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ฟ้าทะลายโจร

Botanical Names

  • Andrographis paniculata (Burm. f.) Wall ex. Nees

Common Names

Thai ฟ้าทะลายโจร (Fa ta lai jone) [1], [2]  น้ำลายพังพอน (Nam Lai Pang Pond) [3]
English King of bitter [4]
Malay  Hempedu bumi [5], [3], [4]
Indonesia Sambiloto or Sambiroto [5]
Chinese Chuan-Xin-Lian, Chunlianqialio, Yiqianxi, Si-Fang-Lian [3]
Indian Kalmegh [4], Kiryato, Maha-tikta, Bhunimba [3]
Japanese Senshinren [3], [4]
Scandinavian Green Chiretta [3]

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Family

  • Acanthaceae

 

Morphology

Andrographis paniculata is an annual herb, extremely bitter in taste in every part of the plant body. It grows erect to a height of 30–110 cm in moist shady places with glabrous leaves and white flowers with rose-purple spots on the petals. The stem dark green, 0.3–1.0 m in height, 2–6 mm in diameter, quadrangular with longitudinal furrows and wings on the angles of the younger parts, slightly enlarged at the nodes; leaves glabrous, up to 8.0 cm long and 2.5 cm broad, lanceolate, pinnate; flowers small, in lax spreading axillary and terminal racemes or panicles; capsules linear-oblong, acute at both ends, 1.9 cm × 0.3 cm; seeds numerous, sub quadrate, yellowish brown. [3]

ฟ้าทะลายโจร

Figure 1. a Andrographis paniculata herb in pod stage with terminal or axillary panicles. b Young plant: aerial and underground parts of AP. c Fruit of AP in capsule form. d Opened capsule. e Rugose seeds of AP inside the fruit. f flowering plant with a small flower. g A flower with opened anther and pollen grains

Geographical Distributions

Andrographis paniculata is distributed in tropical Asian countries. [6] It grows abundantly in south-eastern Asia, i.e. , India, Sri Lanka, Pakistan, Java, Malaysia, and Indonesia, while it cultivated extensively in India, China, and Thailand. [3] It can be found in a variety of habitats, e.g. plains, hill slopes, wastelands, farms, dry or wet lands, sea shores and even road sides. Native populations of plants are spread throughout South India and Sri Lanka which perhaps represent the centre of origin and diversity of the species. [6] It’s a well-known medicinal plant of China, India, Thailand, and Southeast Asia. [7] The herb is also available in northern parts of India, Java, Malaysia (including Penang, Malacca, Pangkor Island which is south of Penang and parts of Borneo), Indonesia, the West Indies (including Jamaica, Barbados and the Bahamas) and elsewhere in the Americas where it is probably an introduced species. The species also occurs in Hong Kong, Brunei, and Singapore, etc. [6]

Chemical Constituents

The aerial parts of the plant (leaves and stems) are used to extract the active phytochemicals. [3] Phytochemical investigations on Andrographis paniculata have revealed the presence of a large number of flavonoids, labdane diterpenoids, stigmasterols and xanthones. Labdane diterpenoids are the major constituents of Andrographis paniculata and can be isolated in free and glycoside forms. Examples of the labdane diterpenoids include andrographolide and andrographiside, neoandrographolide, 6′-acetylneoandrographiside, 14-deoxy-11, 12-didehydroandrographolide, 14-deoxy-11,12-didehydroandrographiside, 14-deoxyandrographolide, 14-deoxyandrographiside, andrographanin andropanoside, isoandrographolide andrographatoside, andropanolide and bis-andrographolides A, B, C and D. Several flavonoids have been isolated from Andrographis paniculata, including the rarely occurring 2′-oxygenated flavonoids, such as 5-hydroxy-7,8,2′-trimethoxy-flavone, 5,2′-dihydroxy-7,8-dimethoxy-flavone, 5-hydroxy-7, 8-dimethoxy-flavone, 5-hydroxy-7,8-dimethoxyflavanone and andrographidine A. To date, only the biological activities of andrographolide, 14-deoxy-11,12-didehydroandrographolide and neoandrographolide have been investigated in any detail; the activities of the other andrographolide derivatives remain largely unknown. [8] The primary bioactive component of the medicinal plant Andrographis paniculata is andrographolide. Andrographolide [C20H30O5; (3-[2-{decahydro-6-hydroxy-5-(hydroxymethyl)-5,8α-dimethyl-2-methylene-1-napthalenyl}ethylidene]dihydro-4-hydroxy-2(3H)-furanone)] is a colorless crystalline bicyclic diterpenoid lactone and has a very bitter taste.) It presents in all parts of the plant, maximally in the leaves (>2%). [3] Although andrographolide is not very soluble in water, it is soluble in acetone, chloroform, ether, and hot ethanol. Crystalline andrographolide was reported to be highly stable, over a period of three months. A simple and rapid method for isolating andrographolide from the leaf of A. paniculata is extraction using a 1:1 mixture of dichloromethane and methanol and then isolated the andrographolide directly from the extract by performing recrystallization. The purity of the compound has been evaluated with thin-layer chromatography (TLC), UV absorption spectrum, high-performance liquid chromatography (HPLC), liquid chromatography-mass spectrometry (LCMS), and differential scanning calorimetry (DSC), which revealed the melting point of andrographolide to be 235.3 °C. [9]

Standard criteria of both Fa-Tha-Li raw material and capsules are stated in Thai Herbal Phamacopoeia. This text refers to “Fa-Tha-Li or Andrographis herb” as the aerial parts of Fa-Tha-Li which contain not less than 6% of total lactones, calculated as andrographolide. Fa-Tha-Li capsules contain an amount of powdered Fa-Tha-Li (Andrographis herb) equivalent to not less than 80.0% and not more than 120.0% of the labeled content of total lactones, calculated as andrographolide. [10]

King-of-bitter

Figure 1. Chemical constituents of Andrographis paniculata. (a) Andrographolide (14a-OH, R = H) andrographiside (14a-OH, R = glc); (b) 14-deoxy-11,12-didehydroandrographolide (R = H), 14-deoxy-11,12-didehydroandrographiside (R = glc); (c) neoandrographolide (R = glc), 6’-acetylneoandrographolide (R = glc-6’-Ac); (d) 14-deoxyandrographolide (R = H), 14-deoxyandrographiside (R = glc); (e) isoandrographolide; (f) andrographanin (R1 = R2 = R3 = H), andropanoside (R1 = OH, R2 = H, R3  = b-D-Glc); (g) andrographatoside; (h) andropanolide; (i) bisandrographolide A, B and C; (j) bisandrographolide D; (k) 5-hydroxy-7,8-dimethoxyflavanone (R = H), andrographidine A (R = glc); and (l) 5-hydroxy-7,8,2’-trimethoxy-flavone (R1 = H, R2 = OMe, R

3 = H), 5,2’-dihydroxy-7,8-dimethoxy-flavone (R1 = R3 = H; R2 = OH), 5-hydroxy-7,8-dimethoxy-flavone (R1 = R2 = R3 = H), 5-hydroxy-3,7,8,2’-tetramethoxyflavone (R1 = R2 = OMe, R3 = H). [8]

Plant material of interest: dried aerial parts

  • General appearance

Mixture of broken, crisp, mainly dark green lanceolate leaves and quadrangular stems; capsule fruit and small flowers occasionally found. Stem texture fragile, easily broken; leaves simple, petiole short or nearly sessile, lanceolate or ovate-lanceolate, with acuminate apex and cuneate-decurrent base, lamina crumpled and easily broken. [11] 

  • Organoleptic properties

Odour: slight, characteristic; taste: intensely bitter. [11] 

  • Microscopic characteristics

Leaf upper epidermis: stomata absent, glandular trichomes present, unicellular and multicellular trichomes rare, cystoliths fairly large; lithocysts large (27–30 mm thick, 96–210mm long and up to 49mm wide); columnar palisade cells; collenchyma in midrib beneath epidermis; parenchyma cells spongy; vascular bundles of lignified xylem in the upper part and lignified phloemin the lower part; spiral, scalariform and reticulate vessels. Leaf lower epidermis: a layer of wavy-walled cells; stomata diacytic; trichomes up to 36mm in diameter and 180 mm long, and cystoliths present. Stem: epidermis has glandular and non-glandular trichomes. Collenchyma dense at the corners of stems; parenchyma contains chloroplastids. Endodermis composed of a layer of thick-walled cells. Wood with spiral, scalariform and pitted xylem vessels; pith composed of large parenchyma cells. Small acicular crystals of calcium oxalate occur in the pith and cortical cells of stem and leaf. [11] 

  • Powdered plant material

Leaf fragments in surface view show upper epidermis with underlying palisade and cystoliths, lower epidermis with underlying palisade cells with stomata, cystoliths and glandular trichomes. Leaf fragments in sectionalview show upper epidermis with palisade cells, spongy parenchyma cells, vascular bundles; and lower epidermis with bundles of xylem associated with fibres; fragments of spiral, scalariform, reticulate and pitted vessels; fragments of epidermal cells from midrib; fragments of parenchyma cells in transverse and longitudinal sections. Bundles of fibres. Fragments of epidermal cells from stem with stomata, cystoliths and glandular trichomes. Scattered cystoliths; scattered unicellular and multicellular trichomes, mostly from epidermal cells in fruit walls; scattered glandular trichomes from bundles of fibres in fruit wall; scattered pollen grains. [11]

  • Powder Microscopy

The dried leaves, root and stem of Andrographis paniculata were analyzed for powder characteristics. Microscopic examination showed fragments of leaf epidermis with diacytic, stomata (Figure 8g) and fairly large cystoliths in upper and lower epidermis (Figure 8 and 8f). Stem and root powder showed abundant pyramidal calcium oxalate crystals (Figure 8c).Vessel elements with bordered pits and intervessel pitting in alternate position (Figure 8b) and lignified fibers with pointed ends (Figure 8d) were observed. Fragment of parenchymatous tissues of the cortex (Figure 8h) were also observed. [12]

Powder-microscopy

Figure 8. Powder microscopy of stem showing cystoliths in parenchymatous cells (×10).

  • Fluorescence Analysis

The use of fluorescence can be very useful adjunct to botanical pharmacognosy, since it can be applied as rapid and easy test to verify certain indentifications of the botanicals. When exposed to the day light, root powder of Andrographis paniculata was found to be white color, stem powder was green and leaf powder was found to be of dark green color. Powder of whole plant mixture was found to be light green color. The Fluorescence property of the powdered drug extracts taken in different solvent systems was analyzed under UV light (long and short). Specimens were recorded as either fluorescent (with color and intensity) or not fluorescent and their responses under UV light are presented in Table 2. [12]

Table 2. Fluorescence properties of the extract of root, stem and leave of Andrographis paniculata in various solvents.

Solvent

Under UV (256 nm)

Under UV (366 nm)

(color & intensity)

Aqueous NFS, L, R milky whiteS, NFL, R
Methanol NFS, L, R whiteS, milky whiteL, R
Ethyl Alcohol NFS, L, R pink- orangeS, L, R
Acetone NFS, L, R

(medium) pinkS, (high) pinkL,

milky whiteR

Chloroform NFS, L, R whiteS, R NFL
Ethyl acetate NFS, L, R

(medium) pinkS, (high) pinkL,

milky whiteR

Benzene NFS, L, R (light) pinkS, (high) pinkL, NFR
Toluene NFS, L, R

(medium) pinkS, (high)

pinkL, NFR

Cyclohexane NFS, L, R (light) pinkS, L, NFR

NF = not fluorescent R = extract of root, S = extract of stem, L = extract of leaf

General identity tests

Macroscopic and microscopic examinations, chemical tests, and thin-layer chromatography for the presence of diterpene lactones. [11]

 

Purity tests

  • Microbiological

Tests for specific microorganisms and microbial contamination limits are as described in the WHO guidelines on quality control methods for medicinal plants. [11]

 

  • Chemical

Not less than 6% of total diterpene lactones, calculated as andrographolide. [11]

 

  • Foreign organic matter

Not more than 2%. [11]

 

  • Acid-insoluble ash

Not more than 2%. [11]

 

  • Water-soluble extractive

Not less than 18%. [11]

 

  • Alcohol-soluble extractive

Not less than 13% using 85% ethanol. [11]

 

  • Loss on drying

Not more than 10%. [11]

 

  • Pesticide residues

The recommended maximum limit of aldrin and dieldrin is not more than 0.05 mg/kg. For other pesticides, see the European pharmacopoeia, and the WHO guidelines on quality control methods for medicinal plants and pesticide residues. [11]

 

  • Heavy metals

For maximum limits and analysis of heavy metals, consult the WHO guidelines on quality control methods for medicinal plants. [11]

 

  • Radioactive residues

Where applicable, consult the WHO guidelines on quality control methods for medicinal plants for the analysis of radioactive isotopes. [11]

 

  • Other purity tests

Total ash test to be established in accordance with national requirements. [11]

 

Plant Part Used

  • Leaf and root [3]

 

Traditional uses

Andrographis paniculata has been used to treat various diseases for centuries in China, India and Malaysia. Historically, it was used during the Indian flu epidemic in 1919 and was credited with reversing the spread of the disease. The India Herbal Pharmacopoeia and World Health Organization (WHO) monographs note that Andrographis paniculata can be used to treat bacterial dysentery, carbuncles, colitis, tuberculosis, malaria, herpes, ulcer and venomous snake bites. In south-east Asian countries, such as Malaysia and Thailand, the plant has been used to treat fever, the common cold and diabetes. Overall, Andrographis paniculata has a broad range of pharmacological properties, including hepatoprotective, hypoglycaemic, cardioprotective, anti-inflammatory, immunostimulatory and anticancer activities. [8] Mostly the leaves and roots have been traditionally used over the centuries for different medicinal purposes in Asia and Europe as a folklore remedy for a wide spectrum of ailments or as an herbal supplement for health promotion (Table 1). The Indian Pharmacopoeia narrates that it is a predominant constituent of at least 26 Ayurvedic formulations.  In traditional Chinese medicine, it is an important “cold property” herb used to rid the body of heat, as in fevers, and to dispel toxins from the body. In Scandinavian countries, it is commonly used to prevent and treat the common cold. In Thailand, this plant was selected by the Ministry of Public Health as one of the medicinal plants to be included in “The National List of Essential Drugs A.D. 1999” (List of Herbal Medicinal Products). [3]