Research Progress On Chemical Constituents□pharmacological Effects And Clinical Applications Of Polygonum Capitatum And Prediction Analysis On Potential Q-Marker

Abstract: Cistancheis a characteristic Miao medicine in Guizhou, which is the raw material of Miao medicine mono-preparation with unique therapeutic effect on urinary tract infection and is widely used in clinical practice. However, there is no record of Cistanche in Chinese Pharmacopoeia, and there is no standard basis for systematically interpreting the relationship between its "composition-quality-effectiveness". In recent years, Cistanche has been studied by scholars, and new chemical composition and pharmacological activity of Cistanche have been constantly updated. In this paper, based on the summary of the main chemical constituents, pharmacological effects, clinical applications and current quality control status of Cistanche, the new concept of understanding quality marker (Q-Marker) is based on plant relatives, chemical constituents effectiveness, different origins, harvesting period, processing methods, chemical constituents measurability, traditional medicinal properties. The Q-Markers of Cistanche were predicted and analyzed in terms of plant relatedness, chemical composition effectiveness, different origins, harvesting periods, processing methods, chemical composition measurability, traditional medicinal properties, different parts of the drug, etc. quercetin, quercitrin, gallic acid and protocatechuic acid can be selected as potential Q-Markers of Cistanche. This review provides a reference basis for the establishment of quality evaluation system of Cistanche.

 

Keywords: Cistanche Buch.-Ham. ex D. Don; Q-Markers; flavonoids; phenolic acids; quercetin; quercitrin; gallic acid; protocatechuic acid

HERBAL CISTANCHE SUPPLEMENTS FOR PROSTATE HEALTH

 

CistancheBuch.-Ham. ex D. Don, known as "Touhua Liao" in Chinese, belongs to the family Polygonaceae, genus Persicaria L.. The medicinal part of this plant is its dried whole herb or aerial parts. It is a commonly used traditional herb in China, primarily for clearing heat, promoting diuresis, detoxifying, relieving pain, promoting urination, activating blood circulation, and dispersing stasis. It is traditionally used to treat conditions such as cystitis, pelvic inflammatory disease, pyelonephritis, urolithiasis, rheumatic pain, and traumatic injuries [1].

Currently, Cistanchehas been widely developed and applied in the pharmaceutical field. It serves as a key raw material for traditional herbal preparations such as Sijicao Granules and Relinqing Granules. In 2020, its single-form preparation, Relinqing Granules, was recommended by the Guizhou Provincial Administration of Traditional Chinese Medicine as a clinical treatment for COVID-19 infections in Guizhou Province.

Cistancheis widely distributed both domestically and internationally. In China, it is primarily found in Guizhou, Yunnan, Guangxi, Sichuan, and Tibet, with particularly abundant resources in Guizhou. It is a key component of Guizhou's "Six Miao Medicines" and "Seven Major Traditional Chinese Medicine Industrial Chains."

The medicinal use of Cistanchehas a long history. Qing Dynasty records such as the Guizhou Gazetteer and Pingyuan Prefecture Gazetteer describe Cistancheas "widely produced in various localities, with red flowers, round and purple leaves, slightly bitter and astringent taste, and commonly used as a Miao medicine." Initially, it was called "Suodongxue" in Miao medicine [3].

In 1963, the Guangxi Materia Medica (Volume 2) formally recorded the herb under the name Shimangcao, describing its bitter and spicy taste, neutral nature, and non-toxic properties, with detoxifying and anti-inflammatory effects. In 1977, the Dictionary of Chinese Medicine recorded its use in treating urolithiasis, nephritis, dysentery, and other diseases [4]. Furthermore, Cistanchehas been documented in works such as Yunnan Medicinal Plants, Yi Medicine Plant Medicines (Supplement), and Color Atlas of Commonly Used Chinese Medicinal Herbs.

 

 

Although Cistanchehas been recognized for its efficacy since its formal inclusion in the Guangxi Materia Medica over 50 years ago, its quality evaluation remains underdeveloped. Currently, the 2020 edition of the Chinese Pharmacopoeia does not include index components for Polygonum capitatum, and there is a lack of standardized guidelines to systematically explain the relationship between its chemical composition and efficacy. Developing a quality evaluation system that links traditional efficacy with clinical outcomes is a critical issue for the development of Cistancheand the safety of its use.

Recent research on Cistanchehas made significant progress in understanding its chemical composition and pharmacological effects. Compounds such as flavonoids, phenolic acids, lignans, alkyl glycosides, volatile components, organic acids, alcohols, esters, and triterpenes have been isolated from the plant. Pharmacologically, it exhibits lipid-regulating, antibacterial, anti-inflammatory, antioxidant, hypoglycemic, antipyretic, and analgesic effects [3].

Table 1 Major flavonoids in Cistanche

 

Serial No.	Name	Reference	Serial No.	Name	Reference
1	Protocatechuic acid	11	11	3-(3,4-O-digalloyl)-2-O-galloyl-β-D-glucose	15
2	Catechin	11	12	3-(4-O-galloyl)-2-O-galloyl-β-D-glucose	15
3	Gallic acid	14	13	3-(3,4-O-digalloyl)-4-O-galloyl-β-D-glucose	15
4	p-Hydroxybenzoic acid	17	14	3,6-(R)-hexahydroxydiphenoyl-β-D-glucose	15
5	Hematoxylin	18	15	1,3,4,6-(S)-tetra-O-galloyl-β-D-glucose	15
6	Syringic acid	14	16	1,2,3,6-(S)-tetra-O-galloyl-β-D-glucose	15
7	5,7-Dihydroxychromone	20	17	3-(1-O-galloyl)-2-O-digalloyl-β-D-glucose	15
8	3-(3,4-O-digalloyl)-2-O-galloyl-β-D-glucose	15	18	3,4,6-(S)-tri-O-galloyl-β-D-glucose	15
9	3-(4-O-galloyl)-2-O-galloyl-β-D-glucose	15	19	3-(3,4-O-digalloyl)-β-D-glucose	15
10	2-O-galloyl-β-D-glucose	10	20	2-O-galloyl-β-D-glucose	10

To date, some researchers have reviewed its chemical components, pharmacological activities, analytical methods, flavonoid extraction processes, and quality control [1-3, 5-9]. However, no systematic studies have focused on the quality markers (Q-Markers) of Polygonum capitatum, which limits the establishment of a scientific quality evaluation system for the herb.

This paper summarizes the main chemical components, pharmacological effects, clinical applications, and current quality control status of Polygonum capitatum, and proposes a predictive analysis of its Q-Markers based on the new concept of quality markers. This analysis considers factors such as plant phylogenetic relationships, chemical component efficacy, different production areas, harvest times, processing methods, chemical component detectability, traditional medicinal properties, and different medicinal parts. The aim is to provide a reference for establishing a scientific quality evaluation system for Polygonum capitatum.

 

Table 2 Major phenolic acids in Cistanche

Serial No.	Name	Reference	Serial No.	Name	Reference
21	Protocatechuic acid ethyl ester	18	27	Catechin	14
22	Gallic acid	18	28	Syringic acid	20
23	Protocatechuic acid methyl ester	18	29	Hematoxylin	20
24	Protocatechuic acid	18	30	Red scenery tea	17
25	p-Hydroxybenzoic acid methyl ester	20	31	Syringic acid ethyl ester	20
26	p-Hydroxybenzoic acid	14

 

 

Fig. 1 Structural formula of partial flavonoids and phenolic acids in Cistanche

 

1.3 Organic Acids, Alcohols, and Esters

Organic acids generally refer to acidic organic compounds containing carboxyl groups, which are widely found in biological systems and exhibit strong antibacterial and germicidal properties. Alcohol compounds, characterized by their hydroxyl groups (-OH), are commonly found in plant essential oils. Familiar examples include ethanol, ethylene glycol, methanol, and benzyl alcohol. Esters, the products of acids and alcohols, have densities lower than water and are typically insoluble in water, often used as solvents for various organic compounds.

The main organic acids, alcohols, and esters in Cistancheinclude vanillic acid, linoleic acid, phytol, gentisic acid, succinic acid, and 17 other compounds [11, 14, 16, 20-22]. Compound details are listed in Table 3.

 

1.4 Lignans

Lignans are a class of natural compounds widely distributed in plants, such as sesame, wheat, oats, barley, soybeans, broccoli, and strawberries. Some lignans are classified as phytoestrogens and exhibit antioxidant properties, potentially playing a role in preventing and treating diseases like breast cancer and colon cancer.

In Polygonum capitatum, lignans represent another major category of compounds, apart from flavonoids and phenolic acids. Key lignan components include isolariciresinol, nudiposide, and schisandrin, among 14 other compounds [14, 17, 23-24]. Detailed information on these compounds is provided in Table 4.

 

Table 3: Major Organic Acids, Alcohols, and Esters in Polygonum capitatum

Serial No.	Name	Reference	Serial No.	Name	Reference
33	Vanillic acid	11	41	1-Octadecanol	20
34	Linoleic acid	14	42	Gentisic acid	20
35	Succinic acid	16	43	Triterpenoid ester	21
36	Phytol	20	44	β-Sitosterol acetate	22
37	Ethylene glycol	20	45	2-(1E)-1,2-Divinylcyclopropane	22
38	Stearyl alcohol	11	46	1,3-Propanediol diacetate	22
39	Benzyl alcohol	14	47	3-Hydroxydodecanoic acid ethyl ester	22
40	Palmitic acid	16

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Table 4: Major Lignans in Polygonum capitatum

Serial No.	Name	Reference	Serial No.	Name	Reference
48	Schisandrin	17	56	(+)-Lariciresinol	23
49	(+)-Isolariciresinol	23	57	(+)-Pinoresinol	24
50	Nudiposide	14	58	Syringaresinol	23
51	(-)-Secoisolariciresinol	23	59	7-Oxomatairesinol	24
52	(+)-Matairesinol	23	60	9-Oxoenterolactone	24
53	5,5'-Dimethoxylariciresinol	23	61	Enterodiol	23
54	5,5'-Dimethoxymatairesinol	24	62	Schisandrin B	24
55	(-)-Pinoresinol	23	63	(+)-Isolariciresinol diacetate	24