Justicia procumbens is a slender, often tufted, prostrate or ascending, branched annual. Stems are 10 to 40 centimeters long. Leaves are elliptic to oblong-ovate or ovate, 7 to 20 millimeters long, 5 to 20 millimeters wide, obtuse at both ends, and entire or with slightly crenated at the margins. Flowers are pink, 6 to 7 millimeters long, and borne in terminal, rather dense cylindric spikes 1 to 5 centimeters long and about 5 millimeters in diameter. Bracts and calyx-teeth are green, linear-lanceolate, and hairy. Fruit is slightly hairy and about 4 millimeters long.
- In open places at low and medium altitudes, from the Batan Islands and northern Luzon to Mindanao, in most islands and provinces.
- Also in China and southward to Australia.
- Contains a bitter alkaloid.
- Study has reported arylnaphthalene lignans as major components; some have shown antiviral and antitumor activities.
- Phytochemical studies yielded justicidin-C and justicidin-D.
- Fractionation studies isolated five 2,3-naphtalide lignans: justicidin-A, neojusticin A, diphyllin, justicidin-D, neojusticin-B and justicidin-E.
- Study yielded three new lignans, Pronaphthalide A, Procumbiene, and Procumbenoside, together with Juspurpudin, a novel natural product, and twelve other known lignans. (see study below) (14)
• Study of whole plant yielded four new lignan glycosides, procumbenosides I, K, L, and M, together with cleistanthin B and five over known arylnaphthalene lignan glycosides. (16)
• Fractionation of the ETOH extract of J. procumbens isolated nine known arylnaphthalide lignans, neojusticin A (1), justicidin B (2), justicidin A (3), taiwanin E methyl ether (4), neojusticin B (5), chinensinapththol methyl ether (6), taiwanin E (8), chinensinaphtho (9), and diphyllin (10), and a new arylnaphthalide lignan characterized as 4'-demethylchinensinaphthol methyl ether (7). (see study below) (17)
• Study of whole plant isolated a new neolignan, named (7'S,8'R)-5,3'-dimethoxy-4,4',9'-etrihydroxy-2-8',9-O-7'neolignan (1), along with two known compounds, secoisolariciresinol (2) and lariciresinol (3). (18)
• Study isolated a new cyclopeptide alkaloid, justicianene A (1) and a new lignan glycoside, procumbenoside H (2). (see study below) (20)
• Study of whole plant isolated one new lignan, rostellulin A (1), four known lignans, justin B (2), justicidin C (3), clinaphthalide A (4), and justicidin A (5), and four known triterpenoids, ursolic acid (6), euscaphic acid (7), 2a-hydroxyursoolic acid (8), and tormentic acid (9). (see study below) (21)
• Study of ethyl acetate and n-butanol extracts of the plant isolated six compounds, identified as justicidin A (1), neojusticin B (2), justicidin B (3), procumbenoside A (4), uracil (5), and procumbenoside E (6). (25)
• Study of ETOH extract of whole plant isolated three novel 14-membered cyclopeptide alkaloids, justicianenes B-D (1-3). (see study below) (28)
• Study of n-BuOH portion of alcoholic extract isolated eight compounds, identified as: hirsutrin (1), isorhamnetin-3-O-ß-D-rutinoside (2), tachioside (3), vanillic acid (4), ferulic acid (5), deoxyuridine (6), adenine (7), procumbenoside F (8). (29)
• Study of whole plant isolated three new arylnaphthalide lignans, 6'-hydroxy justicidin A (1), 6'-hydroxy justicidin B (2). and 6'-hydroxyjusticidin C (3), along with four known ones, neojusticin A (4). chinensinaphthol methyl ester (5), isodiphyllin (6), and taiwanin C (7). (31)
• Study of whole plant isolated six new diarylbutane lignans, namely: justin A (1), (-)-dihydroclusin diacetate (2), secoisolariciresinol dimethyl ether diacetate (3), 5-methoxy-4.4'-di-O-methylsecolaricireinol diacetate (4), justin B (5), and justin C (6), together with three known diarylbutane lignans[2.3-demethoxysecisolintertralin acetate (7), secoisolariciresinol dimethyl ether (8), and 5-methoxy-4,4'-di-O-methylsecolariciresinol (9). (33)
- Plant exudes an unpleasant odor.
- Leaves considered alterative, astringent and expectorant.
- Considered laxative and diuretic.
- Studies have suggested antiviral, cytotoxic, anticancer, antiplatelet, antithrombotic, anti-inflammatory,
antibacterial. anti-HIV, anti-asthma, fungicidal, insecticidal properties.
Leaves, whole plant.
- Used as ingredient in a Taiwan herbal tea.
- Boiled young leaves reportedly edible.
- In the Philippines, leaves are used externally as astringent for the treatment of certain skin eruptions.
- Alterative and expectorant, given as Infusion for asthma, coughs and rheumatism.
- Juice of leaves squeezed in the eyes for treatment of ophthalmia.
- Used as laxative and diuretic.
- Whole plant decoction used for backache, plethora and flatulence.
- In traditional Chinese medicine, used for fever and pain associated with pharyngolaryngeal swelling. Also used for cancer.
• Cytotoxicity / Lignans / Anti-Cancer: Study isolated a new lignan glycoside, procumbenoside A. and 11 known compounds. Known compounds justicidin A, diphyllin, and tuberculatin showed potent cytotoxic effects against some cancer cells in vitro. Two compounds strongly enhanced tumor-necrosis factor-a. (1)
• Inhibition of Benzo(a)pyrene Hydroxylation: Study isolated five lignans: neojusticin A, neojusticin B, justicidin A, justicidin B and chinensinaphthol methyl ether; in vitro effects on rat hepatic cytochrome P450-catalyzed oxidations were studied. Results showed inhibition of monooxygenase activities differentially and neo B may have a role in diminishing the oxidative activation of benzo(a)pyrene. (2)
• Anti-Platelet Aggregation: Study isolated constituents with antiplatelet effect in human platelet-rich plasma. One compound showed strong inhibitory effect on plate aggregation induced by adrenaline in a concentration-dependent manner. (3)
• Anti-Viral Lignans: Study isolated 10 antiviral lignans from the methanolic extract of aerial parts of Justicia procumbens. Some compounds showed strong antiviral activity against vesicular stomatitis virus and low cytotoxicity against cultured rabbit lung cells. (4)
• Anti-Inflammatory: Study of alcohol extract of Justicia procumbens showed promising anti inflammatory activity at a dose of 100 mg/kg weight. (5)
• Cytotoxicity: Study of a methanolic extract of the whole plant showed significant inhibitory activity in vivo against lymphocytic leukemia growth in male mice and in vitro cytotoxicity in human nasopharyngeal carcinoma cell culture assay. (8)
• Justicidin / Tumor Necrosis Factor Inhibition: Exposure of macrophages to liposaccharide induces release of tumor necrosis factor-alpha. Study isolated justicidin which was found to inhibit LPS-stimulated TNF-alpha release from RAW 264.7 macrophages in a concentration- and time-dependent manner. (7)
• Justicidin A / Apoptosis in Human Colorectal Cancer Cells: Justicidin A, an arylnaphthalide lignan significantly inhibited the growth of human colorectal cancer cells HT-29 and HCT-116, causing cell death by apoptosis. Results of the study in mice suggest a chemotherapeutic potential of justicidin A on colorectal cancer cells. (9)
• JR6 / Apoptosis in Human Bladder Cancer: Study identified a new compound 6′-hydroxy justicidin A (JR6) from Justicia procumbens which showed obvious anti-cancer effects. Results showed JR6 may be inducing intrinsic and extrinsic apoptosis pathways. JR6 induced apoptosis through caspase-dependent pathway in human bladder cancer EJ cells, presenting a potential novel pathway to bladder cancer therapy. (11)
• Pesticidal Against Plutella xylostella: Plutella xylostella is an agricultural pest of cruciferous vegetables, causing damage throughout the year. Study of methanol extracts of J. procumbens showed strong concentration related contact toxicity to P. xylostella. LC50 against 3rd instar larvae were 5.17, 4.05, and 3.06 mg/mL within 1, 2, and 3 days after treatment, respectively, while IC50 were 2.02 and 1.40 mg/mL within 1 and 2 days after treatment. The extracts showed strong antifeedant effects and a significant growth inhibitory effect on larval growth of Px. The ME showed a significant dose-dependent repelling effect on adult oviposition of Px. Overall, results showed significant insecticidal activity against Px and a potential for development of a botanical pesticide with high efficacy and low non-target toxicity. (13)
• Cytotoxicity / Lignans: Study yielded three new lignans, a novel natural product, Juspurpudine, and twelve known lignans. Eight of the compounds showed in-vitro cytotoxic activity
against Human LoVo and BGC-823 cell. (see constituents above) (14)
• Suppression of Th2 Cytokines and Amelioration of Induced Airway Inflammation / Anti-Asthma: Study evaluated an anhydrous ethanol extract of J. procumbens (DW2008) for anti-asthmatic activity. Analysis showed major peaks of Justicidin A and B which significantly suppressed Th2 cytokine levels in mouse spleen cells and exhibited a protective effect in ovalbumin-induced airway inflammation and airway responsiveness in a mouse model, suggesting potential as an anti-asthmatic agent. (15)
• Antiplatelet Arylnaphthalide Lignans: Fractionation of the ETOH extract of J. procumbens isolated nine known arylnaphthalide lignans and a new arylnaphthalide lignan characterized as 4'-demethylchinensinaphthol methyl ether (7). Compounds 1, 2, 4, and 8 significantly inhibited platelet aggregation. (see constituents above) (17)
• DW2008S / Antiasthmatic Effect: Previous study showed an ethanolic extract of J. procumbens ameliorated ovalbumin-induced airway inflammation and airway hyperresponsiveness in a mouse model of asthma. This study the antiasthmatic effect and mechanism of action of DW2008S. Study showed DW2008S contains two major ingredients, justicidin A (JA) and justicidin B (JB), which selectively inhibit T helper 2 (Th2) cell responses in concanavalin A-activated spleen cells and polarized Th2 cells. Results suggest DW2008 can potentially ameliorate Th2-driven airway inflammation and bronchoconstriction through negative regulation of TIGIT and blockage of A3 AR and PDE4 activities. (19)
• Cyclopeptide Alkaloids / Cytotoxicity: Study isolated a new cyclopeptide alkaloid, justicianene A (1) and a new lignan glycoside, procumbenoside H (2). Cyclopeptide alkaloids were first observed from the genus Justicia. Compound 2 exhibited cytotoxicity against human LoVo colon carcinoma cells with IC50 of 17.908 ± 1.949 µM. (20)
• Antibacterial / Lignans and Triterpenoids / Whole Plant: Study of whole plant isolated one new lignan, four known lignans, and four known triterpenoids from whole plant of Rostellularia procumbens. The nine compounds were evaluated for antibacterial activity against eight bacterial strains by agar dilution method. Results showed antimicrobial activity with MICs in the range of 1.56-100 µg/mL. (see constituents above) (21)
• Cytotoxic Constituents / Lignans: The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazplium bromide assay showed the ethyl acetate extract of J. procumbens had cytotoxic activity. Study showed the cytotoxic activity could be mainly attributed to lignans. Results suggest potential for the chemical constituents as novel therapeutics. (22)
• Anti-HIV Lignans: Study of J. procumbens isolated 21 lignans including three new ones (1, 2, and 13). The compounds were evaluated for cytotoxic and anti-HIV activities. The new secoisolariciresinol dimethyl ether acetate (13) exhibited anti-HIV-1 activity with IC50 of 5.27 µmol-L and a selective index (SI) value of 2.2. The known arylnaphthalene lignan procumbenoside A (3) and diphyllin (8) exhibited inhibitory activity against HIV-1 with IC50s of 4.95 (SI>6.2) and 0.38 µmol-L (SI=5.3), respectively. (23)
• Antiviral / Arylnaphthalene (ANL) Lignan Glycosides / Stems and Bark: Phytochemical separation of methanol extract of stems and barks isolated 11 ANL glycosides including four pairs of new atropisomers. The ANL compounds displayed great antiviral activity discrepancy between a pair of atropisomers due to geometric orientation. The biologic activity discrepancy caused by axial chirality will inspire synthetic design of novel ANL atropisomers and provide hints to direct synthetic approaches towards antiviral drug development of ANL compounds. (24)
• Antitumor / 6'-Hydroxy Justicidin A (HJA): Study isolated 6'-hydroxy justicidin A (HJA). a potential antitumor active compound from J. procumbens in rat plasma.
• Anti-Inflammatory: Study evaluated a 95% alcohol extract of Justicia procumbens for in vivo anti-inflammatory activity in albino rats. Anti-inflammatory activity was based on plethysmographic measurement of edema produced by sub-plantar injection of formalin in the hind paw of the rats. Results showed promising activity at a dose of 100 mg/kbw. (26)
• Fungicide / Insecticide: Study evaluated various extracts of Justicia procumbens for fungicidal and insecticidal activity. Results showed 8 mg/ml extract of J. procumbens with different polar solvents showed some inhibitory effects on five species of plant pathogenic fungus. Inhibition rates against C. gloeospriodes, P. asparagi and B cinerea were over 50%. A methanol extract showed better fungicial and insecticidal activity, Results suggest potential application as biological agricultural pesticide. (27)
• Cyclopeptide Alkaloids / Cytotoxicity against Cancer Cell Lines / Whole Plant: Study of ETOH extract of whole plant isolated three novel 14-membered cyclopeptide alkaloids, justicianenes B-D (1-3). The compounds were evaluated for cytotoxicity against human cancer cell lines, including breast cancer MCF-7. cervix carcinoma HeLa, lung cancer A549, and H460. Results showed moderate cytotoxicity against the HeLa, A549, and H460 cells with IC50s of 9.13, 23.12, 42.34 µM, respectively. Justicianene D showed weak cytotoxicity against MCZF-7 cells with inh8biition of 50% t 90µM. (28)
• HJC - Arylnaphthalene Lignan / K562 Leukemic Cells: Study isolated and evaluated HJC for ability to suppress proliferation and induce apoptosis of human leukemic K562 cells and its related mechanism. Assays showed HJC remarkable inhibited the growth in KK562 cells by decreasing cell proliferation, reducing SOD activity, enhancing ROS levels, and inducing apoptosis. Activation of caspase-3 indicated HJC may induce intrinsic and extrinsic apoptosis pathways and the HJC apoptosis may be caspase-dependent. Results suggest high-potency antitumor effect and induces apoptosis through a caspase dependent pathway in human leukemia K562 cells. It suggests potential as alternative in leukemia therapy. (30)
• Herbal Ophthalmic Ointment for Allergic Conjunctivitis: Study evaluated various leaves extracts for formulation of a herbal ophthalmic ointment for inflammation of the eye in albino rabbits.
All extracts were subjected to in-vitro antioxidant and in-vitro anti-inflammatory activity. The ethanolic extract showed maximum antioxidant potential and maximum inhibition in protein denaturation method. The ointment at dose of 20 mg (0.4% w//w) showed significant anti-inflammatory effect on induced conjunctivitis, comparable to standard bethamethasone (0.05% w/w). (32)
• Anti-Platelet Aggregation / Neojusticin B: Study evaluated bioactive ingredients (chinensinaphthol methyl ether and neojusticin B) and target protein of Rostellularia procumbens. Results showed the ethyl acetate extract could inhibit platelet aggregation. Chinensinaphthol methyl ester and neojusticin B may target the integrin aIIbß3 protein. (34)
• Antithrombotic / Antiplatelet Aggregation: Study evaluated the antithrombotic and antiplatelet effect of Rostellularia procumbens extract. Antithrombotic effective parts (RPE) and potential active ingredients (JAC) were isolated. RPE and JAC showed no toxicity to platelets. In vitro studies showed RPE and JAC had antiadhesion effects on platelets. In vivo studies showed RPE significantly inhibited the increase of p-selectin and TXB2 and significantly increased the content of 6-keto-PGF1α in the serum of rats. RPE exhibited antithrombotic and antiplatelet activity in vivo and in vitro, possibly via prevention of integrin and αIIbß3 activation, which leads to inhibition of phosphorylation of MAPK family and further suppression of TXA2, which leads to antithrombotic and antiplatelet effects. (35)