydroxy-7-methoxyflavone (X). Similarly,
Ding et al. studied the n-butanol extraction of ethanol extract
of the aerial parts of P. cablin, obtaining several glycosides
from it, including apigenin 7-(O-methylglucuronide), apigenin
7-galacturonide, luteolin 7-O-(6-O-methyl-b-D-glucurono-
pyranoside), quercetin-7-b-D-glucoside, syringaresinol-b-D-
glucoside, verbascoside, orobanchoside and campneoside I [13].
The structures of some main flavonoids found from
P. cablin are shown in Figure 2.
In recent years, apart from these flavone compounds, there
are also some other chemical types of nonvolatile compounds
separated from P. cablin (Figure 3). Two new rearranged
patchoulene sesquiterpene glycosides from P. cablin,
3a-hydroxypatchoulane 3-O-b-D-glucopyranoside (I) and
15-hydroxypatchoulol 15-O-b-D-glucopyranoside (II) were
found [14]. Researchers including Guan et al. [8], Treasure [15]
and Itokawa et al. [10] obtained friedelin (III), epifriedelinol
(IV), oleanolic acid (V), b-sitosterol (VI), eugenol (VII),
cinnamaldehyde (VIII), benzaldehyde (IX), patchoulipyridine
(X), epiguaipyridine (XI), daucosterin (XII).
Article highlights.
.Pogostemon cablin, a well-known Chinese materia
medica in southeast Asia, has been widely used in
gastrointestinal disease and exterior syndromes clinically.
.Systematic review on the pharmacy research and market
performance of P. cablin has been reported for the first
time.
.Although both chemical analysis and therapeutic effects
of P. cablin have been reported substantially, there are
still greatly required for in-depth study on its molecular
mechanisms, bioactive targets, the qualitative, and
quantitative standard of P. cablin.
.Appropriate extracting methods of P. cablin need to be
studied deeply.
.Novel dosage forms are required to be developed for
P. cablin.
This box summarizes key points contained in the article.
M. Chen et al.
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3. Quality evaluation
There are mainly four traditional growing areas of P. cablin
in Guangdong Province of China, which are Shipai (in
Guangzhou city), Zhaoqin (in Zhaoqin city), Zhanjiang
(in Zhanjiang city) and Hainan city. Researchers [17] have
realized that the diversity in plant origins and growing envi-
ronments could result in quality differences between the
decoction slices in clinic and market from the point of view
of the morphological properties, chemical components and
biological activities. Thus, to estimate the appropriate quality
evaluation approach for P. cablin would be the key to assure
clinical effects.
Recently, several methods have been utilized as the tools
for quality control of volatile oil compounds in P. cablin,
such as thin-layer chromatography (TLC), gas chroma-
tography (GC), GC-MS, pyrolysis gas chromatography,
high performance liquid chromatography (HPLC), due to
its acknowledged active materials. Amakura et al. [18]
reported a convenient TLC method of the methanol extract
using patchouli alcohol as a marker for identifying the
crude drug Pogostemoni herba. A gas chromatography-
tandem mass spectrometry (GC/MS/MS) method for the
determination of patchoulic alcohol content in dried
P. cablin were developed [19]. With the cognition of the
necessity to develop multiple indexes for quality evaluation
of Chinese herbs, chemical fingerprint has been increasingly
adopted in quality evaluation of P. cablin. Some researchers
established GC-MS fingerprint of P. cablin oil as its charac-
teristic standard [20,21].Zhanget al. [22] established the pyrol-
ysis gas chromatography fingerprint of 13 P. cablin herbal
samples from multi-origins using fuzzy cluster analysis.
Yuan et al. [23] setupaHPLCfingerprintdetermination
method of P. cablin. GC-FID quantitative analysis were
did [24] and GC-MS qualitative analysis for patchouli
essential oils obtained from fresh, dried and fermented
P. cablin herbs.
Based on these measures, some researchers set out to
evaluate herb quality of P. cablin from different areas with
different growing environment, harvest time and processing
methods. Summarized that P. cablin herbs from different
locations were found to [25] contain different oil types.
Luo et al. [26] reported that P. cablin herbs from Shipai har-
vested in July would be of better quality, comparing the vol-
atile oil constituents of P. cablin from different regions and
harvesting times via GC-MS. Yin [27] established ‘the charac-
teristics of fingerprint data’ of 24 batches of P. cablin herbs
from Shipai, Gaoyao and Hainan areas by GC-MS.
OH
Patchouli alcohol Seychellene α-guaiene δ-guaiene
α-patchlene β-patchoulene
O
O
H
O
CCCH
CH3
CH3
O
Pogostone
β-caryophyllene Aristolone β-maaliene α-pinene
β-pinene α-curcumene γ-selinene δ-elemene
Figure 1. Structure of some main terpenoids in volatile oil of P. cablin.
Analysis of P. cablin from pharmaceutical research to market performances
Expert Opin. Investig. Drugs [Early Online] 3
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Hussin et al. [24] evaluated the essential oils derived from
fresh, dried and fermented plant material by GC-
FID quantitative analysis using an internal standard method
with response factors. A good correlation between genotype
and distribution of P. cablin samples by elucidating its inher-
ent characteristics in different localities applying GC-
MS fingerprint analysis, together with random amplified
polymorphic DNA fingerprint and DNA sequencing analy-
sis. All these studies would be beneficial to testify the genu-
ineness of P. cablin.
4. Pharmacological activities
Various biological activities have been found in many aspects,
such as antiviral activities, antioxidation effect, anti-inflammatory
and analgesic activities and anti-bacterial activities.
4.1 Antiviral activities
The extract of P. cablin derived from SFE-CO
2
has demon-
strated obvious anti-influenza virus FM1 effects on mice
influenza models in vivo evaluated by pulmonary index and
death-protection rate [29].Kiyoharaet al. [30] found that meth-
anol extract from the leaves of P. cablin Benth. showed potent
in vitro antiviral activity (99.8% inhibition at a concentration
of 10 µg/ml) against the influenza virus. Meanwhile, patchouli
alcohol in volatile oil, as the major active principle on the basis
of silica gel column chromatography and reversed-phase
HPLC, showed potent dose-dependent anti-influenza virus
activity against A/PR/8/34 (H
1
N
1
)(IC
50
=2.635µM), but
weak activity against B/Ibaraki/2/85 (IC
50
=40.82µM) and
no activity against A/Guizhou/54/89 (H
3
N
2
). Additionally,
further research [31] reported that the extracts of methanol
and ethyl acetate from P. cablin demonstrated good effects on
R1 = OCH3; R2 = Me; R3 = OCH3; R4 = H; R5 = OH; R6 = Me
5-Hydroxy-4,7-dimethoxyflavone
5-Hydroxy-34,7-trimethoxyflavone
Isisolidone-7-O-α-L-rhamnopyranoside
R1 = OCH3; R2 = Me; R3 = OCH3; R4 = H; R5 = OH; R6 = H
R1 = H; R2 = Me; R3 = OCH3; R4 = H; R5 = OH; R6 = Me
R1 = OH; R2 = H; R3 = OH; R4 = H; R5 = OH; R6 = H
R1 = H; R2 = Me; R3 = OH; R4 = H; R5 = OH; R6 = Me
R1 = H; R2 = Me; R3 = OH; R4 = H; R5 = OH; R6 = H
R1 = OH; R2 = H; R3 = H; R4 = H; R5 = OH; R6 = H
R1 = H; R2 = H; R3 = OCH3; R4 = H; R5 = OH; R6 = H
R1 = OH; R2 = Me; R3 = OH; R4 = H; R5 = OH; R6 = H
R1 = H; R2 = glu; R3 = H; R4 = H; R5 = OH; R6 = H
R1 = H; R2 = H; R3 = H; R4 = OH; R5 = H; R6 = glu-6-p-coum aroyl
R1 = OCH3; R2 = H; R3 = O-gal; R4 = H; R5 = OH; R6 = Me
R1 = OH; R2 = H; R3 = O-gal; R4 = H; R5 = OH; R6 = Me
R1 = OH; R2 = Me; R3 = O-glu; R4 = OH; R5 = OH; R6 = Me
1
2
3
4
5
6
7
8
9
10
11
12
13
14
R = OCH3
R = OH
R1 = OH, R2, R3 = OCH3, R4 = H
R1, R2, R3 = OCH3, R4 = H
R1, R2, R3, R4 = OCH3
R1, R2, R4 = OCH3, R3 = OH
R1, R4 = H, R2 = OCH3, R3 = OH
R1, R2, R3, R4 = OH
R1 = H, R2 = R3 = OH, R4 = H
R1 = R3 = OH, R2 = OCH3, R4 = H
(I)
(II)
(III)
(IV)
(V)
(VI)
(VII)
(VIII)
(IX)
(X)
O
R2O
R4
R5O
R3
R1
OR6
O
H3CO
OH O
OCH3
OH3CO
O
OCH3
OCH3
OCH3
O
OCH3
R
OOH
H3CO
O
R4
R3
OOH
R2
R1
OO
OCH3
OH O
O
H3C
HO
HOHO
Figure 2. Structure of some flavonoids in P. cablin.
M. Chen et al.
4Expert Opin. Investig. Drugs [Early Online]
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anti-coxsackievirus B, with IC
50
being 26.92 and 13.84 µg/ml,
respectively. Although it seems that P. cablin could be a
potential antiviral resource, its mechanism remains unknown
till date.
4.2 Antimicrobial activities
Antibacterial, antifungal and anti-plasmodium activities of
P. cablin have been uncovered. For antibacterial effects,
Liu et al. [32] found that anti-enterobacteria effects of aqueous
extract of Gaoyao Huoxiang is more potent than that of
Zhanjiang Huoxiang, but there are no significant differences
between the volatile oil of these two varieties. Furthermore,
Luo [33] investigated antibacterial effects of the aqueous
extracts from P. cablin on Staphylococcus aureus,Bacillus sub-
tilis,Pseudomonas aeruginosa,Enteritis coccus and Aerobacter
aerogenes, and it interestingly showed the significant activity
in S. aureus, while no effect on Escherichia coli. For antifungal
effects, Su et al. [34] researched the antagonistic effects of
P. cablin oil on 11 kinds of fungal and 5 kinds of bacterium
and showed weak even no effects on Aspergillus flavus,
Aspergillus niger and E. coli. Yang et al. [35] claimed that patch-
ouli oil from China, which principally contains patchouli
alcohol, a-bulnesene and patchoulene, showed the most
potent inhibitory action on 12 kinds of dermatophyte
(a MIC value of 50 -- 400 µg·L
-1
). Besides, the synergistic
action of a combination of patchouli oil and sodium
artesunate against Plasmodium berghei has been observed [36].
4.3 Antioxidation effects
Recently, antioxidation effects of P. cablin are developed.
Hussin et al. [37] investigated the antioxidant effect by
scavenging the 2, 2-diphenyl-1-picryl hydrazyl radical
HO
OH
O
OH
HO HO
OH
HO
H
O
OH
HO HO
OH
O
O
HO
HO
OH
O
HO
O
O
OH
HO
HO OH
H3CO
HO
N
CH2
OO
I II III
IV V VI
VII VIII IX
X XI XII
Figure 3. Structure of some nonvolatile compounds apart from flavonoids in P. cablin.
Analysis of P. cablin from pharmaceutical research to market performances
Expert Opin. Investig. Drugs [Early Online] 5
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(DPPH) to show that the essential oils of P. cablin possessed
appreciable antioxidant and radical scavenging activities.
Meanwhile, patchouli alcohol was found to be the primary
chemical constituent and the potential for therapeutic appli-
cations [38]. In addition, it was reported [39] that the polysac-
charides of P. cablin could remove the hydroxyl radical
(.OH) and superoxide anion radical (O2-.) and its activity
was stronger than that of mannitol. Another study showed
that P. cablin could effectively protect the human neuro-
glioma cell line A172 against both necrotic and apoptotic
cell death induced by hydrogen peroxide (H
2
O
2
), which indi-
cates that P. cablin as a reactive oxygen (ROS)-scavenger
might be the cause of the mechanism [40].
4.4 Anti-inflammatory and analgesic activities
For anti-inflammatory and analgesic applications, it has been
reported that the methanol extract of P. cablin could decrease
the acetic acid-induced writhing responses and the licking
time in rats, and the Carr-induced paw edema inflammation
was significantly reduced. Mechanistic studies showed that
the methanol extract could decrease the levels of malondialde-
hyde in the edema paw by increasing the activities of antioxi-
dant enzymes in the liver, including superoxide dismutase,
glutathione peroxidase and glutathione reductase, as well as
decreasing the cyclooxygenase 2 and tumor necrosis factor-a
activities in the edema paw [41]. Moreover, patchouli oil (i.e.,
effective part of P. cablin Hudan Pill) had the same effects of
anti-inflammation and anti-anaphylaxis as positive groups.
4.5 Other biological activities
Other pharmacological effects of P. cablin have been revealed
recently. Researchers [42] found that patchouli alcohol could
markedly attenuate the ROS level and Ca
2+
which were
induced by Ab25 -- 35, resulting in the decrease of the
apoptosis rate, as well as protect against Ab25 -- 35-induced
toxicity. In addition, P. cablin effectively protected the intes-
tinal barrier function by maintaining the membrane’s fluidity
of epithelial cells through the regulation of the NO and
TNF-ain serum levels [43]. The volatile oil of P. cablin inhi-
bited coughing induced by ammonia and increased the phe-
nol red output of trachea in mice, revealing that it had
significant antitussive and expectorant effects [44].
5. Preparation profile
Thus, in all preparations herein only P. cablin would be applied,
huoxiang in these preparations is the abbreviation of guan-
ghuoxiang. For the reason that Agastache rugosus, other species
in north of China recorded as huoxiang in Chinese classics,
has not collected in Chinese Pharmacopeia since 1985 year,
Agastache having no national confirmed standards could not
be used in clinic and preparations. According to the Chinese
Pharmacopoeia and the drug standards of China’s Ministry of
Health, there are 41 main preparations that contain P. cablin
currently available on the market (Table 1). These preparations
included 19 pills, 5 tablets, 4 granules, 5 capsules, 3 oral liquids,
2 medicinal wines, 1 syrup, 1 moxibustion stick, as well as
1 blocky-shaped tea. In the past decades, these preparations of
P. cablin combined with different herbs based on the TCM
combination principles were used to treat different diseases by
improving rheumatism, relieving the exterior, removing
phlegm, addressing antipyretic and dieresis, as well as regulating
stomach functions.
Table 1. Analysis of specific varieties containing P. cablin.
Dosage form Total types Specific varieties
Dropping pill
and pill
19 Shixiang Fansheng pill Renshen Zaizao pill Xiaoer Zhiwan pill Muxiang Fenqi pill
Niuhuang Zhibao pill Liuhe Dingzhong pill Pinggan Shuluo pill Sizheng pill
Zaizao pill Chenxiang Huaqi pill Chunyang Zhengqi pill Baolong pill
Xiangsu Zhengwei pill Xiangsu Tiaowei pill Xiangsha Yangwei pill Baoji pill
Shugan Hewei pill Huoxiang Zhengqi pill Huoxiang Zhengqi
dropping pill
Granule 4 Wushicha granule Xiaoer Ganmao granule Xiangsha Yangwei
granule
Huoxiang Zhengqi
granule
Tablet 5 Tiaowei Xiaozhi tablet Shuzheng tablet Biyankang tablet Huodan pian
Huoxiang Zhengqi tablet
(Soft) capsule 5 Wushicha capsule Shenkangfu capsule Huoxiang Zhengqi
capsule
Huoxiang Zhengqi
soft capsule
Jiawei Huoxiang
Zhengqi soft capsule
Mistura and
oral liquid
3 Huoxiang Zhengqi
mistura
Kangbingdu mistura Huoxiang Zhengqi
oral liquid
Syrup 1 Xiaoer Fuxiening Syrup
Medicinal wine
and tincture
2 Guogong wine Huoxiang Zhengqi
tincture
Moxibustion 1 Yaoai moxa stick
Blocky-shaped tea 1 Xiaoer ganmao tea
M. Chen et al.
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5.1 Process technologies in preparation
As the 41 varieties of preparations above, five types of techno-
logies used in the process P. cablin in TCM formulas, including
extracting with appropriate solvent, using essential oil directly,
and using herbal powder directly, are summarized in Figure 4.
Based on the result, the most used technology for P. cablin to
yield preparations is grinding herb into powder, which is used
in 20 varieties, especially pills. Because sesquiterpenoids and
their derivatives [45], the effective material basis of P. cablin,
are nonpolar and instable in complicated preparation processes,
this process technology avoids the tedious extract and purifica-
tion process, preventing pharmacological substance loss at the
same time. However, it often leads to excessive microorganisms
as well as poor and slow pharmacological effects in vivo because
of the crude decoction pieces of products. Effective compounds
in herbal powder in pills cannot be easily dissolved in vitro and
be adequately absorbed in vivo. In fact, pills containing
P. cablin were mainly used for acute gastrointestinal disorders;
the poor drug release and absorption caused by this most
traditional technology would be the bottleneck of P. cablin
application.
The second frequently used technology is extracting patch-
ouli oil first and then boiling the herb residues with water
twice, which is used in 12 varieties. Recently, chemical con-
stituents, pharmacological effects and quality control of
P. cablin research have focused primarily on volatile oil. The
developing extraction methods of patchouli oil, such as super-
critical fluid extraction, microwave-assisted extraction and
ultrasonic extraction, have aided in surmounting the draw-
backs of traditional methods, such as steam distillation [46].
Nevertheless, following some flavonoids, sterols and triterpe-
noids separated from nonvolatile parts of P. cablin, researchers
found that these nonvolatile compounds also had biological
activities [47]. The effects of the aqueous extract in relieving
gastrointestinal spasms [48,49], improving digestion func-
tion [17], restraining diarrhea [48] and alleviating vomiting [50]
are even stronger than those of volatile oils. Thus, for P. cablin
it would be very necessary to reserve both volatile oil and
nonvolatile compounds when producing pharmaceutics con-
taining this herb. As to liquid-- liquid extraction, the extraction
yield of effective compounds is generally based on solvents
and time-consuming. Commonly used solvents for the
Tech.4 (2%;1
species)
Tech.3 (5%;2
species)
Tech.2 (29%;12
species)
Tech.1 (49%;20
species)
Tech.5 (15%;6
species)
Figure 4. Process technology classification of P. cablin herb in 41 varieties of products. Tech.1 represents grinding into
powder; Tech.2 represents extracting volatile oil + boiling with water; Tech.3 and Tech.4 represent extracting with ethanol
and water, respectively; Tech.5 represents using patchouli essential oil directly.
Table 2. Analysis of Huoxiang Zhengqi varieties.
Huoxiang Zhengqi
varieties
Form of
P. cablin
Amount of
P. cablin
Usage of
P. cablin
Granule Decoction piece 150 g/1000 units First volatile oil is extracted and the aqueous
extraction of herb residues is then collectedMistura 150 g/1000 ml
Capsule 196 g/1000 units
Pill 150 g/1000 units Percolation method with 70% alcohol
Oral liquid Volatile oil 0.8 ml/1025 ml Mixed with other extract
Tablet 160 g/1000 units
Soft capsule 1.95 ml/1000 units
Dropping pill 1.6 ml/2050 ml First dissolved by alcohol and then mixed with
other extract solutionTincture 160 g/1849 units
Analysis of P. cablin from pharmaceutical research to market performances
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extraction of P. cablin herb are water, aqueous mixtures of
ethanol and acetone. Another two extraction technologies
used for the extraction of P. cablin are extracting with water
and extracting with alcohol, respectively. What deserves to
be mentioned is that, in these 41 preparations, 6 varieties con-
taining P. cablin in Figure 4 used patchouli oil directly instead
of its herbal material. Using active ingredients as the materials
rather than herbs would be the improvement and develop-
ment tendency of modern pharmaceuticals, which would
avoid the shortage from herbal powder and common extrac-
tion processes above. However, for the reason of complex
constitutes of essential oil, different planting environments,
harvesting season and extraction methods would lead to dif-
ferent content and quality of oil in the herbs [37,51]. The fact
that there has been no current standard for patchouli oil
would undoubtedly lead up to the quality instability of
preparations.
5.2 Classic preparation variety
Among all P. cablin products, Huoxiang Zhengqi prepara-
tions are the most popular products. According to Table 2,
nine preparations used the dosage based on the modification
of the Huoxiang Zhengqi formula from the TCM classic
Taiping Heji Jufang in Song Dynasty of China, in which
P. cablin was the most important herb, sovereign drug [52] in
TCM principle called Jun Yao in Chinese. According to the
drug standards above and clinical application, these nine
preparations were used to relieve the exterior and regulate
the spleen-stomach functions for clinical symptoms, such
as colds, headaches, dizziness, abdominal pain, vomiting
and diarrhea.
Surprisingly, not only the prescription but also the usage and
amount of P. cablin in these preparations differed, yet with
same therapeutic function. According to Table 2,thevarieties
of products could be divided into two groups based on the
form of P. cablin used. In Huoxiang Zhengqi preparations,
decoction pieces of P. cablin are used in four pharmaceutical
forms, granules, mistura, capsules and pills, whereas P. cablin
essential oil is used in other Huoxiang Zhengqi products.
Although the volatile oil is identified with significant
Table 3. The overview of Guanghuoxiang.
Drug Amount Health Insurance
Medicine List (A or B)
Essential Medicine
List (A or B)
OTC
Jiawei Huoxiang Zhengqi pill 93 * * 46A, 47B
Huoxiang Zhengqi pill 229 229A * 229A
Huoxiang Zhengqi pill (Concentrated pill) 6 6A * 6A
Huoxiang Zhengqi pill (Watered pill) 1 * * A
Huoxiang Zhengqi dropping pill 1 * * A
Huoxiang Zhengqi oral liquid 2 2B * 2A
Huoxiang tincture 5 * * 5B
Huoxiang Zhengqi tincture 215 215A 215 215A
Huoxiang Qushu tincture 2 * * 2B
Huoxiang Zhengqi mistura 21 * * 21A
Fufang Huoxiang tablet 1 * * B
Huoxiang Zhengqi tablet 60 60B * 60A
Huoxiang Qingwei tablet 3 * * 3A
Huoxiang Wanying powder 1 * * A
Huoxiang Zhengqi capsule 39 39B * 39A
Huoxiang Zhengqi soft capsule 2 2B * 2A
Jiawei Huoxiang Zhengqi soft capsule 1 * * *
Huoxiang Qingwei capsule 4 * * *
Huoxiang Qushu soft capsule 7 * * 7B
Huoxiang Zhengqi granule 8 * * 8A
Huoxiang Zhengqi granule 27 27B * 27A
Huoxiang Qingwei granule 1 * * *
Data sources: SFDA Southern Medicine Economic Research Institute.
*There is no statistics data.
18000
16000
14000
12000
10000
8000
6000
4000
2000
0
2006 2007 2008 2009 2010 2011
-15%
-10%
-5%
0%
5%
10%
15%
20%
25%
14527
16246
13284
11739
11418
Sales (thousand yuan)
Growth rate
11903
22.30%
13.16%
2.81%
-4.07%
0
-10.58%
Figure 5. Market performance of guanghuoxiang products
(2006 -- 2011).
Data sources: SFDA Southern Medicine Economic Research Institute.
M. Chen et al.
8Expert Opin. Investig. Drugs [Early Online]
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For personal use only.
pharmacological effects, as the nonvolatile effective compounds
discussed above, it also would not substitute for P. cablin herb
and differ from the decoction pieces. In addition, even with the
same pattern of P. cablin in formula, there are also differences
with regard to the extracting process and usage, such as in cap-
sule the decoction pieces are extracted with steam distillation,
while percolation with 70% ethanol is adopted in tablet.
Beside, the amount of P. cablin in the nine preparations also
varies significantly. Thus, for the reason of this great difference
it would be difficult to achieve the same therapeutic effects
among these nine Huoxiang Zhengqi preparations.
In fact, some unreasonable phenomenons like the problem
above exert in preparations of P. cablin quite commonly.
Basic reasons of these drawbacks would lack of integrated
researches on its material basis, pharmacokinetic behaviour
in vivo and so on when series preparations are produced to
innovate earlier drugs. While dosage form reformation would
not be simple modification on its either drug delivery path-
ways or appearance but comprehensive improvement includ-
ing process technology and suitable dosage. As is known,
different dosage forms would exhibit different rates of drug
release; for instance, it seems oral liquid pharmaceuticals,
without the drug dissolution process in gastrointestinal tract,
would express pharmacologic effects faster than traditional
solid pharmaceuticals. Similarly, different effect-expression
rate of drugs would benefit in more extensive clinical uses,
reflecting in different therapeutic functions. From this,
there is still considerable work to be done to improve the
development of preparations of P. cablin.
6. Market performance analysis
There are 729 different drug products of guanghuoxiang
registered in State Food and Drug Administration of China
(SFDA), including 330 pills, 245 oral fluid agents, 64 tablets,
54 capsules and 36 granules. According to the statistics of
SFDA Southern Medicine Economic Research Institute, there
are 450 drug products in A Health Insurance Medicine List,
130 drug products in B Health Insurance Medicine List and
215 drug products of Huoxiang Zhengqi tincture in Essential
Medicine List.
Based on the statistics of hospital drug procurement in
nine major cities in China (Beijing, Guangzhou, Nanjing,
Chongqing, Chengdu, Xi’an, Harbin, Shenyang and
Zhengzhou) by SFDA Southern Medicine Economic Research
Institute, the market performance of guanghuoxiang drug
products in China is summarized as Figure 5. The total sales
accounted to 11.903 million Yuan sales in 2006 and grew to
14.527 million Yuan in 2011, representing an annual growth
rate of 3.94%.
Moreover, the top three products (Huoxiang Zhengqi
soft capsule, Jiawei Huoxiang Zhengqi pill and Huoxiang
Zhengqi capsule) account for more than 80% market share
of guanghuoxiang products since 2006. As shown
in Figures 6 and 7, Huoxiang Zhengqi soft capsule is the
most popular product since 2006 and has reached sales of
64.6 million Yuan in 2011. Jiawei Huoxiang Zhengqi pill,
as the second popular product, realized growth rate of
9.09% and reached sales of 18 million Yuan in 2011.
7. Conclusions
To summarize, P. cablin is an important traditional medicine in
both Chinese and southeast Asian countries, such as Malaysia
and India, with thousands of years of history to relieve the exte-
rior and dissipate dampness. Its significant bioactivities in anti-
viral activities, antioxidation effect, anti-inflammatory, and
analgesic activities have aroused great interest of researchers.
Based on P. cablin’s chemical composition, pharmacological
effect, medical preparation, as well as market profile reviewed,
P. cablin shows an effective herbal remedy in clinical application.
8. Expert opinion
This paper reviewed above strongly support the point that
P. cablin has beneficial therapeutic potential as an effective
6000
7000
8000
5000
4000
3000
2000
1000
0
2006 2007 2008 2009 2010 2011
15%
25%
10%
20%
-10%
-5%
5%
0%
6460
6900
20.21%
17.14%
15.72%
4390
Sales (thousand yuan)
Growth rate
5080 4900 5740
0
-6.38%
-3.54%
Figure 6. Market performance of Huoxiang Zhengqi Ruan
Jiaonang (2006 -- 2011).
Data sources: SFDA Southern Medicine Economic Research Institute.
2000
2500
3000
1500
1000
500
0
2006 2007 2008 2009 2010 2011
-50%
-40%
-30%
0%
10%
-20%
20%
-10%
1800
1650
1570
1470
2840
Sales (thousand yuan)
Growth rate
1530
9.09%
5.10%
6.80%
-3.92%
-46.13%
0
Figure 7. Market performance of Jiawei Huoxiang Zhengqi
Wan (2006 -- 2011).
Data sources: SFDA Southern Medicine Economic Research Institute.
Analysis of P. cablin from pharmaceutical research to market performances
Expert Opin. Investig. Drugs [Early Online] 9
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For personal use only.
adaptogenic herbal remedy in clinic. With the increasingly
important preventive role of traditional herbal medicine in
some critical illness, such as malignancy [15], SARS [53],H
1
N
1
influenza virus [54], endocrine disease [55], and neurological
disease [56], increasing number of researchers have been enticed
for potential drug candidates for decades [57]. In spite of the
various dosage forms and huge sale of herbal products recently,
most of natural products still fall into embarrassment that lack
in-depth development [58]. In fact, considering the enormous
varieties of herbal medicine in world, there is only few
natural products approved by US FDA [59] and European
Union [60] largely owing to their relaxing standards [61,62],safety
risk [63,64] as well as pharmaceutical design [65].
As such, for P. cablin, some problems are also needed to be
further resolved to improve its better development for human
health. First, few molecular mechanisms of bioactivities of
P. cablin compounds are known, which goes against its fur-
ther clinical application. Although some pharmacological
compounds separated from P. cablin herb has been confirmed
via cell or animal experiments, there is also a lack in investi-
gating mechanism of pharmacological actions and pharmaco-
kinetic behavior in vivo of effective compounds. Actually, the
bioactivity with multiple targets of natural compounds would
be superior compared with chemical medicines, and the trend
of drug research and development would focus on its molecu-
lar mechanism and active targets. Lu et al. [66] set up the tar-
get-- target and drug-- drug networks of drugs approved by
FDA, finding that the multitarget drugs have much more
potential. Hopkins [67] and Csermely et al. [68] assessed that
multitarget drugs would clinically benefit the drug design
and the next paradigm in therapeutics. Additionally, proper
pharmacokinetic behavior, namely whole state in vivo includ-
ing absorption, distribution, metabolism and excretion pro-
cess, would be the prerequisite in the development of drugs
for clinical purposes [69,70], which would refer to biosynthesis,
structural modification and structure-- activity relationship
studies. As far as effective extract or compounds of P. cablin
is concerned, aimless bioactivities would be seldom helpful
in developing it as drug candidates.
Moreover, the qualitative and quantitative standards of
P. cablin essential oil still need to be established to promote
the growing popularity of patchouli oil in drug development,
fragrance manufacture [71], and food supplement [72],
demand-restricted product standards. For the reason of
complex chemical constituents and multiple types of extract
technologies of P. cablin essential oil, quality control would
be dramatically related to the quality and clinical function
of products, and even guide the novel extract techniques and
process condition for optimization of essential oil. To date,
emerging precise analyzers, such as GC-MS and LC-MS,
have been gradually applied to represent its chemical profile,
while the specific bioactive constituents in essential oil screen-
ing is still to be resolved owing to its multi-
component properties. Last, novel drug delivery systems of
P. cablin need to be developed deeply. According to data
in Table 1, all the products containing P. cablin in current
Chinese drug standards belong to traditional drug forms.
Old process technologies and traditional dosage forms result
in the limited clinical uses, reflecting in the dramatic decrease
in market performance of both whole guanghuoxiang prod-
ucts and Huoxiang Zhengqi soft capsule from 2010 to 2011.
In addition to its application in drug development,
P. cablin is also a potential material with viruses’ inhibitive
functions for environmental sanitation [73], especially in trop-
ical and sub-tropical areas of the world with high incidence of
epidemic disease. The ultimate goal of these discussions
herein is to stimulate new studies and development opinions,
by mean of systematic analyses of the pharmaceutical research
and market profiling of P. cablin, respectively.
Declaration of interest
This study was supported by the Macao Science and Techno-
logy Development Fund (077/2011/A3) and the Research
Fund of University of Macau (MYRG 208 (Y2-L4)-
ICMS11-WYT) and UL016/09-Y4/CMS/WYT01/ICMS.
The authors state no conflict of interest and have received
no payment in preparation of this manuscript.
M. Chen et al.
10 Expert Opin. Investig. Drugs [Early Online]
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For personal use only.
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73. Lee CY. Preparation of Chinese herbal
composite recipe used in environmental
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Affiliation
Meiwan Chen*
1
PhD, Jinming Zhang*
1
,
Yunfeng Lai
1
, Shengpeng Wang
1
, Peng Li
1
PhD,
Jian Xiao
3
PhD, Chaomei Fu
2
, Hao Hu
1
PhD &
Yitao Wang
1,4
Author for correspondence
*Both authors have contributed
equally to this work
1
University of Macau,
Institute of Chinese Medical Sciences,
State Key Laboratory of Quality Research in
Chinese Medicine,
Av. Padre Tomas Pereira S.J., Taipa, Macao,
China
Tel: +00 853 83978538; +00 853 83974691;
Fax: +00 853 28841358;
E-mail: haohu@umac.mo; ytwang@umac.mo
2
Professor,
Chengdu University of Traditional Chinese
Medicine,
Pharmacy College,
Chengdu, China
3
Cixi Hospital,
School of Pharmacy,
Wenzhou Medical College,
Wenzhou, China
4
Professor,
University of Macau,
Institute of Chinese Medical Sciences,
Av. Padre Tomas Pereira S.J.,
Taipa, Macao, China
Analysis of P. cablin from pharmaceutical research to market performances
Expert Opin. Investig. Drugs [Early Online] 13
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... cablin) is a perennial aromatic herb belonging to Lamiaceae family. From its Southeast Asia origins, P. cablin has been widely cultivated in southern China, including Guangdong, Guangxi and Hainan provinces, for over 1,000 years (Chen et al., 2013). Many parts of P. cablin plant, especially leaves and stem, are rich in numerous active components, such as sesquiterpenoids and flavonoids and alkaloids. ...
... Hundreds of different drug products from P. cablin have been registered for use by the State Food and Drug Administration of China (SFDA), including various pills, 245 oral fluid agents, tablets, capsules, and granules (Chen et al., 2013). Therefore, P. cablin represents an effective herbal remedy with great application potential in diverse clinical situations. ...
Article
Full-text available
Farnesyl pyrophosphate synthase (FPPS) plays an important role in the synthesis of plant secondary metabolites, but its function and molecular regulation mechanism remain unclear in Pogostemon cablin . In this study, the full-length cDNA of the FPP synthase gene from P. cablin ( PcFPPS ) was cloned and characterized. The expressions of PcFPPS are different among different tissues (highly in P. cablin flowers). Subcellular localization analysis in protoplasts indicated that PcFPPS was located in the cytoplasm. PcFPPS functionally complemented the lethal FPPS deletion mutation in yeast CC25. Transient overexpression of PcFPPS in P. cablin leaves accelerated terpene biosynthesis, with an ~47% increase in patchouli alcohol. Heterologous overexpression of PcFPPS in tobacco plants was achieved, and it was found that the FPP enzyme activity was significantly up-regulated in transgenic tobacco by ELISA analysis. In addition, more terpenoid metabolites, including stigmasterol, phytol, and neophytadiene were detected compared with control by GC-MS analysis. Furthermore, with dual-LUC assay and yeast one-hybrid screening, we found 220 bp promoter of PcFPPS can be bound by the nuclear-localized transcription factor PcWRKY44. Overexpression of PcWRKY44 in P. cablin upregulated the expression levels of PcFPPS and patchoulol synthase gene ( PcPTS ), and then promote the biosynthesis of patchouli alcohol. Taken together, these results strongly suggest the PcFPPS and its binding transcription factor PcWRKY44 play an essential role in regulating the biosynthesis of patchouli alcohol.
... Pharmacological studies have shown that Herba Pogostemonis contains monoterpene, sesquiterpene, and micromolecular alcohol with the functions of antivirus, antioxidation, anti-inflammatory, analgesic activities, and intestinal barrier function protection [2]. ...
Article
Full-text available
Coronavirus disease 2019 (COVID-19), which causes severe respiratory illness, was first reported in Wuhan, China. The etiology of the disease is a new novel coronavirus named severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), which was reported to share the same origin as SARS-CoV, causing severe public health events in 2002. Unlike the SARS-CoV, which was conquered in the early summer of 2003, this virus was still contagious widely and reached a pandemic level. It can still spread fast even if the season’s temperature is raised. Here, we made a model of pneumonia of human coronavirus 229E (HCoV-229E) with damp-heat syndrome treated by Xiangqin Kanggan granules to find a new medicine for treating these kinds of infectious diseases coronaviruses induced.
... More than 50% of patchouli oil is patchouli alcohol (Miyazawa et al., 2000). Patchouli volatile oil is an important ingredient for perfumes, incense, soaps, and other cosmetic products (Fan et al., 2011;Chen et al., 2013). In China, there are two chemical types, called patchouliol-type patchouli and pogostone-type patchouli. ...
Article
Full-text available
Background Pogostemon cablin (Blanco) Benth. also called patchouli, is a traditional medicinal and aromatic plant that grows mainly in Southeast Asia and China. In China, P. cablin is divided into two chemical types: the patchouliol-type and the pogostone-type. Patchouliol-type patchouli usually grow taller, with thicker stems and bigger leaves, and produce more aromatic oil. Methods To better understand the genetic differences between the two chemical types that contribute to their differences in morphology and biosynthetic capabilities, we constructed de novo transcriptomes from both chemical types using the Pacific Biosciences (PacBio) Sequel platform and performed differential expression analysis of multiple tissues using Illumina short reads. Results In this study, using single-molecule real-time (SMRT) long-read sequencing, we obtained 22.07 GB of clean data and 134,647 nonredundant transcripts from two chemical types. Additionally, we identified 126,576 open reading frames (ORFs), 100,638 coding sequences (CDSs), 4,106 long noncoding RNAs (lncRNAs) and 6,829 transcription factors (TFs) from two chemical types of P. cablin . We adopted PacBio and Illumina sequencing to identify differentially expressed transcripts (DEGs) in three tissues of the two chemical types. More DEGs were observed in comparisons of different tissues collected from the same chemical type relative to comparisons of the same tissue collected from different chemical types. Furthormore, using KEGG enrichment analysis of DEGs, we found that the most enriched biosynthetic pathways of secondary metabolites of the two chemical types were “terpenoid backbone biosynthesis”, “phenylpropanoid biosynthesis”, “plant hormone signal transduction”, “sesquiterpenoid and triterpenoid biosynthesis”, “ubiquinone and other terpenoid-quinone biosynthesis”, “flavonoid biosynthesis”, and “flavone and flavonol biosynthesis”. However, the main pathways of the patchouliol-type also included “diterpene biosynthesis” and “monoterpene biosynthesis”. Additionally, by comparing the expression levels of the three tissues verified by qRT-PCR, more DEGs in the roots were upregulated in the mevalonate (MVA) pathway in the cytoplasm, but more DEGs in the leaves were upregulated in the methylerythritol phosphate (MEP) pathway in the plastid, both of which are important pathways for terpenoids biosynthesis. These findings promote the study of further genome annotation and transcriptome research in P. cablin .
... Recently, extensive studies have indicated that patchouli possesses diverse pharmacological activities, including antimicrobial, antioxidative, antitumor, sedative, and gastrointestinal protective activities (Hu et al., 2017;Kim et al., 2019;Xie et al., 2020). Moreover, patchouli is also an economically important aromatic plant producing essential oil, which is widely used in fragrance and cosmetic industries (Chen et al., 2013). ...
Article
Full-text available
Pogostemon cablin (patchouli), an important medicinal and aromatic plant, is widely used in traditional Chinese medicine as well as in perfume industry. Patchouli plants are susceptible to bacterial wilt disease, which causes significant economic losses by reduction in yield and quality of the plant products. However, few studies focus on the pathogens causing bacterial wilt on patchouli. In this study, strain Pa82 was isolated from diseased patchouli plants with typical bacterial wilt symptoms in Guangdong province, China, and was confirmed to be a highly virulent pathogen of patchouli bacterial wilt. Comparative sequence analysis of 16S rRNA gene showed that the strain was closely related to Kosakonia sp. CCTCC M2018092 (99.9% similarity) and Kosakonia cowanii Esp_Z (99.8% similarity). Moreover, phylogenetic tree based on 16S rRNA gene sequences showed that the strain was affiliated with genus Kosakonia . Further, the whole genome of strain Pa82 was sequenced, and the sequences were assembled and annotated. The complete genome of the strain consists of one chromosome and three plasmids. Average nucleotide identity (ANI) and phylogenetic analysis revealed that the strain belongs to Kosakonia cowanii (designated Kosakonia cowanii Pa82). Virulence-related genes of the strain involved in adherence, biofilm formation, endotoxin and other virulence factors were predicted. Among them, vgrG gene that encodes one of the type VI secretion system components was functionally validated as a virulence factor in Kosakonia cowanii Pa82 through construction of Tn 5 insertion mutants and identification of mutant defective in virulence.
... Species like Illicium anisatum, Melissa officinalis L., Myristica fragrans Houtt. (Jaganathan & Supriyanto, 2012), Pogostemon cablin (Chen et al., 2013), Aphanamixis polystachya (Shaikh et al., 2012), Aegle marmelos (L.) Correa (Baliga et al., 2013), Abutilon indicum L. (Sharma et al., 2013), Acorus calamus L. (Avadhani, 2013), Piper betel (Gundala & Aneja, 2014), Pimenta pseudocaryophyllus (Gomes) Landrum (D'angelis & Negrelle, 2014), and Rabdosia japonica var. glaucocalyx (Xiang et al., 2015) have been also known to possess eugenol in considerable amount. ...
Chapter
Eugenol is a volatile phytoconstituent present in various essential oils isolated from different aromatic medicinal plant. Eugenol acts as a natural antioxidant and has been extensively employed for the treatment of different lifestyle-related ailments. Conventionally, it has been endorsed to cure innumerable problems such as diarrhea, bronchitis, hyperlipidemia, hyperglycemia, arthritis, inflammation liver ailments, cancer, cardiovascular, and skin diseases. Eugenol has been acknowledged as GRAS (generally recognized as safe) by WHO (World Health Organization) and has been recognized as nonmutagenic (Khalil et al., 2017; R, 2015). It has been commonly used in the Ayurveda and Chinese primeval medicines systems. In the modern world, main source of eugenol, i.e., clove is mainly cultivated in Indonesia, Zanzibar, India, Pakistan, and Sri Lanka. Owing to wide range of therapeutic potential and practical applications in day-to-day life, eugenol has drawn the attention of numerous scholars and unlocked the doorway of research about its employment as a medication to cure innumerable diseases. Therefore, it is very substantial to represent the research outcomes associated to the beneficial properties of eugenol in order to explicate its mechanisms of action involved in prevention of several lifestyle-related illnesses and its significance for human health.
Article
Patchouli alcohol (patchoulol), a sesquiterpenoid specifically synthesized by herbal plant Pogostemon cablin, has a variety of pharmacological and biological activities and is widely utilized in the medical and cosmetic industries. However, there are few studies on the transcriptional modulation of patchoulol biosynthesis. Some studies have reported that basic leucine zipper (bZIP) transcription factors (TFs) participate in the biosynthesis of plant terpenoids, but there is no report that bZIP TFs are involved in the modulation of patchoulol biosynthesis. This study was conducted to explain the regulation of patchoulol biosynthesis by PcbZIP44, a bZIP TF identified in patchouli for the first time. PcbZIP44 was highly expressed in roots and stems, and its encoded protein was nuclear localized revealed by protoplast subcellular localization experiment. According to the results of the transient dual-luciferase assay and yeast one-hybrid (Y1H) assays, PcbZIP44 can bind to the PcPTS (patchoulol synthase) gene promoter to repress its activity. Overexpression of the PcbZIP44 gene significantly reduced the content of patchoulol and resulted in a significant down-regulation of the PcPTS gene at the transcriptional level. Correspondingly, virus-induced PcbZIP44 gene silencing (VIGS) significantly increased the content of patchoulol and resulted in a significant up-regulation of the PcPTS gene at the transcriptional level. Therefore, these results suggested that PcbZIP44 negatively regulates patchoulol biosynthesis by inhibiting the PcPTS gene in P. cablin.
Article
Pogostemonis Herba (PH) is the dried aerial parts of Pogostemon cablin (Blanco) Benth, which is mainly distributed and used in Asian countries. PH is an aromatic damp-resolving drug in traditional Chinese medicine (TCM), which is usually used for the treatment of vomiting, chest tension, tiredness, abdominal pain, diarrhea, and headache. In this review, the summary of chemical constituents in the aerial parts, biological activities, history of uses, quality control methods, industrial applications, pharmacokinetics and network pharmacology are reported. By collating the chemical constituents of various parts of PH, a total of 174 components were identified, including 66 terpenes, 6 pyrones, 40 flavonoids, 21 phenylpropanoids, 9 steroids, 4 polysaccharides and 28 others. Pharmacological research has found that PH possesses multi-pharmacological activities, including regulating the gastrointestinal tract, inhibition of pathogenic microorganisms, and anti-inflammation, which provide more scientific interpretation for the clinical usage of PH. In addition, the shortcomings of the current research on PH and the recommendation of future studies on PH are analyzed. We hope this review can provide some insight for further research and applications of PH in future.
Article
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Pogostemon cablin Linn., commonly known as patchouli is an aromatic plant with immense use in aroma and perfumery. The purpose of this study was to examine and compare the chemical composition, antimicrobial activity, and various biological activities of Pogostemon cablin Linn flower and leaf essential oils. The compositional analysis was carried out using GC/MS, while standard biological experiments were used to determine the pharmacological potential of both the essential oils. Patchouli alcohol (27.52%, 44.52%) was found to be the major compound followed by caryophyllene (18.23%, 12.86%) for both flowers and leaves essential oil (EO) respectively. P. cablin flower (PCFEO) and leaf essential oil (PCLEO) exhibited weak to strong antimicrobial activities against selected microbial strains. The mitotic index for flower and leaf EO was 14.38% and 15.20% respectively. PCFEO and PCLEO had chromosomal aberrations of 9.0% and 9.60%, respectively. Both PCFEO and PCLEO had substantial antioxidant activity, with PCLEO exhibiting the highest antioxidant activity (IC 50 = 1.31 µg/mL). Highest anti-inflammatory activity was exhibited by PCLEO (IC 50 = 4.49 µg/mL). Similarly, the anti-diabetic ability of PCLEO (IC 50 = 14.19 µg/mL) was greater than the PCFEO (IC 50 = 15.60 µg/mL). The PCLEO (IC 50 = 7.42 µg/mL) and PCFEO (IC 50 = 12.67 µg/mL) both exhibited better anticholinesterase activity than galanthamine (IC 50 = 22.16 µg/mL). Better tyrosinase inhibitory activity was shown by PCLEO with IC 50 = 4.03 µg/mL than PCFEO IC 50 = 4.44 µg/mL. Apart from their antimicrobial activity, the PCLEO was found to outperform both PCFEO as well as the standards in their respective assays. Thus, the present study affirmed the wide application aspects of patchouli essential oil apart from its aromatic application.
Article
Four new patchoulol-type sesquiterpenoids, including 6α,9β-dihydroxypatchoulol 6-O-β-d-glucopyranoside (1), 6α-hydroxypatchoulol 6-O-β-d-glucopyranoside (2), 3α,9β-dihydroxypathoulol (3), and 4β-hydroxynorpatchoulol 4-O-β-d-glucopyranoside (10), were isolated from the roots of Pogostemon cablin (Blanco) Benth, together with eleven known sesquiterpenoids. Their structures were elucidated on the basis of extensive NMR spectral and high resolution mass spectrometry analysis. This is the second report of patchoulol glucopyranoside from P. cablin and compound 10 represented as the first example of nor-patchoulol glucopyranoside. The anti-influenza virus activities of 1–10 against A/WSN/33/2009 and A/Puerto Rico/8/1934 strains (tamiflu resistant viruses) were evaluated. Compounds 2β,12-dihydroxypathoulol (5) and (5R)-5-hydroxypatchoulol (8) exhibited moderate anti-influenza activity against A/WSN/33/2009 strain with EC50 value of 52.7 μM and 49.6 μM (positive control oseltamivir, EC50 = 6.75 μM). Compounds 8 and pogostol (12) showed potent anti-influenza activity against A/Puerto Rico/8/1934 strain with EC50 values of 3.06 μM and 0.07 μM, respectively, versus the postive control (amantadine, EC50 = 67.9 μM).
Chapter
Plants are the unique source of bioactive compounds. Microbial infections like bacterial, viral, parasitic, and fungal are very common worldwide. The uses of modern medicine face a challenge of resistance and major side effects also. To overcome these problems, herbal medicine is a choice. Globally, the acceptance of herbal medicine increases day by day because of valuable therapeutic effects with fewer side effects. Thymoquinone is a major bioactive compound found in Nigella sativa belonging to the family Ranunculaceae. The advantage of this compound is that it has very little toxicity with several pharmacological effects. Eugenol, the source, has been reported in several plants like clove buds, cinnamon bark, and leaves, tulsi leaves, turmeric, pepper, ginger, oregano, and thyme high concentrations found in clove. Both compounds have revealed antimicrobial properties. From ancient times, these plants were used as curative and preventive to control the microbial infection. Traditional herbal medicine has a drawback that is less bioavailability leads to delayed therapeutic effects. The application of nanotechnology in pharmaceutical overcomes such disadvantages. Scientists developed nanoherbal formulations that are very effective to control microbial disease. Nanoformulations have several advantages like high therapeutic value and high bioavailability, and it can be achieved by novel drug formulation.
Article
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The present study was conducted to investigate the antioxidant and radical scavenging activities of essential oils of four Lamiaceae plants i.e. Pogostemon cablin, Lavandula angustifolia, Melissa officinalis, and Salvia officinalis native to Pakistan. The essential oil contents from the aerial parts of P. cablin, L. angustifolia, M. officinalis and S. officinalis were found to be 1.98, 0.58, 0.25 and 0.46%, respectively. The principal chemical constituent established in P. cablin L. angustifolia, M. officinalis, and S. officinalis essential oils, were patchouli alcohol, linalool, citronellal, and 1,8-cineol, respectively. The antioxidant activity was evaluated by scavenging of 2,2-diphenyl-1-picryl hydrazyl radical (DPPH ●), percent inhibition of linoleic acid oxidation and bleaching β-carotene in linoleic acid system. The essential oils possessed appreciable antioxidant and radical scavenging activities revealing potential for therapeutic applications.
Article
OBJECTIVE: To search some new natural skin antifungal drugs and to exploit the aromatic plant resources. METHOD: The antifungal screening and the major chemical ingredients of the essential oils extracted from the leaves of Agastache rugosa and Pogostemon cablin (patchouli) were studied by media dilution against twelve dermatophytes and opportunistic fungi and by GC-MS technique. The inhibitory activity of three patchouli oils of various geographical origins (China, India and Indonesia Java) were compared. RESULTS: These oils inhibited totally the growth of dermatophytes, but had extremely weak effect against opportunistic fungi in vitro. The Chinese patchouli oil was the most efficacious with a MIC value of 50 ~ 400 μl·L-1, its principal components were patchouli alcohol, α-bulnesene andpatchoulene. The oil of A. rugosa had a poor antifungal effect with MIC of 700 ~ 1000 μl·L-1, it is mainly composed of the menthone derivatives. CONCLUSION: This study suggested that the patchouli oil had specific antifungal effect against dermatophysis with good prospects.
Article
Pachypodol, ombuine, apigenin, rhamnetin, apigetrin and a new flavone, apigenin 7-O-β-D (-6"-p-coumaroyl)-glucoside, were isolated from the aerial part of patchouli, Pogostemon cablin (Labiatae). These compounds were identified by analysis of various spectral data.
Article
Four new patchoulol derivatives, 8α,9α-dihydroxypatchoulol (1), 3α,8α-dihydroxypatchoulol (2), 6α-hydroxypatchoulol (3), and 2β,12-dihydroxypatchoulol (4), were isolated from the aerial part of Pogostemon cablin (Labiatae), together with nine known compounds, sesquiterpenoids 5–8 and flavonoids 9–13. Their structures were elucidated by detailed spectroscopic analysis, using 1D- and 2D-NMR techniques.
Article
Patchouli essential oil is an important raw material for the perfume and cosmetics industries, besides being used as a natural additive for food flavoring. Patchoulol and α-patchoulene are important compounds of patchouli essential oil, and their concentrations are directly proportional to the quality of the oil. Nowadays, the usual method employed to obtain patchouli essential oil is steam distillation; however, this causes thermal degradation of some oil compounds. In this study patchouli essential oil was extracted with supercritical carbon dioxide (scCO2) under different conditions of pressure (8.5 and 14 MPa) and temperature (40 and 50 °C) and also by steam distillation to compare the extraction methods. It was demonstrated that the extraction with supercritical carbon dioxide provided a higher yield and a better quality of patchouli essential oil.
Article
Techniques are described for the micro-analysis of the free volatile sesquiterpenes in plant tissue by direct-loading gas liquid chromatography. Evidence is presented for the accumulation of sesquiterpenes, not only in the external glandular trichomes, but also in specialized internal accumulatory cells. The morphology and development of these external and internal structures are described as seen under light and electron microscopy. Also, while the apical dome of the stem neither shows any specialized accumulatory structures nor contains any detectable sesquiterpenes, the second pair of primordial leaves has glandular trichomes and a sesquiterpene concentration approximately twelve times higher than that in any other part of the plant.